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Chinese oak (Quercus serrata Thunb.) is widely distributed throughout China and plays an important role as a building material. Its seeds (acorns) have served as a traditional herbal medicine in East Asia. Eighteen oleanane-type triterpenoids, including seven previously undescribed (1, 2, and 4–8) and eleven known triterpenoids, were isolated and identified from acorns. Their structures were elucidated using various spectroscopic and chemical methods. All isolated triterpenoids were screened for anti-neuroinflammatory effects by measuring their abilities to inhibit nitric oxide (NO) production in lipopolysaccharide (LPS)-induced BV-2 microglial cells, and most of the triterpenoids exhibited obvious anti-neuroinflammatory activity. Among them, Compounds 1 and 5 exhibited the strongest NO inhibitory activity, reduced the expression of inflammatory cytokines (iNOS, COX-2, and TNF-α), and blocked the nuclear translocation of NF-κB.

Uncontrolled inflammation is associated with many major diseases, and there is still an urgent need to develop new anti-inflammatory drugs. 3α-Angeloyloxy-ent-kaur-16-en-19-oic acid (WT-25) is an ent-kaurane dieterpenoid extracted from Wedelia trilobata, a medicinal plant with potential anti-inflammatory activity. The anti-inflammatory activity of WT-25 is better than that of its analog kaurenoic acid, but the underlying mechanism is still unknown. In this study, our aim was to study the anti-inflammatory effect of WT-25. In xylene-induced edema in mice, WT-25 produced 51% inhibition. WT-25 suppressed nitric oxide (NO) and prostaglandin E2 (PGE2) production in LPS-stimulated RAW264.7 cells by downregulating the expression of nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). WT-25 reduced expression and secretion of TNF-α and IL-6. Moreover, WT-25 inhibited NF-κB activation and its upstream signaling, decreasing phosphorylation IKK and p65 levels. WT-25 also inhibited the phosphorylation of the mitogen-activated protein kinases (MAPKs) family. Additionally, it reduced LPS-induced excessive release of reactive oxygen species (ROS) and maintained mitochondrial integrity in RAW264.7 cells. All these results indicate that WT-25 is a bioactive molecule with the potential to be developed as a novel structured anti-inflammatory drug.

Onion is the most widely cultivated vegetable around the world. In this study, the isolation, concentration, quantification, and bioactivity evaluation of the phenolics in onion peels were investigated. Thirty-four phenolics, including 17 flavonoids and 17 nonflavonoid phenolics, were purified and identified. Among them, there were 2 new unusual epoxyflavanones and a new phenolic constituent, as well as 13 unreported constituents from the genus Allium. The total flavonoids were concentrated, and finally obtained 90.25% of flavonoid content extract. Fifteen main flavonoids were quantified using an ultra-performance liquid chromatography-photodiode array (UPLC-PDA), and quercetin (36.94%) and quercetin 4'-O-β-d-glucopyranoside (15.81%) were the richest contents of flavonoids. The antioxidant and anti-neuroinflammatory capacities were evaluated, and the bioactive results indicated that the flavonoids in onion exhibited pronounced activities. The study suggested that the flavonoids in onion peels could be used in functional food.

Giant crepe-myrtle (Lagerstroemia speciosa (L.) Pers) is widely cultivated as an ornamental plant in southern China and other Southeast Asian countries. Its leaves are also well-known as a popular traditional herb for diabetes and other diseases. In this study, bioactive phytochemical investigation on the extract of its fruits resulted in the isolation and purification of 27 compounds, including 16 sterols (1-16) and 11 triterpenoids (17-27). Their chemical structures were elucidated on the basic of various spectroscopic methods (IR, HR-ESI-MS, 1D and 2D NMR). Among them, there were two new ergostane derivatives and a new ursane triterpenoid, which were identified as 5α,6α-epoxy-3β-hydroxy-(22E,24R)-ergosta-9(11),22-diene-7-one (1), (22E,24R)-ergosta-7,9(11),22-triene-3β,5β,6α-triol (2), and 2-hydroxy-3-oxo-24- norursa-1,4,12-triene-28-oic acid (17). Compounds 1 and 2 exhibited significant anti-neuroinflammatory with the IC50 values of 8.29 ± 0.85 μM and 7.20 ± 1.55 μM, while compounds 1, 2, 7, 13, and 15 were displayed potent anti-proliferative activity against the tested cell lines (HeLa, HepG2, and SGC-7901). The study provided a phytochemical evidence for further development and utilization of the fruits of giant crepe-myrtle in health products.

