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The Euphorbia plants are famous for their diterpenoid constituents with diverse structures and broad biological activities. Herein, the discovery of 15 ingenane diterpenoids including 10 previously unreported ones (1 − 10) from Euphorbia antiquorum was presented. Structures of the undescribed compounds were established via detailed spectroscopic analyses. Meanwhile, a preliminary anti-inflammatory screening revealed that compound 6 showed significant inhibitory activity against the production of nitric oxide, as well as downregulated the expression of COX-2 and IL-6, in lipopolysaccharide-stimulated RAW264.7 macrophages. Further mechanistical exploration revealed that compound 6 could exert its anti-inflammatory effect by inhibiting NF-κB and activating Nrf2 signaling pathways. [Display omitted] [ABSTRACT FROM AUTHOR]

Alstoscholarisine L is an architecturally complex monoterpenoid indole alkaloid with a unique ring fusion pattern, isolated from the leaves of Alstonia scholaris. The 6/5/5/6/6/6-membered rings contain two lactonic rings and one aminal carbon and possess seven contiguous aligned stereocenters, three of which are quaternary. Its structure was elucidated by extensive spectroscopic data analyses, quantum chemical computations, and single-crystal X-ray diffraction. The unusual highly fused, cage-like skeleton is possibly derived from picrinine. The fascinating compound exhibited potential antifungal activity against Candida albicans , and its activity was roughly comparable to the first line antifungal drug fluconazole and significantly more effective than the plant-derived antibacterial drug berberine. [Display omitted] [ABSTRACT FROM AUTHOR]

Two undescribed C 17 -Labdane diterpenoid alkaloids, named forsylinfenines A and B (1 – 2) , attributable to a rare 4,4,10,13-tetramethyl-1(2),3(4),5(10),6(7)-octahydrobenzo[ f ]quinolin skeleton, along with three known β -carboline-type alkaloids (3 – 5), were isolated. The chemical structures including absolute configurations of two undescribed compounds were established by means of integrated spectroscopic techniques and electronic circular dichroism (ECD) calculations. In addition, a plausible biosynthetic pathway for the formation of compounds 1 and 2 was proposed. In vitro , five alkaloids (1 – 5), especially two undescribed alkaloids with rare skeleton (1 – 2), exhibited significant anti-inflammatory activities due to inhibiting the release of TNF- α , IL-6, and IL-1 β , as well as effective anti-oxidant activities owing to preventing the production of ROS in the LPS-induced RAW264.7 cells. [Display omitted] • Two undescribed alkaloids bearing a rare 4b,5,6,7,8,8a,9,10-octahydrobenzo[ f ]quinoline skeleton from Forsythia suspensa. • The absolute structures of two undescribed alkaloids were determined by ECD data. • The plausible biosynthetic pathway of two undescribed alkaloids was proposed. • Two undescribed alkaloids had significant anti-inflammatory activities by inhibiting the release of inflammatory factors. • Two undescribed alkaloids had effective anti-oxidant activities by inhibiting the production of ROS. [ABSTRACT FROM AUTHOR]

In this study have been evaluated the antiproliferative and antioxidant activities of Israeli Pulicaria incisa (Lam.) DC. essential oil (Pi1), of essential oil partially purified by xanthoxylin (Pi2), one of its feature metabolites, and the isolated xanthoxylin (Xan). From the compositional analysis carried out by GC–MS oxygenated monoterpenes class was the main class (71.18 %), with cis -chrysanthenol (55.66 %) as the most abundant components, following by carvotanacetone (11.68 %). Other metabolites represented the second class (20.33 %), being xanthoxylin (15.35 %) the principal metabolites, isolated and characterized by NMR tecniques. Pi1 and Xan showed good antioxidant activity causing a clear reduction in ROS levels and an increase in CAT and SOD activity, while Pi2 showed a reduction in enzymatic activity. Furthermore, Pi1 and Xan demonstrated an apoptotic antiproliferative effect in a dose-dependent manner on solid and hematological tumors, unlike Pi2 which showed lower activity. These data showed that P. incisa EO had interesting antioxidant and antitumor activity and that the biological activities exhibited by the essential oil as a whole are mainly due to xanthoxylin. [Display omitted] • Pulicaria incisa is known for its ethnobotanical use. • P. incisa essential oil was characterized by GC–MS and xanthoxylin was purified. • P. incisa essential oil and xanthoxylin were evaluated as antitumor agents. [ABSTRACT FROM AUTHOR]

Although Aristolochia plants remain controversial due to their toxicity, this group of perianth-bearing plants, which includes the medicinal species Aristolochia esperanzae , is among the most relevant from an ethnobotanical perspective. All parts of A. esperanzae are used in popular medicine in the form of infusion for the treatment of rheumatism. Thus, the anti-inflammatory properties and the chemical composition of the aqueous extract (AELS) obtained from A. esperanzae aerial parts were examined in this research. AELS was analyzed using chromatographic, hyphenated, spectrometric techniques, and a total of 35 compounds, seven alkaloids, one alkamide, seven flavonoids, four phenolic compounds, one terpene lactone, three epoxylignans, two dibenzylbutyrolactolic, five dibenzylbutyrolactone, three furofuran lignans, and two labdane diterpenes, were found in this extract. Four doses of AELS (3−300 mg/kg) were administered, by oral route (p.o.), to female Swiss mice in the carrageenan pleurisy test. The dose of 100 mg/kg was tested in Swiss mice in two models: carrageenan, complete adjuvant Freunds (CFA) and zymosan inflammatory models. The AELS extract was assayed using the methylthiazolidiphenyl-tetrazolium bromide (MTT) test to verify the leukocyte viability, and this showed no cytotoxicity in vitro. AELS significantly interfered with nitric oxide production and reduced leukocyte migration to the pleura following carrageenan stimulation. AELS significantly inhibited nitric oxide production, leukocyte migration, and mechanical hyperalgesia after zymosan-stimulated joint inflammatory process. Therefore, the present study demonstrated that AELS exhibits anti-inflammatory properties and is rich in compounds known for their anti-inflammatory potential, thereby supporting the traditional use of A. esperanzae in treating rheumatism. [Display omitted] [ABSTRACT FROM AUTHOR]

Previously undescribed benzophenone rhamnosides, triadenosides A–F (1 – 6), were isolated from the aerial parts of Triadenum japonicum (Blume) Makino (Hypericaceae), where known compounds including benzophenone rhamnosides (7 and 8), benzophenone C -glucoside (9), flavonols and their glycosides (10 – 17), and biflavone (18) were also isolated and identified. Detailed spectroscopic analysis revealed that triadenoside A (1) was 2,3′,5′-trihydroxy-4,6-dimethoxybenzophenone 2- O - α -L-rhamnopyranoside, while the absolute configuration of the rhamnosyl moiety was confirmed by HPLC analysis. Triadenosides B–E (2 – 5) were assigned as acetyl derivatives of 1 in their rhamnosyl moieties. In contrast, triadenoside F (6) was elucidated to be 2,3′,5′,6-tetrahydroxy-4-methoxybenzophenone 2- O - α -L-(4″- O -acetyl)rhamnopyranoside. Compounds 1 – 18 isolated from T. japonicum as well as some benzophenone derivatives (5a – 5e , 6a , and 8a) prepared from 5 , 6 , and 8 were evaluated for their inhibitory activity against RSL3-induced ferroptosis on human hepatoma Hep3B cells, showing significant inhibitory effects of triadenosides A–E (1 – 5) and their derivatives (5c , 5d , and 5e) with EC 50 values ranging from 18.0 to 41.4 nM comparable to that of a ferroptosis inhibitor, ferrostatin-1, whereas triadenoside F (6) did not exhibit such activity. [Display omitted] • Triadenosides A–F were isolated from the aerial parts of Triadenum japonicum. • Their structures were elucidated as benzophenone rhamnosides by spectroscopic and HPLC analyses. • Triadenosides A–E and their derivatives were found to show potent anti-ferroptosis activities. [ABSTRACT FROM AUTHOR]

