78 results on '"Rongrui Wei"'
Search Results
2. Development of novel salicylic acid–donepezil–rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer’s disease
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Yi Zhou, Ying He, Xue Teng, Jing Mi, Jing Yang, Rongrui Wei, Wenmin Liu, Qinge Ma, Zhenghuai Tan, and Zhipei Sang
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Alzheimer’s disease ,salicylic acid–donepezil–rivastigmine hybrids ,multi-functional agent ,drug-likeness ,scopolamine-induced AD model ,Therapeutics. Pharmacology ,RM1-950 - Abstract
Alzheimer’s disease (AD) is a chronic, progressive brain degenerative disease that is common in the elderly. So far, there is no effective treatment. The multi-target-directed ligands (MTDLs) strategy has been recognised as the most promising approach due to the complexity of the pathogenesis of AD. Herein, novel salicylic acid–donepezil–rivastigmine hybrids were designed and synthesised. The bioactivity results exhibited that 5a was a reversible and selective eqBChE inhibitor (IC50 = 0.53 μM), and the docking provided the possible mechanism. Compound 5a also displayed potential anti-inflammatory effects and significant neuroprotective effect. Moreover, 5a exhibited favourable stabilities in artificial gastrointestinal solution and plasma. Finally, 5a demonstrated potential cognitive improvement in scopolamine-induced cognitive dysfunction. Hence, 5a was a potential multifunctional lead compound against AD. more...
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- 2023
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3. Efficacy of Lagopsis supina to promote blood circulation, remove blood stasis, and block inflammation in a rat model of traumatic blood stasis
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Tingting Xu, Xiumei Wang, Zhongwei He, Li Yang, Rongrui Wei, Guoyue Zhong, and Junwei He
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Lagopsis supina ,Promoting blood circulation and removing blood stasis (PBCRBS) ,Anti-inflammatory ,Traumatic blood stasis (TBS) ,Pharmacy and materia medica ,RS1-441 - Abstract
Abstract Lagopsis supina (Steph) IK. Gal. was a traditional Chinese medicinal plant for promoting blood circulation and removing blood stasis (PBCRBS), anti-inflammatory and diuresis with little scientific validation. The aims of this study were first to evaluate the PBCRBS and anti-inflammatory effects of L. supina in a rat model of traumatic blood stasis (TBS). We demonstrated that an ethanolic extract of L. supina (LS, 460 mg/kg/d) possessed significant PBCRBS and remarkable inhibitory effect on inflammation cytokines, which were associated with renovated amount of the injured muscle fibers, alleviate the degree of the damaged tissue edema, decreased the number of inflammatory cells, increased the number of the capillary hyperplasia by hematoxylin and eosin (HE), as well as remarkably down-regulated ( p < 0.05 or p < 0.01) the levels of inflammation cytokines, including TNF-α, IL-6, IL-8, and IL-10 by ELISA. This finding provide a pharmacological basis and partial interpretation for the clinical application of L. supina, which has therapeutic properties for blood stasis syndrome (BSS) and inflammation-related diseases. more...
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- 2022
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4. Protective effect of the ethyl acetate fraction of Qinghai-Tibet Plateau medicinal plant Chrysosplenium axillare Maxim. against ANIT-induced cholestatic liver injury in mice
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Ziyan Cai, Wenyan Li, Wei Jiang, Jixiao Zhu, Guoyue Zhong, Rongrui Wei, Zejing Mu, and Gang Ren
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Chrysosplenium axillare Maxim. ,α-Naphthylisothiocyanate ,Acute intrahepatic cholestasis ,Therapeutic agents, Mechanism ,Phytochemical analysis ,Other systems of medicine ,RZ201-999 - Abstract
Background: Chrysosplenium axillare Maxim. has been used as a traditional Tibetan herb medicine for hepatobiliary disorder in Qinghai-Tibet Plateau for more than one thousand years. Hypothesis/purpose: we hypothesized that the ethyl acetate-soluble portion extracted from C. axillare (ECA) could exert hepatoprotection effect against α-naphthylisothiocyanate (ANIT)-induced hepatotoxity and acute intrahepatic cholestasis in mice and aimed to investigate its potential mechanism. Study design: male KM mice with acute intrahepatic cholestasis induced by ANIT were orally administered with the ECA (100 and 50 mg/kg B.W.). Mice receiving vehicle (0.5% CMC-Na) served as control. Methods: 48 h after ANIT administration, mice were sacrificed. Blood was collected for serum enzymes and components analysis using commercial kits. Livers were removed for histopathological examination and protein preparation. The protein expression levels of farnesoid X receptor (FXR), bile-salt export pump (BSEP), multidrug resistance associated protein2 (MRP2), Na+-taurocholate co-transporting polypeptide (NTCP), small heterodimer partner (SHP), and cholesterol 7α-hydroxylase (CYP7A1) were evaluated by a western blot analysis. A phytochemical analysis was conducted to characterize the chemical constituents of ECA. Results: oral administration of ECA at both doses (P < 0.05 or P < 0.01) can prevent ANIT-induced increases in levels of serum enzymes and components, including AST, ALT, ALP, DBIL, TBA, and TBIL and improve the liver pathologic change induced by ANIT exposure. Western blot analysis showed that the expression levels of FXR, BSEP, MRP2, NTCP, and SHP in ECA (100 and 50 mg/kg) groups were up-regulated versus model group (P < 0.05 or P < 0.01), and those of CYP7A1 in both ECA treated groups were down-regulated versus model group (P < 0.01). One new highly O-methylated flavonoids, chrysosplenoside I (1), together with fourteen analogues (2–15), was isolated from ECA and structurally identified by spectra analysis. Among them, the two abundant ingredients, chrysosplenosides A and I (11 and 1), were quantitatively determined to have a total content account for 32.2% of ECA. Conclusion: ECA protected against mice liver damage with acute intrahepatic cholestasis induced by ANIT via regulation of the expression of hepatic proteins involved in bile acids synthesis, transportation and re-absorption. These results confirmed the hepatoprotective efficacy of traditional Tibet herb medicine C. axillare and provided the first insight into its related mechanism as well as the potential active ingredients. more...
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- 2021
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5. A Comprehensive Review on Extraction, Structure, Detection, Bioactivity, and Metabolism of Flavonoids from Sea Buckthorn (Hippophae rhamnoides L.)
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Nengxin He, Qinyuan Wang, Huilian Huang, Jie Chen, Guang Wu, Meining Zhu, Feng Shao, Zhihong Yan, Zhipei Sang, Lan Cao, Rongrui Wei, and Qinge Ma
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Pharmacology ,Biophysics ,Cell Biology ,Food Science - Abstract
Sea buckthorn (Hippophae rhamnoides L.) is an important plant with homology of medicine and food. It has rich nutritional and medicinal properties. It is used as a traditional Chinese medicine with therapeutic functions of invigorating spleen, relieving cough, eliminating food, eliminating phlegm, dispersing blood stasis, and promoting blood circulation. This review comprehensively summarized flavonoids from sea buckthorn (Hippophae rhamnoides L.), including extraction methods (solvent extraction, ultrasound-assisted extraction, microwave-assisted extraction, enzyme-assisted extraction, and collaborative extraction), two structure types (18 flavone aglycones and 81 flavone glycosides), detection methods (UV, HPLC, and NMR), bioactivities (antiviral, anti-inflammatory, hepatoprotective, weight-reducing, and hypoglycemic activities), and physiological metabolisms (most of flavonoids are converted into small molecule monophenolic acids through intestinal microbial catabolism). It will supply an important theoretical basis and valuable reference for researching and exploiting sea buckthorn (Hippophae rhamnoides L.) in the future. Practical Applications. Sea buckthorn (Hippophae rhamnoides L.) is an edible and medical plant with many functional properties. A comprehensive review on extraction, structure, detection, bioactivity, and metabolism of flavonoids from sea buckthorn (Hippophae rhamnoides L.) was made in this paper. This review will provide an important foundation for further studies of sea buckthorn (Hippophae rhamnoides L.) focusing on its development and utilization. more...
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- 2023
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6. Coumarin-Xanthone Derivatives with Hepatoprotective Activities from Pyrethrum tatsienense
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Rongrui Wei and Qinge Ma
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Plant Science ,General Chemistry ,General Biochemistry, Genetics and Molecular Biology - Published
- 2023
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7. A New C19-Diterpenoid Alkaloid from Salted Aconiti Lateralis Radix Praeparata
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Rongrui Wei, Lihua Chen, and Qinge Ma
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Plant Science ,General Chemistry ,General Biochemistry, Genetics and Molecular Biology - Published
- 2022
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8. Isolation and Characterization of Anti-Inflammatory Lignans from Oenanthe javanica
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Rongrui Wei and Qinge Ma
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Plant Science ,General Chemistry ,General Biochemistry, Genetics and Molecular Biology - Published
- 2022
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9. Isolation and characterization of auronlignan derivatives with hepatoprotective and hypolipidemic activities from the fruits of Hippophae rhamnoides L
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Qinge Ma, Yang Guan, Zhipei Sang, Jianghong Dong, and Rongrui Wei
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General Medicine ,Food Science - Abstract
The fruit of Hippophae rhamnoides L. is not only used as delicious food with nutritional values, but also served as traditional Chinese medicine with multiple bioactivities.