Lychee is a favorite fruit of the Cantonese and native to Southeast Asia. In this study, the anti-neuroinflammatory bioactive compounds of lychee seeds have been carried out. Five new jasmonates (1, 2, 6-8) and seventeen known compounds were isolated using a series of chemical and chromatographic methods. Their chemical structures were identified through comprehensive spectroscopic analysis. Anti-neuroinflammatory activities were assayed and evaluated for the purified compounds. Most of the compounds exhibited pronounced anti-neuroinflammatory activities on nitric oxide (NO) induced by lipopolysaccharide (LPS) in BV-2 microglia cells. Moreover, compounds 1, 2 and 20 could reduce the expression of LPS-induced pro-inflammatory factors (iNOS and COX-2), inhibit the expression of mRNA levels of iNOS, COX-2, IL-6 and block NF-κB nuclear translocation in dose-dependent manners. This study suggested that lychee phytochemicals could be benefit to some neuroinflammatory-associated diseases, such as Alzheimer's disease.

(3α)-3-(tiglinoyloxy)-ent-kaur-16-en-19-oic acid (WT-26) is an ent-kaurane dieterpenoid extracted from Wedelia trilobata L., a widely cultivated ornamental plant with several scientific reports supporting its anti-inflammatory activity. WT-26 has better anti-inflammatory activity than its analog Kaurenoic acid (ent-kaur-16-en-19-oic acid). Nevertheless, the participation of WT-26 in the main signaling pathway associated with inflammation is lack of study. We aimed to study the anti-inflammatory effect of WT-26 and related signaling cascade in lipopolysaccharide (LPS)-stimulated macrophages. Here, we showed that WT-26 suppressed nitric oxide (NO) and prostaglandin E2 (PGE2) production in LPS-stimulated macrophages by downregulating the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in mRNA and protein level. WT-26 down-regulated tumor necrosis factor α (TNF-α), interleukin-6 (IL-6) and IL-1β production as well. Moreover, WT-26 inhibited the activation of nuclear factor-κB (NF-κB) p65 and its upstream signaling. WT-26 also reduced phosphorylation of mitogen-activated protein kinases (MAPKs) and mTOR. Besides, WT-26 decreased the overproduction of reactive oxygen species (ROS) and protected the mitochondrial integrity in stimulated macrophages. Our study also demonstrated that the autophagy induced by LPS was attenuated by WT-26. Collectively, our data indicated that WT-26 has the potential to be developed as a novel therapeutic agent for inflammatory-related diseases.

Lychee (Litchi chinensis Sonn.) is a famous tropical fruit. While enjoying its delicacy, it also produces a lot of lychee seeds as waste. In this study, bioactive phytochemical study of the seeds of lychee led to the isolation and identification of four methyl jasmonate analogs (1–4), one lignanoside (5), together with fifteen flavonoids (6–20). Their chemical structures were established on the basis of spectroscopic analysis including HR-ESI-MS, 1D and 2D NMR spectra. The anti-inflammatory and antioxidant activities were evaluated for the isolated compounds. Compounds 2 and 3 exhibited notable inhibition on NO production induced by lipopolysaccharides (LPS) in macrophages cell line RAW 264.7. Compound 5 and some flavonoids revealed potent antioxidant capacities. The results disclosed that the methyl jasmonates in lychee seeds may be partially responsible for anti-inflammatory activity of lychee and could be served as anti-inflammatory agent in functional food.

Biotransformation of laxogenin (LG, 1) was performed by the fungus Syncephalastrum racemosum (AS 3.264). Thirteen previously undescribed metabolites were obtained and their structures were elucidated by spectroscopic analysis. S. racemosum catalyzes mainly oxygenation reactions of the B, C, and D rings of the sapogenin to afford metabolites 2–12. Conversion of the spirostanol skeleton to cholestane-type was also encountered in metabolite 13. Rearrangement of F-ring afforded F-ring ‘furanose’ sapogenin was observed in metabolite 14. The substrate and its derivatives were evaluated for their anti-neuroinflammatory activities. LG and metabolites 2, 3, 5, 8–10 and 13–14 exhibited moderate to good inhibitory activities on lipopolysaccharide-induced NO (nitric oxide) production in BV-2 cells. Moreover, 1, 2 and 5 dose-dependently reduced the LPS-induced iNOS and COX-2 expressions.