The Tripleurospermum (L.) Sch.Bip, (Asteraceae) genus, comprises 30 to 40 species widely spread in the northern hemisphere, and across the Mediterranean region. Out of the seven taxa encountered in Greece, four can only be found in specific areas, with limited spread throughout the country. The current work describes the phytochemical investigation, using modern analytical techniques, of the differences between the aerial parts of T. tempskyanum and T. rosellum collected from two floristic regions of Greece (Lesvos isl. and Mt. Parnon) and the common chamomile (Matricaria recutita). GC–MS was first applied for the analysis of the essential oils and dichloromethane extracts, significantly differentiating M. recutita from the Tripleurospermum taxa. Afterwards, a fractionation of T. tempskyanum 's non-polar and polar extracts afforded their major compounds, thus assisting to the unambiguous distinction of different isomers of matricaria lactone, as well as the first-time isolation of demethyl brevisnosideyne. Finally, the polar extracts were analyzed by means of UPLC–Orbitrap–HRMS/MS, revealing similarities among the species, with profiles dominated by cinnamic and flavonoid derivatives and fatty acids, with quantitative differences being observed for specific groups of compounds. Overall, the current study provides novel insight on the phytochemical differentiation between the studied genera and species. [Display omitted] • Tripleurospermum taxa from Greece were investigated. • GC–MS analysis of essential oils and non-polar extracts revealed sample differences. • LC-HRMS analysis of medium/high polarity extracts afforded numerous metabolites. • Matricaria ester isomers were isolated from the non-polar extract of T. tempskyanum. • Demethyl brevisnosideyne was isolated for the first time from T. tempskyanum. [ABSTRACT FROM AUTHOR]

One new polyketide asperfuranone D (1), four new sesquiterpenes derivatives aspergillone C-F (2 – 5) and three known compounds (6 – 8) were successfully isolated from Aspergillus nidulans LZ8, a fungicolous fungi from the macrofungal Ganoderma lingzhi. The structures of these compounds were elucidated by extensive spectroscopic analyses including ultraviolet-visible spectroscopy (UV), mass spectrometry (MS), nuclear magnetic resonance (NMR), and electronic circular dichroism (ECD) calculation. In addition, the anti-inflammatory activities of the new compounds were evaluated using LPS-induced RAW 264.7 cells. The results revealed that compound 5 showed moderate nitric oxide (NO) inhibitory activity with the IC 50 value of 13.19 ± 1.05 μM, while the IC 50 value of the positive control L-NMMA was 41.88 ± 0.91 μM. [Display omitted] • Aspergillus nidulans LZ8 was isolated from Chinese medicinal plant Ganoderma lingzhi. • One new polyketide asperfuranone D (1) and four new sesquiterpenes derivatives aspergillone C-F (2 – 5) were isolated from the fermentation extracts. • Aspergillone F showed moderate nitric oxide (NO) inhibitory activity. [ABSTRACT FROM AUTHOR]

The use of plant bioreactors for the production of medicinal proteins has emerged as a promising and cost-effective alternative to traditional microbial and mammalian cell culture systems. This review provides a focused examination of the critical role of promoters in enhancing the production of therapeutic proteins within plant-based platforms. We discuss the latest advancements in promoter discovery, modification, and optimization for the expression of medicinal proteins in plants. The review highlights the challenges and opportunities associated with various types of promoters, including constitutive, tissue-specific, and inducible promoters, and their impact on medicinal protein yield and quality. Case studies are presented to illustrate the successful application of these promoter engineering techniques in plant bioreactors, emphasizing the potential for scalable and sustainable production of pharmaceutical proteins. Additionally, we explore the strategies for improving promoter function. This review is intended to guide researchers and industry professionals in the selection and design of promoters for the enhanced production of medicinal proteins in plant bioreactors. [Display omitted] [ABSTRACT FROM AUTHOR]

The genus Geum (family Rosaceae) comprises about 70 species, of which several species have been characterized from Eurasia as notably as folk medicines for the treatment of anti-inflammatory, antiseptic, diuretics and astringent. Phytochemical analysis indicated that Geum species produce monoterpenoids, sesquiterpenes, triterpenoids, flavonoids, tannins, phenylpropanoids, and others compounds. Additionally, modern studies have found they possess diverse pharmacological activities such as antioxidant, anti-inflammatory, neuroprotective, antimicrobial, anti-diabetic, cardiovascular, and anti tumor effects. Regardless of the remarkable medical potential of Geum extracts, clinical studies are limited and need to be performed to produce safer and less expensive plant-based drugs. This literature review aims to provide a comprehensive overview of Geum species, covering their traditional uses, phytochemistry, and pharmacological activities, and to summarize the current research status to better understand the application value of Geum plants in modern phytotherapy. [Display omitted] [ABSTRACT FROM AUTHOR]

Nine jatrophane diterpenoids, including six previously undescribed compounds, were extracted and purified from whole plants of Jatropha curcas L. Their structures including absolute configurations were characterized by spectroscopic, quantum chemical Nuclear Magnetic Resonance Spectroscopy, Electronic Circular Dichroism calculation, and Single Crystal X-Ray Diffraction methods. These compounds were evaluated for their ability to reverse multidrug resistance. Among the above compounds, compound 6 showed significant potential as a multidrug resistance modulator, exhibiting higher chemo reversal effects and lower toxicity compared to the positive control verapamil. These findings suggest that compound 6 has promising anticancer properties. Jatrophane diterpenoids from Jatropha curcas, collected from Hainan Province, China. [Display omitted] • Nine jatrophane diterpenoids were isolated from Jatropha curcas, including six undescribed ones. • Their absolute configurations were elucidated by X-ray and ECD analyses. • These compounds exhibited P-gp-mediated MDR reversal activity ranging from 54.4 to 158.1. • The contents of the structure–activity relationship (SAR) was described. [ABSTRACT FROM AUTHOR]

Seven benzylisoquinoline alkaloids, including three new (1 – 3) and four known compounds (4 – 7), were isolated from the embryo of Nelumbo nucifera (Plumula Nelumbinis). Their structures were elucidated by UV, IR, HRESIMS, 1D and 2D NMR, and ECD spectra, as well as optical rotations. All compounds were tested for the antioxidant activity. Compounds 1 – 7 prevented Fe2+ induced lipid peroxidation in mouse liver microsomes, with the inhibitory rates of 76.1, 75.7, 60.0, 82.9, 75.5, 83.8 and 85.3 %, respectively. [Display omitted] • Three new benzylisoquinoline alkaloids were got from Plumula Nelumbinis. • Structures were determined based on HRESIMS, NMR and ECD data. • All benzylisoquinolines showed antioxidant effects. [ABSTRACT FROM AUTHOR]

The genus Thesium, family Santalaceae, comprises about 350 species, and, although many of them are used as functional food and in traditional medicine, there are limited studies evaluating their pharmacological potential. The present study was designed to evaluate the chemical profile, antioxidant, and enzyme inhibition potential of aerial parts and roots of T. bertramii Azn. Extracts were rich in phenolics: MeOH and aqueous extracts of the aerial parts showed the highest total phenolic and flavonoid contents and the best antioxidant activity in most assays. Ethyl acetate extracts of both organs exerted comparable anti-butyrylcholinesterase activity, while their methanol extracts displayed comparable anti-tyrosinase activity. The highest acetylcholinesterase inhibitory activity was recorded from the root's ethyl acetate extract, while that of the aerial parts revealed the best α-amylase and α-glucosidase inhibitory activity. Chemically, the aerial parts were dominated by quercetin derivatives, feruloylquinic acids, caffeoylquinic acids, and elenolic acid glucoside. Roots showed a lower diversity of compounds with elenolic acid, quercetin glycoside, and kaempferol glycoside as major compounds. Additionally, network pharmacology analyses (KEGG and STRING) identified critical molecular pathways and hub genes, including IL6, TNF, BCL-2, and JUN, indicating the multi-target potential of T. bertramii in cancer and cardiovascular diseases. In conclusion, this study assessed the chemical and biological properties of T. bertramii for the first time , and the obtained results indicated the potential of this species as a valuable source of bioactive molecules for the pharmaceutical, food, and cosmetic industries. [Display omitted] [ABSTRACT FROM AUTHOR]