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- 2022
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10. Front Cover: Lipskynoids A–G, New Acyclic Diterpenes from the Flowers of Carpesium lipskyi (Chem. Biodiversity 12/2022)
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Weihong Zhong, Min Li, Rui Gu, Rong Ding, Lan Cao, Zejing Mu, Xiaolang Du, Yulin Feng, Rongrui Wei, Liujuan Zhan, and Guoyue Zhong
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Molecular Medicine ,Bioengineering ,General Chemistry ,General Medicine ,Molecular Biology ,Biochemistry - Published
- 2022
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11. A New Anthraquinone-Aurone Adduct with Hepatoprotective Activity from the Fruits of Cucumis bisexualis
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Qinge Ma and Rongrui Wei
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biology ,Stereochemistry ,Plant Science ,General Chemistry ,biology.organism_classification ,Anthraquinone ,General Biochemistry, Genetics and Molecular Biology ,In vitro ,Adduct ,chemistry.chemical_compound ,chemistry ,Hepg2 cells ,Aurone ,Inhibitory effect ,Cucumis - Abstract
A previously undescribed anthraquinone-aurone adduct 1, named 8-(4′-hydroxy-3′,5′-dimethoxyphenyl)-12-hydroxy-7-(6′′,7′′-dimethylfuran-2′′-one)-9,16-anthraquinone-furochromene-3,2′′-dione, was isolated from the fruits of Cucumis bisexualis. Its structure was determined by comprehensive spectroscopic data and references. Compound 1 was evaluated for its inhibitory effect against the increase in AST and ALT levels in H2O2-induced HepG2 cells in the range of their maximum nontoxic concentration. Compound 1 exhibited moderate hepatoprotective activities in vitro. more...
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- 2021
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12. Lipskynoids A–G, New Acyclic Diterpenes from the Flowers of Carpesium lipskyi
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Weihong Zhong, Min Li, Rui Gu, Rong Ding, Lan Cao, Zejing Mu, Xiaolang Du, Yulin Feng, Rongrui Wei, Liujuan Zhan, and Guoyue Zhong
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Molecular Medicine ,Bioengineering ,General Chemistry ,General Medicine ,Molecular Biology ,Biochemistry - Abstract
Seven new acyclic diterpenes, namely lipskynoids A-G (1-7), were isolated from the flowers of Carpesium lipskyi, a traditional Tibetan herbal medicine with anti-inflammatory and antipyretic-analgesic effects. These new compounds were elucidated by analysis of extensive spectroscopic data including ESI-MS, 1D, 2D NMR, and DP4+ analyses. Biological assays showed that 1-7 display significant inhibitory effects against the NO production in LPS-induced RAW264.7 cells with its IC more...
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- 2022
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13. Isolation and Characterization of Hepatoprotective Anthraquinone Derivatives from Cucumis bisexualis
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Qinge Ma and Rongrui Wei
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chemistry.chemical_compound ,chemistry ,biology ,Stereochemistry ,Positive control ,Anthraquinone Derivatives ,Plant Science ,General Chemistry ,Isolation (microbiology) ,biology.organism_classification ,Anthraquinone ,Cucumis ,General Biochemistry, Genetics and Molecular Biology - Abstract
A new anthraquinone, named 1,3-dihydroxy-2-methylene-(1′-isopentyloxy)-6-methoxymethyl-8-(6′′,7′′,8′′- trihydroxyphenylketonyl)-9,10-anthraquinone (1), and nine known anthraquinone derivatives (2–10), were isolated from Cucumis bisexualis for the first time. Compounds 1–10 were evaluated for their hepatoprotective activity in human L-O2 cells compared with the positive control bifendatatum. Among them, compounds 1, 3, and 8 exhibited moderate hepatoprotective activity in the proliferation of L-O2 cells. more...
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- 2021
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14. Anti-Inflammatory Phenylpropanoid Derivatives from the Aerial Parts of Oenanthe javanica
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Qinge Ma, Rongrui Wei, Zhipei Sang, and Yang Guan
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food.ingredient ,food ,Traditional medicine ,Phenylpropanoid ,Chemistry ,medicine.drug_class ,Oenanthe javanica ,medicine ,Plant Science ,General Chemistry ,General Biochemistry, Genetics and Molecular Biology ,Anti-inflammatory - Published
- 2021
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15. Flavonolignan 2, 3-dehydroderivatives from Oenanthe javanica and their anti inflammatory activities
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Qinge Ma and Rongrui Wei
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Lignan ,food.ingredient ,Traditional medicine ,010405 organic chemistry ,medicine.drug_class ,01 natural sciences ,General Biochemistry, Genetics and Molecular Biology ,Anti-inflammatory ,0104 chemical sciences ,Flavonolignans ,010404 medicinal & biomolecular chemistry ,chemistry.chemical_compound ,food ,chemistry ,Oenanthe javanica ,medicine ,Ic50 values ,Flavonolignan - Abstract
Flavonolignans, for example, silymarin and silybin, have interesting biological activities. For the first time, three new flavonolignans named oenanthenoid A-C (1–3) and nine known flavonolignan derivatives (4–12) were isolated from Oenanthe javanica. Comprehensive spectroscopic data analysis and references were used to identify all of the compounds. The anti inflammatory activities of these isolates (1–12) on RAW264.7 macrophage cells were investigated. Three new compounds (1–3) demonstrated anti inflammatory activity with IC50 values ranging from 6.5 ± 0.6 to 14.7 ± 1.6 µM. Furthermore, two compounds (11 and 12) demonstrated moderate anti inflammatory activity, with IC50 values ranging from 24.1 ± 1.2 to 62.5 ± 1.9 µM. more...
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- 2021
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16. Design, synthesis and biological evaluation of Schiff’s base derivatives as multifunctional agents for the treatment of Alzheimer’s disease
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Zhipei Sang, Zhanpin Qiao, Rongrui Wei, Yumin Leng, Qingfeng Li, Yiyang Zhao, Jian Shi, Wenmin Liu, Yi Zhou, Wang Keren, Qinge Ma, and Shuang Liu
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Antioxidant ,010405 organic chemistry ,Chemistry ,Monoamine oxidase ,medicine.medical_treatment ,Organic Chemistry ,01 natural sciences ,Combinatorial chemistry ,Metal Chelator ,Neuroprotection ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,Design synthesis ,Docking (molecular) ,medicine ,Molecule ,Bioorganic chemistry ,General Pharmacology, Toxicology and Pharmaceutics - Abstract
A series of Schiff’s base derivatives was rationally designed, synthesized, and evaluated as multi-function agents for the treatment of Alzheimer’s disease (AD). The results revealed that compound 3b was a novel multifunctional agent. It acted as a highly selective monoamine oxidase-B inhibitor (IC50 = 8.4 nM), which was explained by the docking study. Compound 3b also was an antioxidant agent (2.3 eq) and could significantly inhibit self-induced Aβ1-42 aggregation (31.8%). Meanwhile, compound 3b was a selective metal chelator and could inhibit Cu2+-induced Aβ1-42 aggregation (62.3%). Furthermore, compound 3b presented good neuroprotective effects on H2O2-induced PC12 cell injury. More importantly, compound demonstrated good blood brain barrier permeability and druglike properties. Therefore, compound 3b, a promising multi-targeted active molecule, offers an attractive starting point for further study in the drug-discovery process against AD. more...
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- 2020
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17. Hypolipidemic Activity of Monacolin Derivatives from the Highland Barley Monascus purpureus
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Qinge Ma, Guoyue Zhong, Wei Jiang, Zhipei Sang, and Rongrui Wei
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2019-20 coronavirus outbreak ,biology ,Coronavirus disease 2019 (COVID-19) ,010405 organic chemistry ,Chemistry ,Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) ,Plant Science ,General Chemistry ,biology.organism_classification ,01 natural sciences ,General Biochemistry, Genetics and Molecular Biology ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,Triglyceride content ,Hepg2 cells ,Monascus purpureus ,Food science - Abstract
A new monacolin derivative, namely (1S,2S,5′R,6R,8aR)-7-hydroxy-2,6-dimethyl-8-prenyl-1,2,6,8atetrahydronaphthalene-4′,5′-dihydro-2H-pyran-1′-one (1), and five known monacolin derivatives (2–6) were separated from the highland barley Monascus purpureus Went. for the first time. Their structures were elucidated on the basis of 1D and 2D NMR, HR-ESI-MS, and relevant references. Compounds 1–6 were tested for their hypolipidemic activities by measuring the triglyceride content in HepG2 cells. Among them, compounds 1 and 2 (10 μM) exhibited moderate hypolipidemic activity. more...
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- 2020
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18. Two New Flavones from Salvia plebeia and Their Anti-Angiogenic Activities
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Qi-Xin Lu, Qinge Ma, Rongrui Wei, Hao-Feng Huang, Lin Jiang, and Dong-Mei Guo
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chemistry.chemical_classification ,Traditional medicine ,biology ,010405 organic chemistry ,Anti angiogenic ,Positive control ,Plant Science ,General Chemistry ,biology.organism_classification ,01 natural sciences ,Flavones ,General Biochemistry, Genetics and Molecular Biology ,0104 chemical sciences ,Axitinib ,010404 medicinal & biomolecular chemistry ,chemistry ,Ic50 values ,medicine ,MTT assay ,Salvia plebeia ,Two-dimensional nuclear magnetic resonance spectroscopy ,medicine.drug - Abstract
Two new flavones, namely 5-hydroxy-2-(4′-hydroxyphenyl)-6,12,13-trimethoxypyrano-xanthene-4,9-dione (1) and 5-hydroxy-2-(3′-methoxy-4′-hydroxyphenyl)-6-methoxy-11-isopropyl-pyranochromene-4,9-dione (2), were isolated from Salvia plebeia. Their structures were elucidated by spectroscopic methods, including extensive 1D and 2D NMR spectral data. Compounds 1 and 2 were evaluated for their anti-angiogenic activities by the MTT assay with axitinib as positive control, and they displayed moderate anti-angiogenic activities with IC50 values of 14.07 and 11.25 μM, respectively. more...