Chinese acorns are served as a healthy food supplementary and cuisine in the local residents. The anti-neuroinflammatory phytochemicals of Chinese acorns have been investigated in this study. Four new triterpenoids (1, 8, 16 and 17), together with thirteen known congeners (2–7, 9–15), were isolated and their structures were elucidated by spectroscopic analysis and chemical degradation. The isolated compounds were evaluated for anti-neuroinflammatory activity. Some triterpenoids showed obvious inhibitory effects on the production of nitric oxide (NO) induced by lipopolysaccharide (LPS) in microglia cells (BV-2). Compounds 1, 2, and 16 could dose-dependently reduce the expression levels of pro-inflammatory mediator iNOS, while compounds 1, 2, 8 and 16 could dose-dependently reduce the COX-2 expression induced by LPS in BV-2 cells. This study suggested that Chinese acorns could be served as healthy product for neuroinflammatory related diseases, such as Alzheimer’s disease.

Mango leaves (Mangifera indica L.) are a kind of crop waste and the present work is focusing on its bioactive constituents. Phytochemical study on the extract of mango leaves resulted in the isolation and identification of 5 benzophenones and 17 flavonoids. Among them, there were 4 new benzophenone glycosides, elucidated as 4′,6-dihydroxy-4-methoxybenzophenone-2-O-(2″),3-C-(1″)-1″-desoxy-β-fructopyranoside, 4,4′,6-trihydroxybenzophenone-2-O-(2″),3-C-(1″)-1″-desoxy-β-fructopyranoside, 4,4′,6-trihydroxybenzophenone-2-O-(2″),3-C-(1″)-1″-desoxy-β-fructofuranoside, and 2,4′,6-trihydroxy-4-methoxybenzophenone-3-C-(2-O-p-hydroxybenzoyl-p-hydroxybenzoyl)-α- d -galactoside, together with eighteen known compounds. The anti-inflammatory, antioxidant and α-glucosidase inhibitory activities of the isolated compounds were evaluated. The results displayed that some phenolics showed significant anti-inflammatory, antioxidant and antidiabetic activities. The study provided a phytochemical evidence for further development and utilization of mango leaves in health products.

Six previously undescribed piperidine alkaloids were isolated from the rhizomes of Alocasia macrorrhiza (L.) Schott. Their structures were elucidated based on 1D and 2D NMR, IR, HR-ESI-MS spectroscopic analysis and the application of a modified Mosher method. All isolated alkaloids were evaluated for cytotoxicity against five human cancer cell lines (CNE-1, Detroit 562, Fadu, MGC-803, and MCF-7) using the MTT method. Only one compound exhibited cytotoxic effects against Detroit 562, Fadu, and MCF-7 cell lines with IC50 values less than 10 μM.

The roots of hairy fig (Ficus hirta Vahl.), known as Cantonese ginseng, is widely used as a plant-derived popular food to improve fatigue resistance by Hakka people in southern China. In the current study, four new phenolics (17, 18, 22 and 24) along with twenty-five known congeners were isolated and purified from the roots of hairy fig. Their structures were elucidated by extensive spectroscopic analysis and chemical degradation. The antioxidant and anti-inflammatory activities of the purified compounds were also evaluated. Results indicated that some phenolics showed moderate antioxidant activity compared to those of l -ascorbic acid in DPPH and superoxide anion radical scavenging capacity assay. Most of the isolated compounds exhibited pronounced inhibitory effects on the lipopolysaccharides (LPS)-induced nitric oxide (NO) production in murine macrophage RAW264.7. The results strongly demonstrated that the phenolics may be partially responsible for the roots of hairy fig’s anti-inflammatory activity.

Microbial transformation of isorhodeasapogenin (1), the major steroidal sapogenin of Tupistra chinensis, was performed with the fungus Syncephalastrum racemosum (AS 3.264). As a result, nine new biotransformation metabolites (2-10) were isolated and their structures were elucidated by spectroscopic analysis. Hydroxylation, oxidation and glycosylation reactions were observed on the B, C, D and F rings of steroidal skeleton. Substrate (1) and its biotransformed metabolites 2-6, 8-10 were evaluated for their anti-neuroinflammatory effect on the NO accumulation induced by LPS in BV-2 cells. All the tested metabolites were found to have more potential anti-neuroinflammatory activity than the substrate. Especially, metabolites 2, 5 and 6 exhibited significant inhibition on NO production after hydroxylation at C-12 or C-15. Moreover, metabolite 2 dose-dependently reduced the LPS-induced protein expression of iNOS and COX-2.