The antioxidant activity of Scorzonera parviflora Jacq. roots were assessed by measuring their ability to scavenge ABTS and DPPH radicals. Bioactivity-guided fractionation was utilized to identify the compound(s) responsible for this activity. The most active phase, ethyl acetate, was isolated using column chromatography. The resulting fractions were then purified using preparative TLC on reverse phase and semi-preparative HPLC. The structures of the pure compounds were elucidated by spectral analysis (MS and 1H, 13C, 2D-NMR). Three undescribed phenolic acid derivatives, namely parvifloric acid A (1) , B (2) , and C (3) , and one new sesquiterpene lactone, parviflorin (4) together with seven known compounds were isolated and identified as scopolin (5) , scopoletin (6) , caffeic acid (7) , protocatechuic acid (8) , 4,5- O -dicaffeoylquinic acid (9) 3,5- O -dicaffeoylquinic acid (10) , and 3,5- O -dicaffeoylquinic acid methyl ester (11). Finally, the pure compounds obtained were tested to evaluate their antioxidant capacities, using ABTS and DPPH radical scavenging potencies. The highest activity was observed with 3,5- O -dicaffeoylquinic acid (10) , followed by its methyl ester. [Display omitted] • The roots of Scorzonera parviflora Jacq. revealed significant anti-oxidant activity. • Three undescribed phenolic acids and one sesquiterpene lactone were isolated. • Seven known compounds including dicaffeoylquinic acid derivatives were isolated. • The highest antioxidant activity was observed by 3,5- O -dicaffeoylquinic acid. [ABSTRACT FROM AUTHOR]

Two new sesquiterpenol caffeates, bausesquitate A (1) and bausesquitate B (2), were isolated from the stems and leaves of Bauhinia brychycarpa. Structures of two compounds were confirmed by UV, IR, HR-ESI-MS, 1D and 2D NMR, ECD spectra and DP4+ probability analysis. In vitro, compounds 1 and 2 showed better inhibitory effect on α -glucosidase than acarbose (IC 50 = 280.50 ± 6.27 μM) with the IC 50 values of 1.81 ± 0.12 μM and 3.79 ± 0.27 μM. Additionally, molecular docking and molecular dynamics simulation were performed to analyze the potential binding sites. [Display omitted] • Bausesquitates A and B, two new sesquiterpenol caffeates were isolated from Bauhinia brachycarpa and the structures of them were confirmed. • Compounds 1 and 2 showed significant inhibitory effect on α -glucosidase with IC 50 values of 1.81 ± 0.12 μM and 3.79 ± 0.27 μM. • The sesquiterpenol units could significantly enhanced the inhibitory activity of caffeic acid on α -glucosidase. • Molecular docking and MD simulation were performed to unveil the potential binding sites and the stability of docking complexes. • This is the first reported occurrence of sesquiterpenol caffeates in the genus Bauhinia. [ABSTRACT FROM AUTHOR]

Two populations of Physalis patula Miller collected in different localities (Querétaro and Teotihuacán) of Central México were analyzed. Eight new compounds including three withanolides, physapatolides A-C (1 – 3), two labdanes, 12- epi -physacoztomatin (10) and physapatulone (12), besides three 12- O -glucosyl labdanes, patulosides A-C (13 – 15), were isolated from these collections. A series of known withanolides, flavonoids, labdanes, sucrose esters, and sterols were also isolated. Withanolides isolated of each population exhibited different substitution patterns of ring D, thus while 15,16-dioxygenated withanolides were found in the Querétaro population, oxygenation occurs at C-14 and C-15 in those isolated from Teotihuacán population. The structures of all the isolated compounds were determined by analysis of their spectroscopic and spectrometric data. The absolute configuration assigned to physapatolide A (1) was confirmed by X-ray diffraction analysis of its acetyl derivative 1a , while those of labdane diterpenoids were based on chemical correlations. The antibacterial activity of 16 of the isolated compounds (1 – 3 , 5 – 9 , 13 , 14 , and 16 – 21) and two derivatives (13a , 14a) was evaluated against five ATCC bacterial strains (Escherichia coli , Klebsiella pneumoniae , Pseudomonas aeruginosa , Staphylococcus aureus and Bacillus subtilis). Compounds 1 – 3 inhibited around 100 % the growth of S. aureus at 250 μ g/mL (w/v). The minimum inhibitory concentrations (MIC) of compounds 1 , 2 , and 3 , against S. aureus were 62.5, 125 and 62.5 μ g/mL, respectively, whereas their MIC's against a Methicillin-resistant S. aureus (MRSA) clinical isolate were 125, 62.5 and 62.5 μ g/mL, respectively. [Display omitted] • New (1 – 3) and known (5 – 8) withanolides were isolated from these populations. • The D-ring substitution pattern of withanolides was different for each population. • 12 R and 12 S -hydroxylabdanes and their glucosides were also isolated. • Both populations contained known methoxylated flavonols, sucrose esters, and sterols. • Among 18 compounds tested, withanolides 1 – 3 showed the best antibacterial activity. [ABSTRACT FROM AUTHOR]

Euodia Fruit is a crude drug used to treat migraine and headaches and is well-known to contain indole alkaloids, which may contribute to the observed pharmacological activities. A methanolic extract of Euodia Fruit exhibited pancreatic lipase inhibitory activity (IC 50 13.9 mg/mL). Bioassay-guided fractionation of the extract led to the isolation of 14 quinolone alkaloids (1 – 14), three indole alkaloids: rutaecarpine (15), evodiamine (16), and dehydroevodiamine (17), and a limonoid: rutaevine acetate (18), among which three quinolone alkaloids (12 – 14) have been previously undescribed. The structures of 12 – 14 were determined by extensive spectroscopic analyses, including two-dimensional (2D) NMR. Compounds 2 , 3 , 6 – 9 , 13 , and 14 exhibited pancreatic lipase inhibitory activity, with IC 50 values ranging from 1.40 to 7.37 mM. The results revealed that the length of the aliphatic side chain and the presence of an olefinic bond at the C-2 side chain of the quinolone alkaloids could impact lipase inhibitory activity. In soybean oil-loaded mice, orally administered evocarpine (8) reduced serum triglyceride levels in a dose-dependent manner. Furthermore, 8 – 14 at 5.0 and 50 μM exhibited peroxisome proliferator-activated receptor (PPAR)-γ ligand-binding activity. [Display omitted] [ABSTRACT FROM AUTHOR]

The medicinal folk plant Tithonia diversifolia A. Gray has traditionally been used to treat hepatitis and liver cancer. However, the anti-fibrotic effect of this plant extract and its main active substances remain unclear. This study aims to elucidate the anti-fibrotic effect of T. diversifolia ethanol extract, identify the main active substances, and explore their possible molecular mechanisms. Firstly, carbon tetrachloride (CCl 4) was injected intraperitoneally to induce liver fibrosis in mice to investigate the protective effect of T. diversifolia ethanol extract. Then, thirty compounds in this extract were identified through liquid chromatography-mass spectrometry (LC-MS/MS) analysis, column chromatography, and spectroscopic analysis. In addition, the anti-fibrotic effect of sesquiterpene lactone compounds were investigated on TGF-β-induced hepatic stellate cell activation. The T. diversifolia ethanol extract significantly inhibits symptoms of carbon tetrachloride-induced liver fibrosis and the collagen deposition in pathological tissues by suppressing the protein expression of various pro-fibrotic factors. A comprehensive profile of thirty-one compounds was established, including nine sesquiterpenes, six phenolic acids, six fatty acids, five phenylpropanoids, and three flavonoids. Notably, one previously unreported sesquiterpene lactone, namely 1β-ethoxydiversifolin 3- O -methyl ether (1), together with twenty-nine known compounds were obatined. Sesquiterpene Tagitinin C shows significant anti-fibrotic effects on TGFβ1-induced HSC-T6 activation by inducing cell apoptosis and regulating the TGF-β1/Smad pathway. The above results indicate that the T. diversifolia extract can effectively alleviate liver fibrosis, with sesquiterpene lactones being a major component. In the future, the germacranolides-type of sesquiterpene lactone Tagitinin C can be developed as a precursor compound for anti-fibrotic therapy. [Display omitted] [ABSTRACT FROM AUTHOR]