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- 2020
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19. Indole Alkaloids from Hosta plantaginea and Inhibition of Steroid 5α-Reductase Activities In Vitro
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Qinge Ma and Rongrui Wei
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Indole test ,Indole alkaloid ,010405 organic chemistry ,Chemistry ,medicine.medical_treatment ,Plant Science ,General Chemistry ,01 natural sciences ,General Biochemistry, Genetics and Molecular Biology ,In vitro ,0104 chemical sciences ,Steroid ,010404 medicinal & biomolecular chemistry ,Biochemistry ,medicine ,Steroid 5α reductase ,Hosta plantaginea - Abstract
A new indole alkaloid (1), together with eight known indole alkaloid derivatives (2–9), was isolated from Hosta plantaginea for the first time. The structures of compounds 1–9 were elucidated on the basis of comprehensive spectroscopic analyses and references. Compounds 1–9 were evaluated for their inhibition of steroid 5α-reductase activity in vitro. Among them, compounds 1 and 2 showed important inhibition of steroid 5α-reductase activities. more...
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- 2020
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20. Hypolipidemic Lactone Derivatives from Highland Barley Monascus
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Qinge Ma and Rongrui Wei
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chemistry.chemical_classification ,biology ,010405 organic chemistry ,Chemistry ,Positive control ,Plant Science ,General Chemistry ,Monascus ,biology.organism_classification ,01 natural sciences ,General Biochemistry, Genetics and Molecular Biology ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,Triglyceride content ,Simvastatin ,Hepg2 cells ,medicine ,Food science ,Lactone ,medicine.drug - Abstract
A new lactone, named 9-allyl-5-methyl-1H-difuro-isochromene-1,8-dione (1), together with nine known lactone derivatives (2–10), was isolated from highland barley Monascus for the first time. Compounds 1–10 were studied by spectroscopic methods and comparison with references and evaluated for their hypolipidemic activities by measuring the triglyceride content in HepG2 cells with simvastatin as positive control. Among them, compounds 1 and 7 (10 μM) exhibited moderate hypolipidemic activities. more...
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- 2020
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21. Neuroprotective Flavonoids from the Aerial Parts of Gynura cusimbua
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Zhipei Sang, Rongrui Wei, Guoyue Zhong, and Qinge Ma
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biology ,Traditional medicine ,Chemistry ,Plant Science ,General Chemistry ,Gynura ,biology.organism_classification ,Neuroprotection ,General Biochemistry, Genetics and Molecular Biology - Published
- 2020
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22. Structurally Diverse Flavonolignans with Immunosuppressive and Neuroprotective Activities from the Fruits of Hippophae rhamnoides L
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Qinge Ma, Dong-Li Shang, Jiang-Hong Dong, Rongrui Wei, and Zhipei Sang
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0106 biological sciences ,Traditional medicine ,biology ,Chemistry ,010401 analytical chemistry ,Hippophae rhamnoides ,General Chemistry ,biology.organism_classification ,Cell survival rate ,01 natural sciences ,Neuroprotection ,0104 chemical sciences ,Flavonolignans ,Phytochemical ,Flavonolignan ,Ic50 values ,General Agricultural and Biological Sciences ,010606 plant biology & botany - Abstract
The fruit of Hippophae rhamnoides L. has been used for centuries in Europe and Asia as a food with high nutritional and medicinal values. In this study, a bioactivity-guided phytochemical investigation of H. rhamnoides L. has resulted in four new dimethylallylated flavonolignans (1-4), four new isopropylpentenone-flavonolignan heterodimers (5-8), two new geranylated flavonolignans (9 and 10), and 14 known flavonolignan derivatives (11-24); they were elucidated by their spectrometric and spectroscopic methods, including HR-ESI-MS, NMR, IR, and UV from the fruit of H. rhamnoides L. for the first time. Among them, compounds 2, 5, 6, 20, and 21 showed potent immunosuppressive activities with IC50 values from 19.42 ± 3.91 to 48.05 ± 12.56 μM. Meanwhile, compounds 1, 4, 11, 12, and 13 showed moderate neuroprotective activities, which increased the cell survival rate from 50.30 ± 4.24% for the model group to 71.63 ± 3.04%, 70.02 ± 4.13%, 61.53 ± 5.93%, 61.08 ± 3.58%, and 65.68 ± 4.88% at 10 μM, respectively. The hypothetical biogenetic pathway and preliminary structure-activity relationship were found and discussed scientifically. more...
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- 2020
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23. Antidepressive Azaanthracene Alkaloids from Corydalis decumbens
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Qinge Ma, Rongrui Wei, and Zhipei Sang
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Traditional medicine ,010405 organic chemistry ,Chemistry ,Alkaloid ,Plant Science ,General Chemistry ,Corydalis decumbens ,Rat brain ,01 natural sciences ,General Biochemistry, Genetics and Molecular Biology ,0104 chemical sciences ,Reuptake ,010404 medicinal & biomolecular chemistry ,Serotonin ,Spectral data - Abstract
A new azaanthracene alkaloid, named 1-aza-4-(4′-hydroxybenzyl)-9,10-dimethoxydioxolobenzo-2-oxo-1,2-dihydroanthracene (1), together with seven known azaanthracene alkaloid derivatives (2–8), were isolated from Corydalis decumbens for the first time. Their structures were elucidated by their spectral data and references. Compounds 1–8 were evaluated for their antidepressive activities by inhibiting reuptake of tritiated serotonin ([3H]-NE and [3H]-5-HT) in rat brain synaptosomes. Among them, compounds 1 and 2 showed moderate antidepressive activities. more...
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- 2020
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24. Hepatoprotective Xanthones from the Aerial Parts of Pyrethrum tatsienense
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Guoyue Zhong, Zhipei Sang, Qinge Ma, and Rongrui Wei
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Traditional medicine ,010405 organic chemistry ,Chemistry ,Pyrethrum tatsienense ,Plant Science ,General Chemistry ,01 natural sciences ,General Biochemistry, Genetics and Molecular Biology ,0104 chemical sciences ,Xanthone Derivatives ,010404 medicinal & biomolecular chemistry ,chemistry.chemical_compound ,Xanthone ,MTT assay - Abstract
A new xanthone, named 1,3,5,9-tetrahydroxy-2-prenyl-4-(3′′ -hydroxy-3′′ -methylbutanoyl)-6,6- dimethylpyranoxanthen-10-one (1), along with five known xanthone derivatives (2–6), were isolated from Pyrethrum tatsienense for the first time. Their structures were elucidated on the basis of extensive spectroscopic analysis and references. Compounds 1–6 were screened for their hepatoprotective activities by MTT assay against D-galactosamine induced toxicities in HL-7702 cells, which revealed that compounds 1, 4, and 5 exhibited moderate hepatoprotective activities. more...
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- 2020
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25. Two Olean-27-carboxylic Acid-Type Triterpenoids as Chemical Markers Isolated from Saxifraga umbellulata
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Wei Jiang, Ren Wu, Gang Ren, Yongwei Qiu, Xiaolang Du, Zejing Mu, Ting Tan, Shanshan Li, Bo Li, Wanzhi Li, Yaxin Hu, Qi Zhang, Rongrui Wei, and Guoyue Zhong
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Molecular Structure ,Saxifragaceae ,Carboxylic Acids ,Molecular Medicine ,Humans ,Bioengineering ,General Chemistry ,General Medicine ,Molecular Biology ,Biochemistry ,Triterpenes - Abstract
Two olean-27-carboxylic acid-type triterpenoids (1 and 2) were isolated from Saxifraga umbellulata (Saxifragaceae), representing the first case in the chemical discoveries of genus Saxifraga. Compound 1 was determined to be a new compound named 'Saxifragic acid' based on the comprehensive spectroscopic and X-ray crystallographic analyses. Compound 2 (deacetylated saxifragic acid) is a known compound reported before, but its absolute configuration through X-ray crystallographic analyses was first described here. In addition, their cytotoxicity against five digestive human cancer cell lines (BGC-823, GBC-SD, CCC-9810, HT-29, and HepG2) and hepatoprotective activity against CCl more...