Durian, known as the king of fruits, is rich in nutrients and bioactive phytochemicals. Propacin is a bioactive coumarinolignoid isolated from durian. In this study, we demonstrated its anti-inflammatory effect on lipopolysaccharide (LPS)-induced RAW264.7 cells and explored the underlying mechanism. Propacin suppressed nitric oxide (NO) and prostaglandin E2 (PGE2) production in LPS-stimulated macrophages significantly by downregulating the mRNA and protein expression of nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Moreover, propacin decreased the overexpression of the LPS-induced reactive oxygen species (ROS) and maintained the mitochondrial integrity in active macrophages. Furthermore, propacin inhibited the translocation of the nuclear factor-κB (NF-κB) p65 subunit into the nucleus and the phosphorylation of mitogen-activated protein kinases (MAPKs), especially JNK and ERK. Collectively, these data indicated that propacin may have the potential to be developed as a novel therapeutic agent for inflammatory-related diseases.

Solanum nigrum L. (also called as European black nightshade) has been traditionally used as folk medicine and food in some regions. Phytochemical investigations of the immature fruits of S. nigrum yielded five steroidal alkaloid glycosides (1–5), including an unprecedented nor-spirosolane type steroidal alkaloid with a five-membered ring A (1) and two novel spirosolane type steroidal alkaloid glycosides (2, 3), together with eight known phenolic compounds (6–13). Their structures were elucidated on the basis of spectroscopic and chemical methods, including IR, NMR, HR-ESI-MS, and GC analyses. Five steroidal alkaloid glycosides were tested for their potential antiproliferative effects against HL-60, U-937, Jurkat, K562, and HepG2 cell lines and inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in a macrophage cell line RAW 264.7. Compound 1 exhibited significant inhibition on NO production with an IC50 value of 23.4 ± 2.0 μM, compared to positive control indomethacin (IC50, 47.40 ± 4.50 μM). Compound 4 exhibited significant cytotoxicity against all tested cell lines.

Ficus altissima, an evergreen arbor belonging to the Moraceae family, is mainly cultivated in the tropics and subtropics of South and Southeast Asia with the characteristic of exuberant vitality and luxuriant foliage. In this article, four new prenylated isoflavones (1-4), along with ten previously described isoflavones (5-14) and two known prenylated coumaronochromones (15 and 16) were firstly obtained from the fruits of F. altissima. Their structures were identified by various spectroscopic techniques including specific optical rotation, HR-ESI-MS and NMR. The isolated products were evaluated for their anti-proliferative activities against three human tumor cell lines (HepG2, MCF-7 and MDA-MB-231) through MTT assay. Compounds 2, 3 and 16 exhibited obvious anti-proliferative activities against MDA-MB-231 cell line and compounds 3, 13 and 16 showed effective cytotoxic effects on HepG2 cell line in a concentration-dependent manner, as verified by the colony formation assay, cell and nucleus morphological assessment and apoptosis assay. Meanwhile, compounds 5 and 12 exhibited significant inhibition activities on NO production in LPS-stimulated RAW 264.7 cell line compared with positive control indometacin. The phytochemical investigation of the fruits of F. altissima in this study could provide the evidence for the discovery of lead compounds.

Morinda (Morinda officinalis) is widely consumed as a health-care herb in Asia and reported to possess various biological activities. In this study, anti-inflammatory phytochemicals were investigated and two pairs of new methyl-2-naphthoate enantiomers (1a/1b, 2a/2b), one new anthraquinone (3), three new natural unknown anthraquinones (5–6, 23), and eighteen known anthraquinones were isolated and elucidated from the roots of morinda. Anti-inflammatory activities of the isolated compounds were assessed in lipopolysaccharide-stimulated RAW 264.7 macrophages. Compounds 2b and 19 significantly inhibited the production of NO with IC50 values of 34.32 ± 4.87 and 17.17 ± 4.13 μM (indomethacin, IC50 26.71 ± 6.32 μM), and they were further corroborated via immunoblotting, quantitative real-time PCR and immunofluorescence staining assays. They could dose-dependent suppress lipopolysaccharide-stimulated pro-inflammatory factors (COX-2 and iNOS) production and block nuclear translocation of NF-κB. The results implied that reasonable consumption of morinda may be beneficial for preventing and reducing the occurrence of inflammatory-associated diseases.

Phytochemical investigations of the rhizome of Tupistra chinensis led to the isolation of ten new furostanol saponins along with fourteen known spirostanols. Their chemical structures were elucidated on the basis of spectroscopic and chemical methods, including IR, NMR, MS, and GC analyses. The antiproliferative effects against FaDu and Detroit 562 cell lines and inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in a macrophage cell line RAW 264.7 were assayed for all the isolated compounds. Compound 14 exhibited significant antiproliferative effects against FaDu and Detroit 562 cells with IC50 values of 1.1±0.1 and 1.2±0.1μM, respectively. Compounds 1, 2, 6, 13, 16, 19 and 24 exhibited inhibitory effects on NO production with IC50 values ranging from 15.7 to 46.2μM.