Four new iridoids elucidated as jasmigeniposide C (1), jasmigeniposide D (2), jasmigeniposide E (3), and jasmigeniposide F (4), along with six known iridoids (5 – 10) were isolated from the flowers of Gardenia jasminoides. Their structures were determined on the basis of spectroscopic analyses and chemical reactions. The antioxidant activities of these compounds were preliminarily evaluated by DPPH radical scavenging assay. The results revealed that compounds 1 – 5 exhibited some antioxidant activity. Notably, compound 2 displayed the most potent antioxidant activity among the tested compounds. [Display omitted] [ABSTRACT FROM AUTHOR]

Five new coumarins, including three phenypropaninized coumarins edgegardnerols A–C (1 – 3), two bicoumarins edgegardnerols D and E (4 and 5), along with eight known analogues, were isolated and identified from the dried buds of E. gardneri. Their structures were elucidated by comprehensive analysis of their NMR, IR, UV, HR-ESI-MS, and ECD data. Furthermore, the absolute configurations of the glucose moiety were confirmed by HPLC analysis after acidic hydrolysis and chemical derivatization. The cytotoxic activities of all isolated compounds were evaluated against A549 and SMMC-7721 cell lines. Among the tested isolates, compound 12 showed the most potent cytotoxicity with IC 50 values of 22.65 μM and 25.83 μM in these two cell lines, respectively. Compared with cisplatin (29.78 μM), compound 12 exhibited stronger cytotoxic activity in A549 cell line. The preliminary structure-activity relationship showed that 7-hydroxy group on coumarin skeleton was structurally required for the cytotoxity against the A-549 and SMMC-7721 cell lines. [Display omitted] • Five new coumarins were isolated and identified from Edgeworthia gardneri. • Umbelliferone (12) exhibited the most potent cytotoxicity in A549 and SMMC-7721 cell lines. • This investigation may contribute to the discovery of potential anticancer agents. • This study will broaden the application of Edgeworthia gardneri in anticancer fileld. [ABSTRACT FROM AUTHOR]

Three previously undescribed 5,6,7,8-tetrahydro-2-(2-phenylethyl)chromones, (5 S ,6 R ,7 S ,8 S)-8-chloro-5-ethoxy-6,7-dihydroxy-2-[2-(4′-methoxyphenyl)ethyl]-5,6,7,8-tetrahydrochromone (1), (5 R ,6 S ,7 R ,8 R)-8-chloro-5-ethoxy-6,7-dihydroxy-2-(2- phenylethyl)-5,6,7,8-tetrahydrochromone (2), (5 S ,6 R ,7 S ,8 R)-5,8-dichloro-6,7- dihydroxy-2-[2-(4′-methoxyphenyl)ethyl]-5,6,7,8-tetrahydrochromone (3), and 28 known analogues (4 – 31) were isolated from the stems of Aquilaria sinensis. Their structures were characterized by the spectroscopic methods, and the absolute configuration was resolved by circular dichroism (CD) spectroscopy. Bioactivity evaluation indicated that compounds 3 – 8 had significant inhibition effect in the production of NO in an inflammatory cell model with relatively lower IC 50 values of 5.54, 11.44, 3.68, 7.15, 10.26 and 13.04 μM, respectively, compared to the positive control indomethacin (IC 50 = 23.03 μM). [Display omitted] • Three new and twenty-eight known chromones derivates were isolated from the stems of Aquilaria sinensis. • Three new compounds have chlorine atoms substituted at the cyclohexene ring. • Compounds 3 – 8 had excellent anti-inflammatory activity (IC 50 value ranges from 3.68 to 13.04 μ M). [ABSTRACT FROM AUTHOR]

Hymenocallis littoralis , commonly known as Coastal Spider lily, is a perennial herbaceous plant in the Amaryllidaceae family. It is native to tropical and subtropical regions of the Americas, celebrated for its remarkably beautiful flowers. In this study, five previously undescribed chromones, one new benzopyran, along with five known chromones and fourteen known flavonoids, were identified. Among these, compounds 6 , 9 , 12 , 18 , 19 , 20 , and 22 were natural products isolated from H. littoralis for the first time. Their structures were determined using spectroscopic techniques (NMR and MS). Anti-inflammatory activities of the isolated chromone and benzopyran were evaluated in lipopolysaccharide (LPS) stimulated RAW 264.7 macrophage cells. Compound 11 exhibited significant inhibitory effects on nitric oxide (NO) production with an IC 50 value of 38.24 μ M. Further investigations revealed that compound 11 exerted its anti-inflammatory activity by preventing the nuclear translocation of NF- κ B and down-regulating the expression of pro-inflammatory factors, including iNOS, COX-2, IL-1 β , and IL-6, in a concentration-dependent manner. This study provides evidence that benzopyran from H. littoralis may serve as a potential source of an anti-inflammatory agent. A previously undescribed benzopyran with potential anti-inflammatory activity along with five new chromones were isolated and identified from Hymenocallis littoralis (Jacq.) Salisb. [Display omitted] • Non-alkaloid components in the bulbs of Hymenocallis littoralis were investigated. • Six undescribed compounds were isolated and identified from H. littoralis. • Compound 11 is a benzopyran, and compounds 1–10 are chromones. • Compound 11 suppressed the expression of iNOS and COX-2 in RAW 264.7 cells. [ABSTRACT FROM AUTHOR]

The Piperaceae family is distributed widely in tropical and subtropical areas. It encompasses around 5 genera and over 3000 species. They are distinguished by the substantial chemical diversity and potential medicinal applications. Amide alkaloids, as the main secondary metabolites in the Piperaceae family, exhibit various biological activities, and the discovery of [2 + 2] and [4 + 2] amide alkaloid dimers has led to a surge in phytochemical research on Piperaceae plants. Although the identification of these dimers has been gradually increasing in recent years, there remains a lack of comprehensive and systematic evaluations of these compounds. This review aims to summarize the latest advancements in the research on natural amide alkaloid dimers, focusing on their structural diversity, biological activities and biosynthetic pathways, and the enzymatic advances of [2 + 2] and [4 + 2] cyclase enzymes. Until October 2024, research has documented 99 amide alkaloid dimers, including 37 dimers possessing [2 + 2] cyclobutanes skeletons and 62 [4 + 2] cyclohexene skeletons derived from the Piperaceae family. These compounds demonstrate a range of in vitro biological activities including anti-inflammatory, anticancer, acetylcholinesterase inhibitory, anti-platelet aggregation, hepatoprotective, antimalarial, antitubercular, anti-diabetic and notable interactions with CYP3A4 and CYP2D6 enzymes. A systematic review of these [2 + 2] and [4 + 2] amide alkaloid dimers in Piperaceae family can provide a critical scientific foundation and theoretical support for the discovery and development of novel pharmaceutical agents. [Display omitted] [ABSTRACT FROM AUTHOR]