- Published
- 2021
26. Structurally diverse Monascus pigments with hypolipidemic and hepatoprotective activities from highland barley Monascus
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Zhi-Pei Sang, Qinge Ma, Jiang-Hong Dong, Rongrui Wei, and Mao-Hua He
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Spectrometry, Mass, Electrospray Ionization ,Lipid accumulation ,Gas Chromatography-Mass Spectrometry ,Mass Spectrometry ,chemistry.chemical_compound ,Pigment ,Structure-Activity Relationship ,Drug Discovery ,Spectroscopy, Fourier Transform Infrared ,Structure–activity relationship ,Food science ,Benzofuran ,Fermentation in food processing ,Hypolipidemic Agents ,Pharmacology ,biology ,Chemistry ,Hordeum ,General Medicine ,Pigments, Biological ,Monascus ,biology.organism_classification ,Solid-state fermentation ,Liver ,Hepg2 cells ,visual_art ,visual_art.visual_art_medium ,Spectrophotometry, Ultraviolet - Abstract
Highland barley Monascus has historically been used in solid state fermentation and traditional fermented foods in Tibet. It is possessed of the characteristics of medicine and food. Three new 8,13-unsaturated benzocyclodiketone-conjugated Monascus pigments (1–3), three new benzofuran Monascus pigments (4–6), three new butylated malonyl Monascus pigments (7–9), and eleven known Monascus pigment derivatives (10−20) were isolated from highland barley Monascus for the first time. Their structures were determined by analyzing NMR, MS, UV, and IR spectral data and compared with relevant references. Among them, compounds 2, 4, 6 showed important inhibition of pancreatic lipase activity, and decreased significantly FFA-induced lipid accumulation in HepG2 liver cells. Additionally, compounds 1, 10, 14, 16, 18 exhibited certain hepatoprotective activities against the damage in acetaminophen-induced HepG2 cells. The plausible biogenetic pathway and preliminary structure activity relationship of the selected compounds were scientifically summarized and discussed in this work. more...
- Published
- 2021
27. Structural characterization, hepatoprotective and antihyperlipidemic activities of alkaloid derivatives from Murraya koenigii
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Meiling Wang, Ai-Guo Wang, Qinge Ma, Haichao Wu, Jian-Bo Yang, Teng-Fei Ji, Rongrui Wei, Guoyue Zhong, Hongxia Guo, Ping Jiang, and Yulun Su
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Murraya ,biology ,Traditional medicine ,010405 organic chemistry ,Chemistry ,Alkaloid ,Plant Science ,biology.organism_classification ,01 natural sciences ,Biochemistry ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,Agronomy and Crop Science ,Biotechnology - Abstract
Three new alkaloids (1-3) and a new natural alkaloid (4), named (1′R,3′R,4′R,6′S)-endocycliomurrayamine-A (1), 3-formyle-7-hydroxy-9H-carbazole-1-O-β- d -glucopyranoside (2), 4′-hydroxyphenyl-6-ethyl-1H-pyrrole-2-carboxaldehyde (3), and 4-hydroxyphenoxy-N-methyl-propanamide (4), together with thirteen known alkaloid derivatives (5–17) were isolated from Murraya koenigii. Among them, compounds (8–17) were isolated from this plant for the first time. The structures of compounds (1–17) were elucidated on the basis of their spectroscopic analysis and references. Compounds 1, 15, 16, and 17 (10 μM) showed moderate hepatoprotective activities against d -galactosamine-induced HL-7702 cells damage. Compounds 2, 3, 9, and 13 showed moderate activation of PPARα and PPARγ receptors. more...
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- 2020
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28. Anti-Ache Benzylbenzofuran Derivatives from Silene conoidea
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Ma Qinge, Guoyue Zhong, and Rongrui Wei
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biology ,Aché ,Stereochemistry ,Chemistry ,language ,Ic50 values ,Plant Science ,General Chemistry ,Spectral data ,biology.organism_classification ,General Biochemistry, Genetics and Molecular Biology ,language.human_language ,Silene conoidea - Abstract
A new benzylbenzofuran, named 5′,7-dihydroxy-6-propenyl-2-(11′,12′-dimethylpyran)-benzylbenzofuran (1), and seven known benzylbenzofuran derivatives (2–8) were isolated from Silene conoidea L. for the first time. The structures of compounds 1–8 were identified by their spectral data and reference data. Compounds 1–8 were evaluated for anti-acetylcholinesterase (AChE) activities for the first time. Compounds 1, 2, 5, and 6 showed anti-AChE activities with IC50 values ranging from 12.55–85.43 μM. more...
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- 2019
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29. Hypolipidemic phenanthraquinone derivatives from Heleocharis dulcis
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Rongrui Wei, Qinge Ma, and Zhipei Sang
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Triglyceride content ,Biochemistry ,Simvastatin ,Hepg2 cells ,medicine ,Positive control ,Biology ,Ecology, Evolution, Behavior and Systematics ,medicine.drug - Abstract
Three new phenanthraquinones (1–3), together with seven known phenanthraquinone derivatives (4–10) were isolated from Heleocharis dulcis for the first time. Their structures were established on extensive NMR, MS, UV, IR experiments in conjunction with their references. Compounds (1–10) were evaluated for their hypolipidemic activities for the first time. Compounds 1, 3, 7, and 9 (10 μM) exhibited significant hypolipidemic activities by measuring the triglyceride content in HepG2 cells with simvastatin as positive control. The chemotaxonomic significance of compounds (1–10) was also discussed. more...
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- 2019
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30. Neuroprotective Aurones from Sophora japonica
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Qinge Ma, Rongrui Wei, and Zhipei Sang
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chemistry.chemical_compound ,chemistry ,Traditional medicine ,Sophora japonica ,Aurone ,Ic50 values ,Plant Science ,General Chemistry ,Neuroprotection ,General Biochemistry, Genetics and Molecular Biology - Abstract
A new aurone, named (Z)-4,5-methylenedioxy-6-hydroxybenzene-2[(2′,3′,4′-trimethoxy)-2-methyl-2(4-methyl-3-penten-1-yl)-2H-1-benzopyran-5-yl)methylene]-3-benzofuranon (1), and nine known aurones (2–10) were isolated from Sophora japonica L. for the first time. Compounds 1–10 were evaluated for their neuroprotective activities against 6-OHDA-induced cell death in SH-SY5Y cells. Compounds 1, 3, 8, and 10 exhibited significant neuroprotective activities with IC50 values in the range of 2.89–6.02 μM. more...
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- 2019
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31. Lagopsis supina exerts its diuretic effect via inhibition of aquaporin-1, 2 and 3 expression in a rat model of traumatic blood stasis
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Lingbing Zeng, Junwei He, Rongrui Wei, Yuye Zhu, Tingting Xu, Guoyue Zhong, and Li Yang
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Male ,Urinary system ,medicine.medical_treatment ,Diuresis ,Blood stasis ,Pharmacology ,Aquaporins ,Kidney ,Microcirculation ,Rats, Sprague-Dawley ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,Drug Discovery ,medicine ,Animals ,Diuretics ,030304 developmental biology ,0303 health sciences ,Lamiaceae ,Aldosterone ,Plant Extracts ,business.industry ,Angiotensin II ,Hormones ,chemistry ,030220 oncology & carcinogenesis ,Aquaporin 1 ,Blood Circulation ,Diuretic ,business - Abstract
Ethnopharmacological relevance Lagopsis supina has been used as a traditional medicinal herb for centuries in China. In folk medicine, it is used for promoting blood circulation and removing blood stasis (PBCRBS), anti-inflammatory and diuretic activities. Modern pharmacological investigation have shown that L. supina have an improvement in blood and lymphatic microcirculation, myocardioprotective, and antioxidative activities. Although the pharmacological research of L. supina was more, there was no report on the diuretic activity. Aim of the study This study was to evaluate the diuretic activity and the underlying mechanism of an ethanol extract of L. supina (LS) in a rat model of traumatic blood stasis (TBS). Materials and methods There were 30 male Sprague-Dawley rats that were randomly assigned to the control group, TBS group, and LS group (10 animals in each group). LS was administered orally (460 mg/kg) once daily for 7 successive days. The control group and TBS group were given an equal amount of 0.3% sodium carboxymethyl cellulose (CMC-Na). For the efficacy evaluation, the urine output volume, the urinary electrolyte concentrations (Na+, K+, Cl- and Ca2+) and pH value, the levels of angiotensin II (Ang II), atriopeptin (ANP), anti-diuretic hormone (ADH) and aldosterone (ALD), as well as aquaporin (AQP)-1, 2 and 3 protein expressions were detected in a rat model of TBS. The protein expressions of AQP-1, 2 and 3 were detected by quantitative immunohistochemistry (IHC) and Western blot analysis. Results In the efficacy evaluation, rat models treated with LS showed a significant increase in the total urine output (p Conclusions This is the first reported notable diuretic effect by LS, which probably was through the suppression of the renin-angiotensin-aldosterone system (RAAS) and the regulation of the signaling pathways of AQP-1, 2 and 3 protein expressions. Based on our results, we conclude that L. supina carries out its diuretic effect mainly by down-regulating the levels of AQP-1, 2 and 3 expressions in TBS rat model. These data also embody the traditional Chinese medicine (TCM) application principle of Huo xue li shui. These findings suggest that LS may warrant further evaluation as a possible agent for the diuretic drug in clinical applications. Further research is underway to elucidate the active compounds responsible for the diuretic activity of LS. more...