Acorns serve as an important role as an important cash crop in human history and are a source of food for many countries. In this study, ten pentacyclic triterpenes, three of which were novel, were isolated from acorns (Quercus serrata var. brevipetiolata). The structures of novel triterpenoids were established based on the interpretation of chemical and spectroscopic analyses, including IR, HR-ESI⿿MS, and NMR experiments (1D and 2D NMR), which were elucidated to be 3,23-O-methyl butyrate-2α,3β,19α,23-tetrahydroxy-urs-12-en-28-oic acid β- d -glucopyranosyl ester (1), 3,23-O-methyl butyrate-2α,3β,19α,23-tetrahydroxy-olean-12-en-28-oic acid β- d -glucopyranosyl ester (2), and 23-acetoxy-2α,3β,19α-trihydroxyurs-12-en-28-oic acid (3), respectively. All isolated compounds were tested for their inhibitory effects on LPS-induced nitric oxide (NO) production in RAW 264.7 macrophages. Most of the triterpenes from acorns showed pronounced anti-inflammatory activities compared to positive control indomethacin. Furthermore, based on the results of the nitric oxide assay, production of pro-inflammatory markers including interleukin-6 (IL-6) and interleukin-8 (IL-8) of compound 1⿿3 in TNF-α stimulated RAW 264.7 were investigated by ELISA, which showed these pentacyclic triterpenes may be responsible with the two pro-inflammatory cytokines for the anti-inflammatory activity of acorn.

Chinese onion ( Allium chinense ) is widely cultivated as a vegetable, native to China and cultivated in many other countries. Its bulbs are commonly processed into pickles and spices. In this study, seven new spirostanol saponins ( 5 , 7 , 9 – 11 , 13 and 15 ) together with ten known congeners ( 1 – 4 , 6 , 8 , 12 , 14 , 16 and 17 ) were isolated from the bulbs of Chinese onion and their structures were elucidated by spectroscopic analysis and chemical degradation. The isolated components were evaluated for anti-inflammatory and anti-proliferative activities. As a result, compounds 4 and 8 showed potent inhibitory effects on the lipopolysaccharides (LPS) induced nitric oxide (NO) production in murine macrophage RAW264.7. Compound 13 displayed potential inhibitory activity against five human cancer cell lines with IC 50 values of 1.43–6.81 µ M. Compound 14 exhibited significant selective inhibition against these cancer cells (IC 50 2.22–15.58 µ M), in comparison with the normal cells MRC-5 (IC 50 > 100 µ M).

Chinese hickory (Carya cathayensis Sarg.) is a common and nutritious nut. Twenty-nine phenolic compounds, together with three quinones and three triterpenoids, were isolated from Chinese hickory husks. Their structures were determined by comprehensive spectroscopic methods. The total methanolic extract, chloroform and ethyl acetate fractions and all the isolated compounds were evaluated for antioxidant activity and neuroprotective effects on SH-SY5Y cells, as well as the effects on the expression of PPAR-γ in 3T3-L1 cells. Quercetin (10) and protocatechuic acid methyl ester (24) showed pronounced antioxidant activities in all of the different antioxidant assays and neuroprotective effect against H2O2-induced oxidative stress. Some of the flavonoids could significantly decrease the mRNA expression level of PPAR-γ by approximately 70%. The present study provided supplement information for the evaluation of antioxidant activity and health benefit of Chinese hickory.

Mulberry (Morus alba L.) fruit is a delicious, fleshy, succulent berry, which is served as a famous fruit in many countries and as traditional herb in China. In our current study, three new (1, 44, 47) and forty-seven known compounds were isolated and identified from mulberry fruit. Anti-neuroinflammatory, antioxidant and antidiabetic activities of these compounds were evaluated in vitro. Compound 7 significantly inhibited nitric oxide (NO) production induced by lipopolysaccharides (LPS) in microglia cells (BV-2) with the IC50 value of 10.09 ± 0.51 μM. Compounds 1, 5, 7, and 14 dose-dependently reduced the expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). Simultaneously, they could block LPS-induced nuclear translocation of nuclear factor-κB (NF-κB). Moreover, phenols from mulberry fruit displayed evidently antioxidant and antidiabetic activities. These results suggested that reasonable consumption of mulberry might assist people to prevent and reduce the occurrence of neuroinflammatory and oxidative related diseases.