Anxiety and depression are mental disorders that have been exponentially increasing over the last decades. Psychopharmacology emerged to try to alleviate the symptoms of these disorders; however, the side effects and the time it takes to achieve the desired effect are factors that decrease the search for and adherence to treatment. To remedy this situation, new compounds capable of improving the performance of these medications and reducing their adverse effects have been sought. The use of medicinal plants has been widely employed for this purpose. Mauritia flexuosa F.L., a palm tree with high incidence in Brazil, has been heavily targeted as all its parts are usable. The objective of this study is to evaluate the effects of fixed oil from the fruit of the buriti palm in models of depression and anxiety. The phytochemical profile of this oil and its toxicity were also investigated. The experiments conducted included the open field, rotarod, forced swim, and elevated plus maze tests. As a result, it was observed that the fixed oil from buriti palm presented 18 compounds, with elaidic acid being the major one, and showed no signs of toxicity. However, it demonstrated a possible stimulating activity in the open field test and had no effect on the motor system in the rotarod test. Furthermore, it exhibited an antidepressant-like effect in the forced swim test but an anxiety-like effect in the elevated plus maze test. Therefore, buriti oil may potentially be used in new formulations to assist in the treatment of anxiety and depression. [Display omitted] [ABSTRACT FROM AUTHOR]

Trifoliate yam (Dioscorea dumetorum) is traditionally used to treat diabetics in Nigeria. However, almost no information is available on its antidiabetic constituents and their natural variance. Hence, the activity of methanolic tuber extracts of 67 trifoliate yam accessions from the largest collection in Africa was proven by four colorimetric antidiabetic and antioxidant in vitro assays, as diabetes is also linked with oxidative stress. For the first time, selected accessions were also analyzed by planar bioactivity profiling. It has a comparatively higher, more differentiated information content, is more sustainable in terms of material consumption, and enables straightforward compound prioritization and characterization. Up to a dozen individual antioxidant zones were revealed as well as one prominent zone inhibiting α-glucosidase and α-amylase. The latter inhibition zone was tentatively assigned to palmitic, linoleic, oleic, linolenic, oxo-nonanoic fatty acids by direct elution to heated electrospray ionization high-resolution mass spectrometry. [Display omitted] • Antidiabetic potential of 67 African trifoliate yam accessions was explored for tailor-made food. • For the first time, characteristic antidiabetic and antioxidative profiles were obtained by planar assays. • Elimination of matrix interference ensured planar assays outperformed in vitro assays • Targeted characterization of bioactive compounds by high-resolution mass spectrometry. • Palmitic, linoleic, oleic, linolenic, oxo-nonanoic acids were tentatively assigned to the antidiabetic zone. [ABSTRACT FROM AUTHOR]

2-(2-Phenylethyl)chromones (PECs), the pivotal constituents responsible for the distinctive aroma and pharmacological potential of agarwood, are primarily obtained through extraction from natural materials. The restricted availability of agarwood has, however, hindered a comprehensive and systematic evaluation of their biological properties. In this study, we have chemically synthesized a total of 38 PEC derivatives, including 23 new compounds that had not been previously isolated from agarwood. These compounds were then evaluated for their inhibitory effects on nitric oxide release, neutrophil superoxide production, as well as their activities against tyrosinase, acetylcholinesterase, and α -glucosidase. The preliminary screening resulted in the identification of promising leads with potential therapeutic activities, and the structure-activity relationship of the synthesized PECs have also been briefly discussed. The results provide a foundation for the synthesis and pharmacological exploration of PECs, which sheds light on the pharmacological potential of agarwood's secondary metabolites. [Display omitted] [ABSTRACT FROM AUTHOR]

Cellular senescence, the irreversible arrest of cell division, is a hallmark of aging and a key contributor to age-related disorders. Targeting senescent cells represents a promising therapeutic approach to combat these ailments. This review explores the potential of Garcinia species, a genus rich in flavonoids with established antioxidant and anti-inflammatory properties, as a source of natural anti-senescence agents. We investigate the intricate connections between aging, cellular senescence, and oxidative stress, highlighting the detrimental effects of free radicals on cellular health. Furthermore, we analyze the diverse array of flavonoids identified within Garcinia and their established cellular mechanisms. We critically evaluate the emerging evidence for the anti-senescence potential of flavonoids in general and the limited research on Garcinia flavonoids in this context. By identifying existing knowledge gaps and paving the way for future research, this review underscores the exciting potential of Garcinia flavonoids as natural anti-senescence agents. These agents hold promise for not only promoting healthy aging but also for the development of cosmeceutical products that combat the visible signs of aging. [Display omitted] [ABSTRACT FROM AUTHOR]

Polygala tenuifolia Willd., a famous traditional Chinese medicine, has been widely applied to treat central nervous system diseases. In this study, P. tenuifolia root extract exhibited a moderate anti-ischemic effect on in-vitro oxygen-glucose deprivation/reperfusion (OGD/R) model. In transient middle cerebral artery occlusion (tMCAO) rats, P. tenuifolia root extract significantly attenuated brain infarction and neurological deficits in a dose-dependent manner. Compared with the sham group, the release of damage-associated molecular patterns (DAMPs)-HMGB1 in the ischemic brain was significantly higher, which was inhibited by P. tenuifolia root extract. To further explore such neuroprotective effects whether associated with aseptic inflammation, HMGB1-activated BV2 microglial cells model was established. The extract of P. tenuifolia was found to inhibit the downstream inflammatory response driven by HMGB1, with an IC 50 value of 49.46 μg/mL. In addition, the extract was also found to be able to directly interact with HMGB1 in the surface plasmon resonance (SPR) experiment. Phytochemical studies showed that the extract of P. tenuifolia root contains a large number of terpenoids, oligosaccharides and phenolic compounds, which likely contribute to the above observed biological activities. Our results not only provide some data support for the clinical application of P. tenuifolia against cerebral ischemia, but also clarify the potential target of P tenuifolia 's anti-inflammatory properties. [Display omitted] • Polygala tenuifolia root extract exhibited significant anti-ischemia effect on OGD/R cell model and tMCAO rats. • P. tenuifolia was found to dose-dependent inhibit the downstream inflammatory response driven by HMGB1 after ischemic stroke. • The anti-neuroinflammatory activity of P. tenuifolia is related to its effective ingredients and interaction with HMGB1. [ABSTRACT FROM AUTHOR]

Globally, Alzheimer's disease is an urgent public health concern with the ageing population in developing nations. Recent studies have identified isosteroidal alkaloids as promising therapeutic agents for Alzheimer's treatment. Fritillaria species are well-known rich sources of steroidal and isosteroidal alkaloids. In this context, the current study focuses on the biochemometric-guided isolation of three previously undescribed and two known isosteroidal alkaloids as acetylcholinesterase (AChE) inhibitors from the bulbs of Fritillaria cirrhosa D.Don. The isolated molecules were characterized by NMR, HR-ESI-MS, FT-IR, and DP4+ analysis. Subsequently, all isolates were evaluated for AChE inhibitory activity using Ellman's method. Among the evaluated molecules, 1 (IC 50 : 33.0 ± 4.4 μM) and 5 (IC 50 : 24.7 ± 4.5 μM) showed promising AChE inhibition in vitro. Enzyme kinetic studies of isolated molecules revealed mixed inhibition kinetics with K i varying from 1.3 to 24.4 μM. Moreover, the in silico studies showed excellent binding affinities of isolated molecules with the target protein and good drug-like ADMET properties. The present study identified new isosteroidal alkaloids as promising AChE inhibitors from F. cirrhosa bulbs via a biochemometric approach and advocated their further exploration for treating neurodegenerative disorders. [Display omitted] [ABSTRACT FROM AUTHOR]

Two unusual isosativene sesquiterpene derivatives, named dendronobilol A (1) and dendronobilside A (2), and two unusual sativene sesquiterpene derivatives, named dendronobilsides B (3) and C (4), had been isolated from the stems of Dendrobium nobile. The structures of all the compounds were established using spectroscopic methods and by comparison with literature data, and their absolute configurations were confirmed via single-crystal X-ray diffraction data and electronic circular dichroism (ECD) calculations. Dendronobilol A (1) and dendronobilside A (2) possessed a unique tricyclo[4.3.0.12, 8]decan ring system, while dendronobilsides B (3) and C (4) presented a unique tricyclo[4.4.0.02, 8]decan core carbon skeleton. The above two types of sesquiterpene derivatives had been isolated and purified from plants for the first time. Compounds 1 and 2 exhibited significant effects on glucose consumption with doses of 20 and 40 μmol/L in insulin-resistant HepG2 cells, and thus improve insulin resistance. [Display omitted] • Four unusual sesquiterpene derivatives were isolated from Dendrobium nobile • Dendronobilol A possesses a unique tricyclo[4.3.0.12, 8]decan ring system. • Dendronobilsides B and C present a unique tricyclo[4.4.0.02, 8]decan ring system. • Improving insulin resistance was confirmed with isolated isosativene sesquiterpenes [ABSTRACT FROM AUTHOR]