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- 2019
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32. Protective effect of the ethyl acetate fraction of Qinghai-Tibet Plateau medicinal plant Chrysosplenium axillare Maxim. against ANIT-induced cholestatic liver injury in mice
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Guoyue Zhong, Ji-Xiao Zhu, Wenyan Li, Cai Ziyan, Gang Ren, Wei Jiang, Zejing Mu, and Rongrui Wei
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Liver injury ,Chemistry ,Multidrug resistance-associated protein 2 ,Chrysosplenium axillare Maxim ,Pharmacology ,Phytochemical analysis ,Cholesterol 7 alpha-hydroxylase ,medicine.disease ,Therapeutic agents, Mechanism ,α-Naphthylisothiocyanate ,Other systems of medicine ,Hepatoprotection ,Cholestasis ,Oral administration ,Small heterodimer partner ,medicine ,Farnesoid X receptor ,Acute intrahepatic cholestasis ,RZ201-999 - Abstract
Background: Chrysosplenium axillare Maxim. has been used as a traditional Tibetan herb medicine for hepatobiliary disorder in Qinghai-Tibet Plateau for more than one thousand years. Hypothesis/purpose: we hypothesized that the ethyl acetate-soluble portion extracted from C. axillare (ECA) could exert hepatoprotection effect against α-naphthylisothiocyanate (ANIT)-induced hepatotoxity and acute intrahepatic cholestasis in mice and aimed to investigate its potential mechanism. Study design: male KM mice with acute intrahepatic cholestasis induced by ANIT were orally administered with the ECA (100 and 50 mg/kg B.W.). Mice receiving vehicle (0.5% CMC-Na) served as control. Methods: 48 h after ANIT administration, mice were sacrificed. Blood was collected for serum enzymes and components analysis using commercial kits. Livers were removed for histopathological examination and protein preparation. The protein expression levels of farnesoid X receptor (FXR), bile-salt export pump (BSEP), multidrug resistance associated protein2 (MRP2), Na+-taurocholate co-transporting polypeptide (NTCP), small heterodimer partner (SHP), and cholesterol 7α-hydroxylase (CYP7A1) were evaluated by a western blot analysis. A phytochemical analysis was conducted to characterize the chemical constituents of ECA. Results: oral administration of ECA at both doses (P < 0.05 or P < 0.01) can prevent ANIT-induced increases in levels of serum enzymes and components, including AST, ALT, ALP, DBIL, TBA, and TBIL and improve the liver pathologic change induced by ANIT exposure. Western blot analysis showed that the expression levels of FXR, BSEP, MRP2, NTCP, and SHP in ECA (100 and 50 mg/kg) groups were up-regulated versus model group (P < 0.05 or P < 0.01), and those of CYP7A1 in both ECA treated groups were down-regulated versus model group (P < 0.01). One new highly O-methylated flavonoids, chrysosplenoside I (1), together with fourteen analogues (2–15), was isolated from ECA and structurally identified by spectra analysis. Among them, the two abundant ingredients, chrysosplenosides A and I (11 and 1), were quantitatively determined to have a total content account for 32.2% of ECA. Conclusion: ECA protected against mice liver damage with acute intrahepatic cholestasis induced by ANIT via regulation of the expression of hepatic proteins involved in bile acids synthesis, transportation and re-absorption. These results confirmed the hepatoprotective efficacy of traditional Tibet herb medicine C. axillare and provided the first insight into its related mechanism as well as the potential active ingredients. more...
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- 2021
33. Isolation and characterization of neuroprotective lignans from salted Aconiti lateralis Radix Praeparata
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Chen Lihua, Rongrui Wei, and Ma Qinge
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Positive control ,Pharmacology ,01 natural sciences ,Applied Microbiology and Biotechnology ,Biochemistry ,Neuroprotection ,PC12 Cells ,Lignans ,Analytical Chemistry ,Desipramine ,medicine ,Animals ,Radix ,Spectral data ,Molecular Biology ,Aconitum ,Cell Death ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,General Medicine ,0104 chemical sciences ,Rats ,010404 medicinal & biomolecular chemistry ,Neuroprotective Agents ,Biotechnology ,medicine.drug - Abstract
Six lignans (1-6) were isolated from salted Aconiti lateralis Radix Praeparata for the first time. These isolates were elucidated as hedyotisol-A (1), (7″R,8″R)-8″-syringaresinol-4″-hydroxy-3″,5″-dimethoxyphenyl-7″,9″-propanediol (2), lariciresinol-4-O-β-d-glucopyranoside (3),(7S,8S)-4-hydroxy-3-methoxy-7,8-(2′,1′-O-β-d-glucopyranosyl)phenyl-propanetriol (4), (+)-isolariciresinol (5), and (+)-lyoniresinol (6) by analyzing extensive and comprehensive spectral data and compared with the data described in the literature, respectively. Compounds (1-6) were evaluated for their neuroprotective activities against corticosterone-induced cell death in PC12 cells with desipramine as the positive control drug. Among them, compounds 1 and 2 showed moderate neuroprotective activities, which increased the survival rates of PC12 cells from 45.50 ± 2.23% to 65.98 ± 1.29%, 58.19 ± 2.94% at 10 µm, respectively. more...
- Published
- 2021
34. 5-Aminonaphthalene derivatives as selective nonnucleoside nuclear receptor binding SET domain-protein 2 (NSD2) inhibitors for the treatment of multiple myeloma
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Qiongyu Shi, Cong Li, Zhanqing Cong, Yubo Zhou, Su Mingbo, Meiyu Geng, Jiang Wang, Xu Han, Fulin Lian, Xingling Zheng, Xingjun Li, Naixia Zhang, Xun Huang, Jia Li, Hong Liu, Hong Yang, Xuhong Fu, Shuni Wang, Rongrui Wei, and Chunpu Li more...
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Cell cycle checkpoint ,Methyltransferase ,Cell Survival ,Antineoplastic Agents ,Apoptosis ,Naphthalenes ,01 natural sciences ,03 medical and health sciences ,Histone H3 ,Structure-Activity Relationship ,Drug Discovery ,Tumor Cells, Cultured ,Humans ,Enzyme Inhibitors ,Cytotoxicity ,030304 developmental biology ,Cell Proliferation ,Pharmacology ,0303 health sciences ,Dose-Response Relationship, Drug ,Molecular Structure ,010405 organic chemistry ,Chemistry ,Organic Chemistry ,General Medicine ,Methylation ,Cell Cycle Checkpoints ,Histone-Lysine N-Methyltransferase ,Molecular biology ,0104 chemical sciences ,Repressor Proteins ,Nuclear receptor ,Histone methyltransferase ,Drug Screening Assays, Antitumor ,Multiple Myeloma - Abstract
Approximately 20% of multiple myeloma (MM) are caused by a chromosomal translocation t (4; 14) that leads to the overexpression of the nuclear receptor binding SET domain-protein 2 (NSD2) histone methyltransferase. NSD2 catalyzes the methylation of lysine 36 on histone H3 (H3K36me2) and is associated with transcriptionally active regions. Using high-throughput screening (HTS) with biological analyses, a series of 5-aminonaphthalene derivatives were designed and synthesized as novel NSD2 inhibitors. Among all the prepared compounds, 9c displayed a good NSD2 inhibitory activity (IC50 = 2.7 μM) and selectivity against both SET-domain-containing and non-SET-domain-containing methyltransferases. Preliminary research indicates the inhibition mechanism of compound 9c by significantly suppressed the methylation of H3K36me2. Compound 9c specifically inhibits the proliferation of the human B cell precursor leukemia cell line RS4:11 and the human myeloma cell line KMS11 by inducing cell cycle arrest and apoptosis with little cytotoxicity. It has been reported that the anti-cancer effect of compound 9c is partly achieved by completely suppressing the transcriptional activation of NSD2-targeted genes. When administered intraperitoneally at 25 mg/kg, compound 9c suppressed the tumor growth of RS4:11 xenografts in vivo and no body weight loss was detected in the tested SCID mice. more...
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- 2021
35. Isolation and characterization of neolignan derivatives with hepatoprotective and neuroprotective activities from the fruits of Citrus medica L. var. Sarcodactylis Swingle
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Zhipei Sang, Qinge Ma, Fang Wang, Rongrui Wei, Jiang-Hong Dong, Ming Yang, and Huang Xiaoying
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Citrus ,Magnetic Resonance Spectroscopy ,Cell Survival ,Molecular Conformation ,Protective Agents ,01 natural sciences ,Biochemistry ,PC12 Cells ,Lignans ,Structure-Activity Relationship ,food ,Functional food ,Drug Discovery ,Animals ,Humans ,Spectral data ,Molecular Biology ,chemistry.chemical_classification ,Traditional medicine ,010405 organic chemistry ,Organic Chemistry ,Glycoside ,Hep G2 Cells ,food.food ,0104 chemical sciences ,Citrus medica ,Rats ,010404 medicinal & biomolecular chemistry ,chemistry ,Hepg2 cells ,Fruit - Abstract
The fruit of Citrus medica L. var. sarcodactylis Swingle is a functional food with rich nutrients and medicinal values because of its content of bioactive compounds. A bioactivity-guided chemical investigation from the fruits of C. medica L. var. sarcodactylis Swingle afforded three new benzodioxane neolignans (1–3), three new phenanthrofuran neolignan glycosides (4–6), two new biphenyl-ketone neolignans (7–8), two new 1′,7′-bilignan neolignans (9–10), as well as fourteen known neolignan derivatives (11–24), which were isolated and characterized from the fruits of C. medica L. var. sarcodactylis Swingle for the first time. These neolignan derivatives were determined by extensive and comprehensive analyzing NMR, HR-ESI-MS, UV, IR spectral data and compared with the data described in the literature. Among them, compounds 1–3 and 12–13 exhibited moderate hepatoprotective activities to improve the survival rates of HepG2 cells from 46.26 ± 1.90% (APAP, 10 mM) to 67.23 ± 4.25%, 62.87 ± 4.43%, 60.06 ± 6.34%, 56.75 ± 2.30%, 58.35 ± 6.14%, respectively. Additionally, compounds 7–8 and 21–22 displayed moderate neuroprotective activities to raise the survival rates of PC12 cells from 55.30 ± 2.25% to 66.94 ± 3.37%, 70.98 ± 5.05%, 64.64 ± 1.93%, and 62.81 ± 4.11% at 10 μM, respectively. The plausible biogenetic pathway and preliminary structure–activity relationship of the selected compounds were scientifically summarized and discussed in this paper. more...