The seeds of Quercus serrata Thunb. (acorns) have been served as a healthy food in Asia. In this study, five previously undescribed triterpenoids, along with nineteen known triterpenoids were isolated from acorns. Their structures were identified on account of spectroscopic analysis and GC-MS analysis after acid hydrolysis. Meanwhile, the inhibitory effects on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in microglia cells (BV-2) of the identified triterpenoids were evaluated. All these compounds revealed overt anti-neuroinflammatory activity expect for 7. Compounds 1, 16 and 17 had potent inhibitory effects on protein and mRNA expression of iNOS and COX-2 in LPS-induced BV-2 cells. Bioactive triterpenoids 1, 2, 16 and 17 could block LPS-induced NF-κB nuclear translocation. This study suggested that acorns could be served as natural healthy product against neuroinflammatory-associated diseases, such as Alzheimer's disease.

Chinese olive is served as a famous fruit and traditional herb in China. In this study, the anti-neuroinflammatory and antioxidant phytochemicals of Chinese olive fruits were investigated. Three new phenylpropanoids (2, 6, 19), together with sixteen known congeners, have been isolated and identified. A variety of bioactivities related to the traditional healthy benefits of Chinese olive, including anti-neuroinflammatory, antioxidant and antidiabetic, have been evaluated for the identified compounds. The phenylpropanoids could significantly inhibit the production of nitric oxide induced by lipopolysaccharide (LPS) in microglia cells (BV-2). Compounds 2, 6, and 19 could dose-dependently reduce the expression levels of pro-inflammatory mediator iNOS and COX-2 expressions induced by LPS in BV-2 cells. Meanwhile, some phenylpropanoids showed remarkable antioxidant and antidiabetic activities. This study suggested that Chinese olive could be served as a healthy product for neuroinflammatory related diseases, such as Alzheimer's disease.

Five new furospirostanol saponins (1–5), four new spirostanol saponins (6–9), along with one known spirostanol saponin were isolated from the rhizome of Tupistra chinensis. The chemical structures were determined by spectroscopic and chemical methods, including IR, NMR, MS, and GC analyses. The antiproliferative effects against five human cancer cell lines were assayed for all the isolated compounds. Compounds 6–10 showed potent cytotoxic activities against the five cancer cell lines. The isolated compounds were evaluated the inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide in a macrophage cell line RAW 264.7. Compounds 6–10 showed significant inhibition on NO production with IC50 values between 3.1 and 4.4 μM.

Background Our previous study has revealed that the spirostanol saponins isolated from the rhizomes of Rohdea chinensis (Baker) N. Tanaka (synonym Tupistra chinensis Baker) (Convallariaceae) (a reputed folk medicine) exhibited potent antiproliferative activity. However, the underlying mechanism of purified saponins remains unclear. More studies are necessary to assess the apoptosis and autophagy activities of the saponins from R. chinensis and clarify their antiproliferative mechanisms. Purpose The present study certificated the potential antiproliferative activity and mechanism of 5β-spirost-25(27)-en-1β,3β-diol-1-O-α-L-rhamnopyranosyl-(1→2)- β-D-xylopyranosyl-3-O-α-L-rhamnopyranoside (SPD), a spirostanol saponin from R. chinensis, against human acute promyelocytic leukemia cells (HL-60). Methods The antiproliferative activity of SPD in vitro was evaluated by MTT assay compared with cis-dichlorodiammineplatinum (II). The autophagic activity was assessed using MDC staining and western blot, cell apoptosis inspection was detected by Annexin V-FITC/PI double staining and the mitochondrial membrane potential was detected by JC-1 fluorescence dye combined with flow cytometry. The potential mechanisms for protein levels of apoptosis and autophagy were evaluated by western blot. Results Treatment of HL-60 cells with SPD resulted in growth inhibition (IC50 value of 2.0 ± 0.2 µM, after 48 h treatment) and induction of apoptosis and autophagy. Results from Annexin V-FITC/PI double-staining assay and mitochondrial membrane potential detection showed that apoptosis was happened after SPD treatment. The regulation of caspase-3, Bax, Bcl-2, PARP following SPD treatment contributed to the induction of mitochondria-dependent apoptosis. Meanwhile, SPD induced autophagy related with Akt/mTOR/p70S6K signaling and activated of AMPK signaling pathway. Furthermore, blocking autophagy with bafilomycin A1 reduced the cytotoxicity of SPD in HL-60 cells. Conclusion The antiproliferative, apoptosis and pro-death autophagy activities of SPD suggested that spirostanol saponins from R. chinensis would be a potential cytotoxic candidate against acute promyelocytic leukemia.