Garcinia smeathmannii is a well-known plant for its uses in the effective treatment of intestinal parasites, skin eruptions and skin burns. The dichloromethane-methanol (2:3) crude extract of the leaves of G. smeathmannii led to the isolation and characterization of twenty compounds (1 − 20) using chromatographic and spectroscopic techniques. Extracts and compounds were screened in vitro for their anti-inflammatory (ROS), antiglycation and antileishmanial (L. tropica) activities. Compounds were also screened for their in silico anti-inflammatory activities using Maestro 4.2.1 software with the co-crystal complex structures of the ovine oCOX-1: meloxicam (PDB Id: 4O1Z) and murine mCOX-2: meloxicam (PDB Id: 4M11) proteins. An unprecedented flavonol (1) and a flavone dimer (2) together with eighteen known compounds (3 − 20) were characterized. All the tested samples in vitro revealed no antiglycation and antileishmanial activities. Beside, extracts revealed moderate anti-inflammatory activities (IC 50 ranging from 24.1 ± 2.0 to 34.7 ± 0.8 μg/mL). Only compound (13) revealed an anti-inflammatory activity which was 9.33 times more active than the reference (Ibuprofen, IC 50 = 11.2 ± 1.9 μg/mL) with IC 50 of 1.2 ± 0.0 μg/mL. Compounds (2 – 9 , 11 – 13 and 19 – 20) were docked and the docking scores were ranging from −10.178 to −6.119 (kcal/mol) which were in agreement with the experimental anti-inflammatory activity. These results are in agreement with the traditional uses of the leave of G. smeathmannii as cataplasm for skin eruption and as analgesic agent. [Display omitted] • Phytochemical investigation of Garcinia smeathmannii (Planch. & Triana) Oliv. • Chemophenetic significance of the isolated compounds. • Anti-inflammatory (ROS), antiglycation and antileishmanial (L. tropica) screening of samples from G smeathmannii. • Molecular docking of the isolated compounds for anti-inflammatory potencies. [ABSTRACT FROM AUTHOR]

Peucedanum japonicum (the family Umbelliferae) is a perennial herbaceous plant with various crucial traditional values for coughs, colds, headaches, and inflammatory responses. For drug developments, the current research aims to offer an overview of the previous results in the three main aspects of traditional use, phytochemistry, pharmacological values, and molecular mechanisms regarding this medicinal species. By chromatographic analysis and separation, more than 120 isolated compounds have been obtained. Khellactone-type coumarins and phenolic compounds are the primary phytochemical classes with some coumarins, such as calipteryxin, praerutorin A, and pteryxin, being the main metabolites. Pharmacological activities of P. japonicum constituents included anticancer, antioxidative, antimicrobial, antiviral, antiplatelet, and tyrosine inhibitory activities, especially anti-inflammation and anti-obesity. It is worth mentioning that the obtained constituents joined to protect the neurons, bone, and urine systems, and exerted vasorelaxant. In general, the underlying mechanism of anti-inflammatory action can be explained by mitogen-activated protein kinase/nuclear factor-kappa B (MAPK/NF-κB) signaling pathway, whereas anti-obesity activity is deduced from regulating lipid metabolism-related genes. It also noted that pteryxin is the most active compound, but the clinical studies and synthesis of new derivatives containing enhanced medicinal values have been still limited, which should be improved. [Display omitted] [ABSTRACT FROM AUTHOR]

Three new neoclerodane diterpenoids (1–3), two new steroids (4–5), one new monoterpene (6), one new derivative of benzaldehyde (7) and one new iridoid glycoside (8), along with 19 known phenolic compounds, were isolated from Clerodendrum trichotomum. Their structures were established by a combination of detailed spectroscopic analyses (1D and 2D NMR) and high resolution electrospray ionization mass spectroscopy (HRESIMS). The isolated compounds were screened on α -glucosidase inhibitory and the peroxisome proliferator-activated receptor gamma (PPAR- γ) agonist activities, and the results showed that three phenylethanoid glycosides, verbascoside (9), leucosceptoside a (10), and isoacteoside (13), and two flavonoids, apigenin (22) and luteolin (26) showed potent inhibitory effects against α-glucosidase, with IC 50 values in the range from 15 to 700 μM. In addition, four flavonoids apigenin 7 -O-β -D-glucuronide (19), apigenin (22), luteolin (26), and quercetin (27) exhibited significant PPAR- γ agonistic activities with EC 50 values in the range 2.3–24.9 μM. [Display omitted] • Three new neo-clerodane diterpenoids, two new steroids, one new monoterpene, one new derivative of benzaldehyde and one new iridoid glycoside, were isolated and elucidated by comprehensive spectra anlyses. • Compounds 9 , 10 , 13 , 22 and 26 showed strong inhibitory capacity against α-glucosidase (IC 50 values ranging from 15 to 700 μM) • Compounds 19 , 22 , 26 and 27 exhibited significant peroxisome proliferator-activated receptor gamma (PPAR- γ) agonistic activity (EC 50 values in the range 2.3–24.9 μ M). [ABSTRACT FROM AUTHOR]

Six new prenylated flavonoids, named visconaeas A-F (1–6), and eleven known isopentenyl flavonoids (7–17) were isolated from Dodonaea viscosa (L.) Jacq. The structures of the separated compounds were determined through comprehensive spectral analysis and quantum chemical calculations. These compounds were tested for their anti-Zika virus and cytotoxicity activities. The results indicated that compound 4 showed low cytotoxicity and strong anti-Zika virus potential with EC 50 16.34 μM. [Display omitted] [ABSTRACT FROM AUTHOR]

Delphinium belongs to Ranunculaceae, which is widely distributed in Northwest China. In folk, this genus of plants has analgesic, anti-inflammatory, and insecticidal effects. By studying non-alkaloid components in the whole herbs of Delphinium forrestii , we obtained a total of 11 compounds (1 − 11), including five new (1 – 5) and six known polyphenols (6 – 11). On the basis of chemical evidences and spectral data analysis (UV, Optical rotation data, 1D/2D-NMR and HR-ESI-MS), the structures of new compounds were elucidated. The inhibitory effect of compounds 1 – 11 on lipopolysaccharide (LPS) induced NO production in RAW 264.7 cells was detected. Compounds 4 and 11 showed significant inhibitory effects. This study indicated the presence of compounds with good anti-inflammatory activity among non-alkaloid components in the whole herbs of Delphinium forrestii. [Display omitted] • Five new and six known non-alkaloid components were isolated from the whole herbs of Delphinium forrestii. • UV, NMR, ORD and HR-ESI-MS were used to determine the structure of new compounds. • Two compounds showed significant anti-inflammatory effects. [ABSTRACT FROM AUTHOR]

The prevalence of chronic venous disease (CVD) is relatively high, it affects 20–80 % of the population worldwide. CVD may affect any veins in the human body, however, the veins of the lower extremities are the most susceptible to this condition. Among therapeutic possibilities for CVD, mainly chronic venous insufficiency, some medicinal plants (Ruscus aculeatus L., Aesculus hippocastanum L., Centella asiatica (L.) Urb.) and their active compounds (ruscoside, aescin, asiaticoside) or close derivatives also have important places. This review describes shortly the updated knowledge on pathophysiology, clinical manifestations, evaluation, and diagnostics of CVD as well as treatment modalities. The primary focus of this review is on the existing knowledge about botanical medications for treating chronic venous disease (CVD). It covers the chemical makeup of these plant drugs, their pharmacological effects, results from clinical trials involving humans, and any associated safety concerns. [Display omitted] [ABSTRACT FROM AUTHOR]