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- 2020
36. Structural elucidation and neuroprotective activities of lignans from the flower buds of
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Qinge, Ma, Rongrui, Wei, Xiaodong, Zhang, Zhipei, Sang, and Jianghong, Dong
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Magnetic Resonance Spectroscopy ,Neuroprotective Agents ,Cell Death ,Molecular Structure ,Magnolia ,Plant Extracts ,Nerve Degeneration ,Humans ,Flowers ,Oxidopamine ,Lignans ,Cell Line - Abstract
Two new lignans, 3,4-(10-methoxy-phenylallyl)-9″-((10'-isopropanol-3',4'-furan)-phenylacetyl)-8″-dioxane-7″-O
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- 2020
37. Hepatoprotective homoisoflavonoids from the fruits of Cucumis bisexualis
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Qinge Ma, Zhipei Sang, and Rongrui Wei
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China ,030309 nutrition & dietetics ,Wild fruit ,Biophysics ,Protective Agents ,Cucumis ,03 medical and health sciences ,0404 agricultural biotechnology ,Column chromatography ,Alanine aminotransferase ,Hepatoprotective Agent ,Spectral data ,Pharmacology ,0303 health sciences ,Traditional medicine ,biology ,Plant Extracts ,Chemistry ,04 agricultural and veterinary sciences ,Cell Biology ,biology.organism_classification ,040401 food science ,Fruit ,Hepg2 cells ,Food Science - Abstract
Cucumis bisexualis has been widely served as a beneficial wild fruit in China. Four new homoisoflavonoids (1-4), together with eight known homoisoflavonoid derivatives (5-12) were isolated from the 90% EtOH extract of C. bisexualis, using repeated open column chromatography and preparative thin-layer chromatography. They were elucidated based on the analysis of spectral data and references from the fruits of C. bisexualis for the first time. These compounds (1-12) were evaluated for their in vitro inhibitory effects against the increase of aspartate aminotransferase and alanine aminotransferase levels in H2 O2 -induced HepG2 cells in the range of their maximum nontoxic concentration. Among them, compounds 3, 4, 8, and 9 exhibited certain hepatoprotective activities. PRACTICAL APPLICATIONS: Cucumis bisexualis A.M. Lu & G.C. Wang is an edible and medical fruit with many functional properties. A detailed study was made to identify the bioactive constituents of C. bisexualis and four new homoisoflavonoids (1-4) and eight known homoisoflavonoid derivatives (5-12) were isolated from the fruits of C. bisexualis for the first time. Compounds 3, 4, 8, and 9 exhibited certain hepatoprotective activities. This study suggests that natural compounds isolated from C. bisexualis could be used as promising hepatoprotective agents. more...
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- 2020
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38. Neuroprotective Sesquiterpenes from Capsella bursa-pastoris
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Zhongling Cao, Rongrui Wei, and Qinge Ma
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010404 medicinal & biomolecular chemistry ,biology ,Traditional medicine ,010405 organic chemistry ,Chemistry ,Capsella bursa-pastoris ,Plant Science ,General Chemistry ,biology.organism_classification ,01 natural sciences ,General Biochemistry, Genetics and Molecular Biology ,0104 chemical sciences - Published
- 2018
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39. Structurally diverse biflavonoids from the fruits of Citrus medica L. var. sarcodactylis Swingle and their hypolipidemic and immunosuppressive activities
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Ye Tang, Qinge Ma, Rongrui Wei, Zhipei Sang, and Jiang-Hong Dong
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Citrus ,Cell Survival ,Swine ,Positive control ,Biochemistry ,Structure-Activity Relationship ,food ,Drug Discovery ,Concanavalin A ,medicine ,Ic50 values ,Animals ,Biflavonoids ,Humans ,Structure–activity relationship ,Enzyme Inhibitors ,Spectral data ,Pancreas ,Molecular Biology ,Cell Proliferation ,Hypolipidemic Agents ,chemistry.chemical_classification ,Dose-Response Relationship, Drug ,Molecular Structure ,Traditional medicine ,Organic Chemistry ,Biflavonoid ,Hep G2 Cells ,Lipase ,food.food ,Citrus medica ,Orlistat ,chemistry ,Fruit ,Immunosuppressive Agents ,Spleen ,medicine.drug - Abstract
The fruit of Citrus medica L. var. sarcodactylis Swingle is not only used as a traditional medicinal plant, but also served as a delicious food. Six new (3′→7″)-biflavonoids (1–6), and twelve known biflavonoid derivatives (7–18) were isolated and characterized from the fruits of C. medica L. var. sarcodactylis Swingle for the first time. Their structures were determined by extensive and comprehensive analyzing NMR, HR-ESI-MS, UV, and IR spectral data coupled with the data described in the literature. Compounds (1–18) were evaluated for their hypolipidemic activities with Orlistat as the positive control, and assayed for their immunosuppressive activities with Dexamethasone as the positive control, respectively. Among them, compounds (1–3) exhibited moderate inhibition of pancreatic lipase activity by inhibiting 68.56 ± 1.40%, 56.18 ± 1.57%, 53.51 ± 1.59% of pancreatic lipase activities at the concentration of 100 μM, respectively. Compounds (4–6) and 8 showed potent immunosuppressive activities with the IC50 values from 16.83 ± 1.32 to 50.90 ± 1.79 μM. The plausible biogenetic pathway and preliminary structure activity relationship of the selected compounds were scientifically summarized and discussed in this study. more...
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- 2021
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40. CTC clusters induced by heparanase enhance breast cancer metastasis
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Hong Yang, Xun Huang, Xiong Zhang, Juan Yan, Xuhong Fu, Meiyu Geng, Rongrui Wei, Jian Ding, Xingling Zheng, and Danni Sun
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0301 basic medicine ,Breast Neoplasms ,Article ,Metastasis ,03 medical and health sciences ,0302 clinical medicine ,Breast cancer ,Circulating tumor cell ,Cell Line, Tumor ,Cell Adhesion ,medicine ,Animals ,Humans ,Pharmacology (medical) ,Heparanase ,Neoplasm Metastasis ,Cell adhesion ,Cell Aggregation ,Glucuronidase ,Pharmacology ,Mice, Inbred BALB C ,Chemistry ,Cancer ,General Medicine ,Intercellular Adhesion Molecule-1 ,Neoplastic Cells, Circulating ,medicine.disease ,Cell aggregation ,Up-Regulation ,src-Family Kinases ,030104 developmental biology ,Focal Adhesion Kinase 1 ,030220 oncology & carcinogenesis ,Cancer cell ,Cancer research ,Female ,Paxillin - Abstract
Aggregated metastatic cancer cells, referred to as circulating tumor cell (CTC) clusters, are present in the blood of cancer patients and contribute to cancer metastasis. However, the origin of CTC clusters, especially intravascular aggregates, remains unknown. Here, we employ suspension culture methods to mimic CTC cluster formation in the circulation of breast cancer patients. CTC clusters generated using these methods exhibited an increased metastatic potential that was defined by the overexpression of heparanase (HPSE). Heparanase induced FAK- and ICAM-1-dependent cell adhesion, which promoted intravascular cell aggregation. Moreover, knockdown of heparanase or inhibition of its activity with JG6, a heparanase inhibitor, was sufficient to block the formation of cell clusters and suppress breast cancer metastasis. Our data reveal that heparanase-mediated cell adhesion is critical for metastasis mediated by intravascular CTC clusters. We also suggest that targeting the function of heparanase in cancer cell dissemination might limit metastatic progression. more...