Four new phenylpropanoids (1-4) along with ten known phenolics were isolated and purified from the roots of hairy fig (Ficus hirta Vahl.). Their structures were elucidated by the extensive spectroscopic analysis and chemical degradation. The anti-inflammatory activities of the purified compounds were evaluated. Results indicated that the extracts and some purified compounds exhibited pronounced inhibitory effects on the lipopolysaccharides (LPS) induced nitric oxide (NO) production in murine macrophage RAW 264.7 compared to indomethacin, which suggested that hairy fig could be served as an anti-inflammatory agent for health products.

Significance DNA methylation is generally considered an epigenetic mark for transcriptional gene silencing. In this work, we generated loss-of-function mutant alleles of SlDML2 . We characterized the mutant fruits that failed to ripen and discovered that SlDML2 is required for the demethylation and activation of genes important for fruit ripening, including genes involved in fruit pigment and flavor synthesis, ethylene synthesis and signaling, and cell wall hydrolysis. Unexpectedly, we found that SlDML2-mediated DNA demethylation is also necessary for fruit ripening-induced repression of hundreds of genes involved in photosynthesis and cell wall synthesis and organization. Our study has therefore revealed a broad and critical role of DNA methylation as an activation mark for the expression of many genes in a eukaryotic organism.

Solanum nigrum L. or European black nightshade (Solanum genus) is a common weed of crops and gardens. The berries and leaves of S. nigrum L. are consumed as food or vegetable in some regions and reported to possess a range of biological activities. In this study, nine new steroidal saponins, solanigrosides Y1–Y9 (1–6, 10–12), together with seven known congeners, were isolated from the berries of S. nigrum. Their potential inhibitory effects on nitric oxide (NO) and IL-6 and IL-1β production induced by lipopolysaccharide (LPS) in macrophages cell line RAW 264.7 were evaluated. Compound 1 exhibited significant inhibition on NO production with an IC50 value of 9.7 μM, and some compounds exhibited significant inhibition effects on the LPS-induced IL-6 and IL-1β production. These results suggest that the steroidal saponins from berries of S. nigrum demonstrated pronounced anti-inflammatory activity and might be explored as a healthy benefit agent.

Structured platinum nanoclusters Ptn (n = 5–30) capped by poly(N-vinylpyrrolidone) (PVP) have unique and highly attractive properties as potential selective catalysts. We show that the assembly of Pt mononuclear compounds in aqueous and tetrahydrofuran (THF) solutions under UV irradiation proceed via several steps: formation of linear Ptn clusters (n = 2–8), coalescence into mesocrystals, and transformation into Pt nanocrystals. The “quantum” size range of Ptn (n = 5–100) clusters is intermediate between those clusters with molecular properties and those with metallic properties. The PVP “cage” acts as a nano reactor and can hinder diffusion of photoexcited Pt atoms. The diffusion of the Pt from the polymer cage is strongly affected by the hydrophobic or hydrophilic property of the solution. An aqueous solution of [PtCl6]2– + PVP transforms into noncrystalline aggregates of molecules of less than 1.5–2 nm in diameter, whereas in THF solution Pt nanocrystals increase proportional to the UV irradiation time...

We characterize the surface chemical states of reactants and catalysts under reaction conditions to elucidate the composition effect of platinum–iron bimetallic nanoparticles on catalytic hydrogenation of organic molecules. The catalytic hydrogenation of ethylene is drastically accelerated on the surface of 2 nm PtFe bimetallic nanoparticles as compared to pure Pt. Sum frequency generation (SFG) vibrational spectroscopy indicates that incorporation of Fe into Pt nanoparticle catalysts weakens the adsorption of ethylidyne, an inactive spectator species, on the catalyst surface. Similarly, the turnover frequency of cyclohexene hydrogenation is also significantly enhanced by incorporating Fe into Pt nanoparticle catalysts. Ambient-pressure X-ray photoelectron spectroscopy (AP-XPS) reveals the surface composition and oxidation states of the PtFe nanoparticles under reaction conditions. The oxidation state distribution of Fe responded to the gas atmosphere and the probing depth, whereas the Pt remained largely...