Crossopteryx febrifuga (Rubiaceae) is a plant widely used in traditional African medicine to treat tryapnosomiasis. The aim of our study was to evaluate the antitrypanosomal activity of C. febrifuga extracts and to identify the compounds responsible for this activity. We prepared 4 extracts by successive maceration of plant leaf powder in n-hexane , dichloromethane, methanol and water. The antitrypanosomal activity of the extracts was assessed on Trypanosoma brucei brucei and their selectivity on Leishmania mexicana mexicana and human non cancer WI38 fibroblast cells. The dichloromethane extract, the most antitrypanosomal (IC 50 of 9.3 ± 0.8 μg/mL) was fractionated on an Open Column Chromatography to give 14 fractions. Fractions 6–9 were the most active with an IC 50 ranging from 1.3 to 2.1 μg/mL. All fractions were analyzed by UPLC-ZenoTOFHRMS, followed by manual dereplication of metabolites detected in the most active fractions. Manual dereplication was aided by the Molecular Network (MN) and SIRIUS. Metabolic profiling of fractions 6–9 has enabled us to identify 33 compounds, most of which were reported for the first time in C. febrifuga. These include buddlenol C (6), naringenin (7), maslinic acid (22), corosolic acid or isomer (24), asperphenamate (25), hydroxyoctadecenoic acid (29), sumaresinolic acid or isomer I and II (30 and 31), glycyrrhetinic acid (32) and oleanolic acid (36). The bioactivity-based approach identified maslinic (22), corosolic (24), and oleanolic (36) acids as linked to the antitrypanosomal activity. The data obtained support the traditional use of C. febrifuga in the traditional treatment of trypanosomiasis. Further studies are required to verify the activity observed in vivo. [Display omitted] • Antitrypanosomal activity and cytotoxicity of Crossopteryx febrifuga leaf extracts and its fractions are determined • Thirty-three compounds are identified in the most active fractions using HPLC-MS/MS analysis and Molecular Networking • Dereplication on SIRIUS gave an excellent result • Bioactivity-Based approach allowed to predict the compounds responsible for antitrypanosomal activity in C. febrifuga [ABSTRACT FROM AUTHOR]

Phytochemical investigation of the stems of Mallotus paxii Pamp. led to the isolation and identification of four new compounds, including three neolignans (1 – 3) and one phenol (13), along with eight known neolignans (4 – 12) and one known phenol (14). Their structures were determined by spectroscopic methods, including NMR, MS and ECD analyses. Bioassay demonstrated that malloapelin A (4) exhibited a most potent anti-inflammatory activity to NO release with IC 50 value of 21.32 μM. Furthermore, malloapelin A (4) markedly decreased the secretion of TNF- α , iNOS, and NF- κ B and inhibited the expression of COX-2 and NF- κ B/p65 in LPS-induced RAW264.7 cells in a dose-dependent manner. [Display omitted] • Four new compounds, including three neolignans (1 – 3) and one phenol (13), along with eight known neolignans (4 – 12) and one known phenol (14) were isolated and characterized from the stems of Mallotus paxii Pamp. • The absolute configuration of 1–3 was established by ECD calculations. • Malloapelin A (4) markedly decreased the secretion of TNF- α , iNOS, and NF- κ B and inhibited the expression of COX–2 and NF- κ B/p65 in LPS-induced RAW264.7 cells in a dose-dependent manner. [ABSTRACT FROM AUTHOR]

Fungal infection caused by Candida albicans is a serious health problem, and as drug resistance worsens, new sources for therapeutic compounds are needed. Traditional Chinese medicine represents a wealth of such sources, and can be designed as suppositories for the treatment of recurrent vulvovaginal candidiasis (RVVC). This study aimed to develop a Pulsatilla suppository containing the n-butanol extract of Pulsatilla decoction (BEPD) to treat RVVC. A Pulsatilla suppository containing BEPD was prepared, and its performance, weight, drug content, dissolution time and percentage, stability, toxicology, and pharmacodynamics were evaluated. Biological compatibility tests and clinical evaluations were performed in female Sprague–Dawley rats. The Pulsatilla suppository melted completely within 30 min. In vitro anti- C. albicans activity, stability changes, and toxicology tests indicated stability and safety in the rats. Compared with RVVC model rats, high-dose BEPD suppository (40, 60 mg/kg) can significantly reduce the vaginal fungal load of rats, relieve neutrophil infiltration, reduce the content of TLR/MyD88 pathway-related proteins, and reduce the expression of inflammatory factors such as NLRP3, demonstrating the efficacy of the Pulsatilla suppository in RVVC. Pulsatilla suppository plays a role in the treatment of RVVC by inhibiting the activation of NLRP3 inflammasome through TLR/MyD88 signaling pathway. [Display omitted] [ABSTRACT FROM AUTHOR]

Two undescribed 3,5-dimethylorsellinic acid (DMOA) derived meroterpenoids, namely pancosterpenoids A (1) and B (2), were discovered from the EtOAc extract of the deep-sea sediment-derived fungus Penicillium pancosmium A6A. The gross structures were established by detailed analysis of the spectroscopic data (NMR and HRESIMS spectra), while their absolute configurations were resolved by comparing the experimental and calculated ECD data as well as X-ray single crystal diffraction analysis. Pancosterpenoid A (1) was the first representative of DMOA-derived meroterpenoids possessing a 6/6/6/5/5 pentacyclic system, while pancosterpenoid B (2) belongs to a class of rare 13-nor-citreohybridone meroterpenoids. Two metabolites were evaluated the antiviral effects against severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) trVLP pseudovirus. As a result, compounds 1 and 2 showed moderately inhibitory activities with IC 50 values of 22.37 and 18.12 μM, respectively. [Display omitted] [ABSTRACT FROM AUTHOR]

The husks of Xanthoceras sorbifolia Bunge have gradually attracted widespread attention in recent years due to the abundant resources and ideal pharmacological activities, with barrigenol-like triterpenoid saponins being its biological constituents. In this study, a feature-based molecular networking (FBMN) was utilized to perform the targeted isolation of triterpenoids. As a result, six undescribed barrigenol-type saponins (1–6) along with fourteen known analogues (7–22) were isolated from the extract of X. sorbifolia husk. Their structures were determined through a comprehensive analysis of NMR and HRMS spectroscopic data. Among them, compounds 1–3 are a specific type of saponin featuring a fucose moiety attached at C-21. The antitumor activities of isolated compounds were evaluated and compounds 7 , 9 and 10 showed significant inhibitory activities against A549 and HepG2 cell lines in a dose-dependent manner. [Display omitted] [ABSTRACT FROM AUTHOR]