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- 2018
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41. Aspirin disrupts the mTOR-Raptor complex and potentiates the anti-cancer activities of sorafenib via mTORC1 inhibition
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Aijun Shen, Min Huang, Xingling Zheng, Danni Sun, Meiyu Geng, Xiaoyang Dai, Xun Huang, Juan Yan, Jian Ding, Rongrui Wei, Xuhong Fu, and Hongchun Liu
- Subjects
Niacinamide ,0301 basic medicine ,Sorafenib ,MAPK/ERK pathway ,Cancer Research ,Carcinoma, Hepatocellular ,Antineoplastic Agents ,Apoptosis ,mTORC1 ,AMP-Activated Protein Kinases ,Mechanistic Target of Rapamycin Complex 1 ,Pharmacology ,Mice ,03 medical and health sciences ,0302 clinical medicine ,Tuberous Sclerosis Complex 2 Protein ,Animals ,Humans ,Medicine ,Protein kinase B ,Cells, Cultured ,PI3K/AKT/mTOR pathway ,Adaptor Proteins, Signal Transducing ,Cell Proliferation ,Mice, Knockout ,Aspirin ,business.industry ,Phenylurea Compounds ,TOR Serine-Threonine Kinases ,Tumor Suppressor Proteins ,Anti-Inflammatory Agents, Non-Steroidal ,Liver Neoplasms ,AMPK ,Cancer ,Regulatory-Associated Protein of mTOR ,Fibroblasts ,Embryo, Mammalian ,medicine.disease ,Xenograft Model Antitumor Assays ,Gene Expression Regulation, Neoplastic ,030104 developmental biology ,Oncology ,Multiprotein Complexes ,030220 oncology & carcinogenesis ,Drug Therapy, Combination ,business ,medicine.drug - Abstract
Aspirin is associated with a reduced risk of cancer and delayed progression of malignant disease. Adenosine 5'-monophosphate (AMP)-activated protein kinase (AMPK)-mTOR signaling is believed to partially contribute to these anticancer effects, although the mechanism is unclear. In this study, we revealed the mechanism underlying the effects of aspirin on AMPK-mTOR signaling, and described a mechanism-based rationale for the use of aspirin in cancer therapy. We found that aspirin inhibited mTORC1 signaling through AMPK-dependent and -independent manners. Aspirin inhibited the AMPK-TSC pathway, thus resulting in the suppression of mTORC1 activity. In parallel, it directly disrupted the mTOR-raptor interaction. Additionally, the combination of aspirin and sorafenib showed synergetic effects via inhibiting mTORC1 signaling and the PI3K/AKT, MAPK/ERK pathways. Aspirin and sorafenib showed synergetic anticancer efficacy in the SMMC-7721 model. Our study provides mechanistic insights and a mechanism-based rationale for the roles of aspirin in cancer treatment. more...
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- 2017
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42. Cytotoxic Anthraquinones from the Aerial Parts of Acalypha australis
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Qinge Ma, Liu Wenmin, Rongrui Wei, Zhipei Sang, and Guo Xiuhuan
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biology ,Traditional medicine ,010405 organic chemistry ,Chemistry ,Plant Science ,General Chemistry ,biology.organism_classification ,01 natural sciences ,General Biochemistry, Genetics and Molecular Biology ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,chemistry.chemical_compound ,Anthraquinones ,Acalypha australis - Published
- 2017
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43. Acute toxicity of Potentilla anserina L. extract in mice
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Dul Dram, Zhen Dan, Junwei He, Qinge Ma, Cui-Zhu Zhao, Jia-Jie Duo, and Rongrui Wei
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Male ,Potentilla anserina ,Physiology ,Renal function ,Administration, Oral ,Autopsy ,Crude drug ,Kidney ,Kidney Function Tests ,General Biochemistry, Genetics and Molecular Biology ,03 medical and health sciences ,Eating ,Mice ,Random Allocation ,0302 clinical medicine ,Liver Function Tests ,Toxicity Tests, Acute ,Animals ,Medicine, Chinese Traditional ,030304 developmental biology ,0303 health sciences ,Plant Extracts ,Body Weight ,Acute toxicity ,Liver ,030220 oncology & carcinogenesis ,Case-Control Studies ,Toxicity ,Maximum dose ,Potentilla ,Female ,Liver function - Abstract
Potentilla anserina L. is not only a medicinal plant, but also a traditional cuisine. Hence, an acute toxicity study was performed to confirm its safety profile. Forty Kunming mice were randomly divided into two groups: control group and P. anserina L. extract group. Using the maximum dosage method, the P. anserina L. extract group was given the maximum dose within 12 h, equivalent to 345.6 g/kg crude drug. The control group was given distilled water. After administration, toxicity symptoms of mice were observed, body weight and food intake were recorded. After 14 days, blood was collected to measure biochemical parameters, autopsy was carried out to observe the changes of organs, and the vital organs were separated, weighed, and preserved for histopathological examination. The results showed that P. anserina L. extract group had no toxic symptoms. The activity, weight, and diet of mice were normal, and no abnormality was found in organ index, renal function, liver function, anatomical observation, and histopathological examination. Therefore, the maximum oral dosage (345.6 g/kg) of P. anserina L. was good safety. This study indicated that P. anserina L. had a large safety range and the clinical application was safe. more...
- Published
- 2020
44. Isolation and characterization of flavonoid derivatives with anti-prostate cancer and hepatoprotective activities from the flowers of Hosta plantaginea (Lam.) Aschers
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Rongrui Wei, Qinge Ma, Junwei He, Guoyue Zhong, and Zhipei Sang
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Male ,Antineoplastic Agents ,Flowers ,Protective Agents ,Cell Line ,03 medical and health sciences ,Prostate cancer ,0302 clinical medicine ,Flavonoid derivatives ,Drug Discovery ,LNCaP ,medicine ,Ic50 values ,Humans ,Carbon Tetrachloride ,030304 developmental biology ,Pharmacology ,Flavonoids ,0303 health sciences ,biology ,Traditional medicine ,Liliaceae ,Cancer ,Hosta ,Prostatic Neoplasms ,medicine.disease ,biology.organism_classification ,Liver ,030220 oncology & carcinogenesis ,Chemical and Drug Induced Liver Injury ,Hosta plantaginea - Abstract
Ethnopharmacological relevance The flower of Hosta plantaginea (Lam.) Aschers (Liliaceae) is a traditional medicinal material in Mongolian medicine for treating sore throat, hoarseness, pulmonary fever, and toxic fever in folk. The present work investigated anti-prostate cancer and hepatoprotective activities of flavonoid derivatives from H. plantaginea (Lam.) Aschers. Aim of the study: To isolate and identify the chemicals of H. plantaginea (Lam.) Aschers for anti-prostate cancer and hepatoprotective activities. Materials and methods Active chemicals were isolated and purified from H. plantaginea (Lam.) Aschers by chromatographic methods, and their structures were established on spectroscopic analysis and references. These compounds were evaluated for their anti-prostate cancer activities using the LNCaP prostate cancer cells, and assayed for their hepatoprotective activities on CCl4-induced injury of human L-O2 cells, respectively. Results Four new flavonol-lignan heterodimers (1–4), together with nine known flavonoid derivatives (5–13) were isolated from this plant for the first time. Among them, some compounds exhibited moderate anti-prostate cancer and hepatoprotective activities. Conclusion Compounds 1, 2, 5, and 6 showed anti-prostate cancer activities using the LNCaP prostate cancer cells with IC50 values of 17.84, 33.26, 54.13, and 81.55 μg/mL, and compounds 3, 4, 8, and 9 exhibited moderate hepatoprotective activities, respectively. A preliminary structure-activity relation was summarized in this paper. more...
- Published
- 2020
45. Hypouricemic Effects of Extracts from Urtica hyperborea Jacq. ex Wedd. in Hyperuricemia Mice through XOD, URAT1, and OAT1
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Surina Han, Guoyue Zhong, Rongrui Wei, Ji-Xiao Zhu, Wei-Zao Luo, Daorina Han, and Wu-Li-Ji Ao
- Subjects
food.ingredient ,Article Subject ,Allopurinol ,Renal function ,Crude drug ,Pharmacology ,urologic and male genital diseases ,01 natural sciences ,General Biochemistry, Genetics and Molecular Biology ,03 medical and health sciences ,chemistry.chemical_compound ,0302 clinical medicine ,food ,In vivo ,medicine ,Hyperuricemia ,General Immunology and Microbiology ,Urtica ,nutritional and metabolic diseases ,General Medicine ,medicine.disease ,0104 chemical sciences ,Gout ,010404 medicinal & biomolecular chemistry ,chemistry ,030220 oncology & carcinogenesis ,Uric acid ,Medicine ,medicine.drug - Abstract
Urtica L. has been long used for gout in traditional Tibetan medicine and is closely related to the effect of reducing uric acid. This study aimed to investigate the effect of Urtica hyperborea Jacq. ex Wedd. (UW) on lowering uric acid and its mechanism by using HK2 cells and hyperuricemia mouse model. Petroleum ether extract (UWP), ethyl acetate extract (UWE), n-butanol extract (UWB), and alcohol-soluble extract (UWA) from UW were prepared, and HK2 cells were treated with various parts extracts to observe the expression of uric acid transporter at 25, 50, and 100 μg/mL for 24 h. Moreover, hyperuricemia mice were administered orally various parts extracts at 0.78 and 2.34 g/kg (crude drug dose converted by extraction rate) to observe the change of hepatic XOD, serum ADA, renal function, and uric acid transporter. In vitro experiments showed that UWA can remarkably elevate OAT1 expression and decrease URAT1 expression in HK2 cells. In vivo experiments showed that UWP, UWE, UWB, and UWA showed remarkable activity in reducing uric acid, rendering a substantial decline in the SUA level in hyperuricemia mice. Compared with the hyperuricemia and allopurinol groups, UWB and UWA had significant protective effects on renal injury. At the same time, UWA can significantly reduce the activity of XOD and ADA, reduce the expression of URAT1, and increase the expression of OAT1. These results indicated that UWA had an outstanding uric acid lowering effect and did not affect renal function. This may be related to increased uric acid excretion and decreased uric acid production, mediated by renal OAT1, URAT1, liver XOD, and serum ADA. UWA may be a potential drug against hyperuricemia. more...