Inflammation is the body's protective immune response to tissue damage. Ginseng has a long history of medicinal use, and its active ingredient ginsenosides have anti-inflammatory effects. Ginseng fruit rare saponins (GFRS) is a transformation product of ginseng saponins and rich in a variety of rare saponins. We used HPLC-DAD method to study GFRS rare saponins with ginsenoside F4, R -Rg 3 , S Rg 3 , Rk 1 , Rg 6 , Rg 5 , Rk 3 and Rh 4. However, there is no study on the use of GFRS to reduce skin inflammation. This study enriched the action pathway of GFRS through network pharmacology and revealed the anti-inflammatory effect of GFRS for the first time. In vitro experiments showed that GFRS could significantly reduce the release of NO in lipopolysaccharide (LPS) -induced RAW264.7 cells and HaCaT cells, and reduce the secretion and expression of inflammation-related factors Interleukin-6 (IL-6), Tumor necrosis factor-α (TNF-α) and Interleukin-17 A (IL-17 A), thereby reducing cell inflammatory damage. In the imiquimod (IMQ) -induced mouse inflammatory model, the therapeutic effect of GFRS on the pathogenesis of psoriasis-like dermatitis was studied. In vivo experiments showed that the skin erythema, scales, thickness and inflammatory infiltration of GFRS-treated mice were reduced, and the psoriasis area severity index score was significantly lower than that of IMQ group. GFRS restored IMQ-induced spleen size and reduced the secretion and expression of TNF-α, IL-6, Interferon-γ (IFN-γ) and IL-17 A in serum. In summary, our results demonstrate that GFRS alleviates IMQ-induced dermatitis symptoms, effectively reduces the secretion of inflammatory factors, and inhibits IL-17 A expression. [Display omitted] • GFRS significantly reduced LPS-induced NO release from RAW264.7 and HaCaT cells. • GFRS decreased the secretion and expression levels of LPS-induced inflammatory cytokines TNF-α and IL-6 in HaCaT cells. • GFRS attenuated the symptoms of IMQ-induced psoriatic dermatitis in mice and inhibited IL-17 A expression. [ABSTRACT FROM AUTHOR]

Artemisia plants are well-known for their abundant sesquiterpene compounds, which encompass various structural types and exhibit a range of biological activities. In this study, a systematic investigation of Artemisia atrovirens revealed the presence of germacrane-type sesquiterpenes for the first time. This included the discovery of 10 new compounds and three known analogues, among which were two rare dimeric germacrane-type compounds. Their structures were fully characterized through a comprehensive analysis involving MS, IR, 1D- and 2D-NMR spectroscopic data, single crystal X-ray diffraction, density functional theory (DFT) NMR calculations, and time-dependent DFT electronic circular dichroism (TDDFT ECD) calculations. Furthermore, all isolated compounds were evaluated for their anti-inflammatory activity in LPS-stimulated RAW 264.7 murine macrophages. Compound 10 demonstrated a potent inhibitory effect on NO production, with an IC 50 value of 4.01 ± 0.09 μM. This study highlights the diverse chemical repertoire of Artemisia species and underscores their potential in drug discovery and development. [Display omitted] • Germacrane-type sesquiterpenes were reported from the title plan for the first time. • Ten new germacrane-type sesquiterpenes including two rare dimers were described. • Compound 10 showed a potent anti-inflammatory effect with an IC 50 value around 4 μM. [ABSTRACT FROM AUTHOR]

Leading by the antiviral activities against HSV-2 virus, bioactivity-guided the fraction of crude alkaloids from seeds of Peganum harmala led to the isolation of nine structurally novel indole alkaloids, pegaharolines A − I (1 – 9), and 11 known ones (10 − 20). Compound 3 was an unusual 6/5/5/5 spirotetracyclic indole-derived alkaloids featuring a classic bicyclic indole unit fused with an additional pyrrolizine ring via a spiral atom (C-3). Compound 4 was determined as a novel indole alkaloid, characterized with a rare hexacyclic 6/5/6/5–6/6 ring system, by a single-crystal X-ray diffraction. Compounds 5 and 6 were peculiar indole dimers featuring with the rare carbon skeleton of an octacyclic scaffold. Compounds 1 – 6 were six racemates. Most compounds exhibited different levels of antiviral activities against HSV-2. Especially, the anti-HSV-2 activity of compound 1 (IC 50 = 0.90 ± 0.10 μM) was much better than that of the positive control (acyclovir, IC 50 = 1.12 ± 0.15 μM). In this study, the discovery of anti-HSV-2 components from the seeds of P. harmala , could benefit development and utilization of this plant in antiviral medicinal products. [Display omitted] [ABSTRACT FROM AUTHOR]

Eighteen compounds, among them phenylpropanoids (1 – 2), neolignans (3 – 9), a megastigmane (10), a phenyl glucoside (11), flavonoids (12 – 14), and N-containing compounds (15 – 18) were isolated from the methanolic extract of the whole plant of L. cartilagineum. The structures of the compounds were determined by NMR and MS measurements. The composition of the essential oils prepared from the flowers and fruits of L. cartilagineum was investigated using GC and GC–MS measurements. The essential oils were rich in aliphatic aldehydes and hydrocarbons, but low in sulfur-containing compounds, e.g., isothiocyanates. The extracts prepared from the aerial parts and roots of the plant, the essential oil, and the isolated compounds (1 – 9) were tested for antiproliferative activity against COLO 205 and COLO 320 cell lines and antibacterial activity on Lactobacillus rhamnosus. Dehydrodiconiferyl alcohol γ'-methyl ether (5) possessed marked antiproliferative activity against both human tumor cell lines. Neither the extracts nor the compounds affected the growth of the bacteria and did not influence the biofilm formation of L. rhamnosus. Based on the results, it can be concluded that L. cartilagineum is non-toxic to the human gut microbiome forming L. rhamnosus. [Display omitted] [ABSTRACT FROM AUTHOR]

Two new meroterpenoids, arneuchrols A and B (1 and 2), together with twelve known analogs (3 – 14) were isolated from the root of Arnebia euchroma. The structures of 1 and 2 including their absolute configurations were elucidated by NMR, HRESIMS, and DFT calculation of their NMR and ECD data. The structure of pseudoshikonin I, firstly isolated from Lithospermi radix was revised as shikonofuran E (4). Anti-triple negative breast cancer (anti-TNBC) and antimicrobial activities of the isolated compounds were tested. Compounds 3 , 4 , 6 , 7 , 9 , 10 , and 13 exhibited potent inhibitory activity against TNBC (MDA-MB-231 cells) with IC 50 values in the range of 0.18–4.58 μM. Compound 10 displayed antifungal activity against five plant pathogenic fungi with MIC values in the range of 6.25–25 μg/mL. Compound 9 exhibited antibacterial activity against Micrococcus lysodeikticus with MIC value of 12.5 μg/mL. [Display omitted] • Two new meroterpenoids were isolated from Arnebia euchroma. • The structure of pseudoshikonin I was revised. • The quantum calculation of NMR and ECD data was applied for structure elucidation. • The anti-triple negative breast cancer (anti-TNBC) and antimicrobial activities of the isolated compounds were evaluated. • Compounds 3 exhibited potent inhibitory effect against TNBC (MDA-MB-231 cells). [ABSTRACT FROM AUTHOR]

Polygala japonica Houtt. (P. japonica), a member of the Polygala genus in the Polygalaceae family, has been historically utilized in traditional folk medicine as an expectorant, anti-inflammatory, anti-bacterial, and anti-depressant agent. This paper systematically reviews the latest research in botany, traditional uses, phytochemistry, pharmacology, and pharmacokinetics, aiming to provide a scientific foundation for the future development and application of P. japonica and to explore its potential value comprehensively. Approximately 86 compounds have been isolated from P. japonica , with triterpenoid saponins being the most prevalent and bioactive components. Extensive pharmacological activities of P. japonica extracts or compounds have been confirmed in vivo and in vitro , including anti-inflammatory, anti-depressant, neuroprotective, anti-obesity, anti-apoptotic, and skin-protective effects. Additionally, P. japonica has demonstrated significant curative effects and relatively clear pharmacological mechanisms in treating inflammatory and nervous system diseases. Specific components of its primary triterpenoid saponins are rapidly absorbed in the body. This review advocates for deeper scientific research on P. japonica , noting that most current research remains in its early stages and many reported biological activities require further clinical validation. Despite this, the traditional medical use of P. japonica across various cultures attests to its broad application value. Presently, the pharmacological activities of P. japonica extracts and compounds provide a scientific basis for its traditional uses. Future research must ensure the safety and effectiveness of P. japonica through in-depth pharmacokinetic studies, and the establishment of a refined and standardized quality evaluation system is essential for its clinical development and application. [Display omitted] • This review is the latest and comprehensive. • About 86 compounds were reported from P. japonica. • In vitro and in vivo studies have demonstrated that P. japonica possesses a wide range of pharmacological effects. [ABSTRACT FROM AUTHOR]