- Published
- 2020
- Full Text
- View/download PDF
46. Hepatoprotective and neuroprotective flavanes from the fruits of Ulmus pumila L. (Ulmaceae)
- Author
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Qinge, Ma, Rongrui, Wei, Dongli, Shang, Zhipei, Sang, Wenmin, Liu, and Zhongling, Cao
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Ulmaceae ,Neuroprotective Agents ,Liver ,Plant Extracts ,Cell Line, Tumor ,Fruit ,Ulmus ,Humans ,Protective Agents - Abstract
Phytochemical study of the EtOAc fraction (active extract) of the fruits of Ulmus pumila L. resulted in the isolation of thirteen flavane derivatives, and they were identified by their precise spectral data and literature. All the compounds (1-13) were obtained from the fruits of U. pumila L. for the first time. Meanwhile, the compounds (1-13) were assayed for their hepatoprotective and neuroprotective activities, respectively. Compounds 1, 2, 5, 7 and 8 (10μM) exhibited remarkable hepatoprotective activities, and compounds 9, 10, and 13 showed significant neuroprotective activities with IC50 values of 4.08, 5.34, and 2.02μM, respectively. more...
- Published
- 2019
47. Bioactivity-guided isolation of aurone derivatives with hepatoprotective activities from the fruits of Cucumis bisexualis
- Author
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Qinge Ma, Rongrui Wei, and Zhipei Sang
- Subjects
biology ,Traditional medicine ,Molecular Structure ,Chemistry ,Cell Survival ,Phytochemicals ,Positive control ,biology.organism_classification ,Isolation (microbiology) ,General Biochemistry, Genetics and Molecular Biology ,Cucumis ,Cell Line ,chemistry.chemical_compound ,Phytochemical ,Coumarins ,Aurone ,Hepatocytes ,Humans ,Carbon Tetrachloride ,Benzofurans ,Cell Proliferation - Abstract
Bioactivity-guided phytochemical investigation of Cucumis bisexualis has led to the isolation of three new coumarin-aurone heterodimers (1-3), along with six aurone derivatives (4-9) were isolated from C. bisexualis for the first time. Their structures were determined by their extensive spectroscopic data and comparison with the values reported in the references. All isolated compounds (1-9) were evaluated for their hepatoprotective activities on human L-O2 cells, which compared with positive control of Bifendatatum. Among them, compounds 1, 2, and 7 exhibited moderate hepatoprotective activities to promote effects on the proliferation of L-O2 cells. more...
- Published
- 2019
48. Hypouricemic Effects of Extracts from
- Author
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Surina, Han, Rongrui, Wei, Daorina, Han, Jixiao, Zhu, Weizao, Luo, Wuliji, Ao, and Guoyue, Zhong
- Subjects
Male ,Organic Cation Transport Proteins ,Plant Extracts ,nutritional and metabolic diseases ,Organic Anion Transporters ,Hyperuricemia ,urologic and male genital diseases ,Kidney ,Cell Line ,Uric Acid ,Disease Models, Animal ,Mice ,Organic Anion Transport Protein 1 ,Antigens, Neoplasm ,Animals ,Humans ,Urticaceae ,Research Article - Abstract
Urtica L. has been long used for gout in traditional Tibetan medicine and is closely related to the effect of reducing uric acid. This study aimed to investigate the effect of Urtica hyperborea Jacq. ex Wedd. (UW) on lowering uric acid and its mechanism by using HK2 cells and hyperuricemia mouse model. Petroleum ether extract (UWP), ethyl acetate extract (UWE), n-butanol extract (UWB), and alcohol-soluble extract (UWA) from UW were prepared, and HK2 cells were treated with various parts extracts to observe the expression of uric acid transporter at 25, 50, and 100 μg/mL for 24 h. Moreover, hyperuricemia mice were administered orally various parts extracts at 0.78 and 2.34 g/kg (crude drug dose converted by extraction rate) to observe the change of hepatic XOD, serum ADA, renal function, and uric acid transporter. In vitro experiments showed that UWA can remarkably elevate OAT1 expression and decrease URAT1 expression in HK2 cells. In vivo experiments showed that UWP, UWE, UWB, and UWA showed remarkable activity in reducing uric acid, rendering a substantial decline in the SUA level in hyperuricemia mice. Compared with the hyperuricemia and allopurinol groups, UWB and UWA had significant protective effects on renal injury. At the same time, UWA can significantly reduce the activity of XOD and ADA, reduce the expression of URAT1, and increase the expression of OAT1. These results indicated that UWA had an outstanding uric acid lowering effect and did not affect renal function. This may be related to increased uric acid excretion and decreased uric acid production, mediated by renal OAT1, URAT1, liver XOD, and serum ADA. UWA may be a potential drug against hyperuricemia. more...
- Published
- 2019
49. Apigenin-rivastigmine hybrids as multi-target-directed liagnds for the treatment of Alzheimer's disease
- Author
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Yu Lintao, Jian Shi, Qinge Ma, Wenmin Liu, Zhipei Sang, Cheng Xinfeng, Zhenghuai Tan, Wang Keren, Gaofeng Zhu, Yiyang Zhao, and Rongrui Wei
- Subjects
Antioxidant ,medicine.medical_treatment ,Rivastigmine ,Pharmacology ,Ligands ,01 natural sciences ,Neuroprotection ,03 medical and health sciences ,chemistry.chemical_compound ,Structure-Activity Relationship ,Alzheimer Disease ,Drug Discovery ,medicine ,Potency ,Animals ,Humans ,Apigenin ,Zebrafish ,030304 developmental biology ,0303 health sciences ,Amyloid beta-Peptides ,Dose-Response Relationship, Drug ,Molecular Structure ,010405 organic chemistry ,Organic Chemistry ,General Medicine ,Metabolism ,Acute toxicity ,0104 chemical sciences ,Rats ,Molecular Docking Simulation ,Neuroprotective Agents ,chemistry ,Butyrylcholinesterase ,Microsome ,Acetylcholinesterase ,Microsomes, Liver ,Cholinesterase Inhibitors ,medicine.drug - Abstract
Here we reported novel apigenin-rivastigmine hybrids were rationally designed and synthesized by the multi-target-directed ligands (MTDLs) strategy, their activity in vitro results revealed that compound 3d showed significant antioxidant potency (ORAC = 1.3 eq), and it was a reversible huAChE (IC50 = 6.8 μM) and huBChE (IC50 = 16.1 μM) inhibitor. 3d also served as a selective metal chelator, and it significantly inhibited and disaggregated self-mediated and Cu2+-mediated Aβ1-42 aggregation, and also inhibited hAChE-mediated induced Aβ1-40 aggregation. Compound 3d exhibited remarkable neuroprotective effect and hepatoprotective activity. In addition, compound 3d presented favourable blood-brain barrier penetration in vitro and drug-like property. Further, the in vivo assay displayed that 3d indicated remarkable dyskinesia recovery rate and response efficiency on AD zebrafish, and exhibited surprising protective effect on Aβ1-40-mediated zebrafish vascular injury. More importantly, 3d did not indicate obvious acute toxicity at dose up to 2000 mg/kg, and could improve scopolamine-induced memory impairment. Subsequently, the regulation of multi-targets for 3d were further confirmed through transcriptome sequencing of brain hippocampi, which also offered novel potential targets and opened a new way to treat Alzheimer’s disease. More interestingly, the metabolism of 3d in vitro indicated that 4 metabolites in rat liver microsome metabolism, 2 metabolites in human liver microsome metabolism, and 4 metabolites in intestinal flora metabolism, which offered supports for the preclinical study of 3d. Overall, this study exhibited that compound 3d was a promising advanced compound targeted multiple factors associated with AD. more...
- Published
- 2019
50. Structurally diverse coumarin-homoisoflavonoid derivatives with hepatoprotective activities from the fruits of Cucumis bisexualis
- Author
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Qinge Ma, Zhi-Pei Sang, Jiang-Hong Dong, and Rongrui Wei
- Subjects
China ,Wild fruit ,Phytochemicals ,Positive control ,Protective Agents ,01 natural sciences ,Cucumis ,chemistry.chemical_compound ,Coumarins ,Drug Discovery ,medicine ,Humans ,Acetaminophen ,Flavonoids ,Pharmacology ,Molecular Structure ,Traditional medicine ,biology ,010405 organic chemistry ,Chemistry ,Hep G2 Cells ,General Medicine ,biology.organism_classification ,Coumarin ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,Fruit ,Hepg2 cells ,Cucurbitaceae ,medicine.drug - Abstract
Cucumis bisexualis is a favorite wild fruit with high nutritional and medicinal values because of its bioactive constituents. Four previously undescribed coumarin-homoisoflavonoid derivatives (1–4), together with seven known coumarin and homoisoflavonoid derivatives (5–11) were isolated from the fruits of C. bisexualis for the first time. All the compounds were elucidated by their extensive and comprehensive spectroscopic data and references. Compounds (1−11) were evaluated for their hepatoprotective activities in HepG2 cells by the acetaminophen (APAP)-induced damage model at 10.0 μM with bicyclol as the positive control. Among them, compounds 1, 3, 5, and 6 showed moderately hepatoprotective activities to improve the HepG2 cell survival rates from 51.68 ± 2.49% (APAP, 10 mM) to 71.55 ± 4.08%, 65.95 ± 4.39%, 60.77 ± 3.44%, 62.94 ± 2.30%, respectively. more...
- Published
- 2021
- Full Text
- View/download PDF
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