Five new lignanamides (1-5), and one new monoindole alkaloid (6), along with eight known compounds (7-14) were isolated and identified from the rhizomes of Alocasia macrorrhiza (giant taro). All purified compounds were evaluated for their inhibitory effects on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, and the antiproliferative activities against human nasopharyngeal carcinoma epithelial (CNE-1), human gastric carcinoma (MGC-803), and human breast cancer (MCF-7) cell lines by MTT method. Compounds 2, 4, 7 and 8 exhibited significant inhibitory effects on NO production with the IC50 values of 2.35±0.38, 9.20±0.94, 3.45±0.39 and 7.96±0.56μM, respectively. The results suggested the lignanamides and monoindoles might be responsible for the anti-inflammatory activity of giant taro and might be potential anti-inflammatory candidates.

Mango (Mangifera indica L.) is a succulent tropical fruit. Bioactive phytochemical investigation has been carried out to the leaves of mango. Three new benzophenone glycosides, along with 14 known compounds, were purified and identified. The novel benzophenones were elucidated to be 2,4,4′,6-tetrahydroxy-3′-methoxybenzophenone-3-C-β-d-glucopyranoside (1), 4,4′,6-trihydroxybenzophenone-2-O-α-l-arabinofuranoside (7), and 4′,6-dihydroxy-4-methoxybenzophenone-2-O-(2″),3-C-(1″)-1″-desoxy-α-l-fructofuranoside (11). The α-glucosidase inhibitory, NO production inhibitory, and antioxidant activities were assessed for the purified benzophenones and triterpenoids. Some benzophenones showed moderate α-glucosidase and NO inhibitory activities. The IC50 value of the α-glucosidase inhibitory of isolated compounds 1, 13, and 14 were 284.93 ± 20.29, 239.60 ± 25.00, and 297.37 ± 8.12 μM, respectively. Most compounds showed moderate effects to reduce the NO content in 50 and 100 μM. The above results of bioactivity powerful...

Background Harmine, a β-carboline alkaloid from Peganum harmala, has multiple anti-tumor activities, especially for its folk therapy for digestive system neoplasm. However, the underlying mechanism of harmine on gastric cancer remains unclear. Purpose To illuminate the potential anti-tumor activity and mechanism of harmine against gastric cancer cells. Methods/Study designs The anti-proliferative activity of harmine in vitro was evaluated by MTT assay. The autophagic activity induced by harmine was assessed using GFP-LC3 transfection. FITC/PI double staining was applied for the apoptosis inspection. The mitochondrial membrane potential was detected by JC-1 fluorescence probe. The potential mechanisms for proteins level in autophagy and apoptosis were analyzed by Western blot. Results Harmine exhibited potent effects on both autophagy and apoptosis. Treatment with harmine could enhance dots of GFP-LC3 in cells. Meanwhile, the process had connection with Beclin-1, LC3-II, and p62 by the inhibition of Akt/mTOR/p70S6K signaling. However, high concentration of harmine led to apoptosis characterized by the propidium/Annexin V-positive cell pollution, cell shrunk and the collapse of mitochondrial membrane potential. The regulation of Bcl-2, Bax and the gathering of cleaved-PARP, cleaved-caspase 3 and cleaved-caspase 9 contributed to the induction of apoptosis. In addition, 10 μM LY294002 (a specific inhibitor of PI3K/Akt) combination with 40 μM harmine significantly increased the cytotoxicity to the gastric cancer cells and up-regulated both the apoptosis-related protein (cleaved-PARP, cleaved-caspase-3) and autophagy-related protein (Beclin-1, LC3-II, and p62). Adding the inhibitor of autophagy, 3-MA or BafA1, increased the viability of harmine-exposured gastric cancer cells, which confirmed the role of autophagy played in the gastric cancer cell death induced by harmine. Conclusion Harmine might be a potent inducer of apoptosis and autophagy, which offered evidences to therapy of harmine in gastric carcinoma in the folk medicine.

Tupistra chinensis is widely distributed in southwestern China and its rhizome is a famous folk medicine for the treatment of carbuncles and pharyngitis. Its chemical identity of potent antiproliferative and anti-inflammatory constituents has been carried out in this study. Twenty-three polyhydroxylated spirostanol saponins, including nine novels, were isolated and identified. The new spirostanol saponins were elucidated as spirost-25(27)-en-1β,2β,3β,4β,5β-pentol-2-O-β-D-xylopyranoside (1), spirost-25(27)- en-1β,2β,3β,4β,5β-pentol-2-O-α-L-arabinopyranoside (2), spirost-25(27)-en- 1β,3α,5β-triol (12), spirost-25(27)-en-1β,3α,4β,5β,6β-pentol (13), spirost-25(27)-en- 1β,2β,3β,5β-tetraol-5-O-β-D-glucopyranoside (16), 5β-spirost-25(27)-en-1β,3β-diol- 3-O-β-D-glucopyranosyl-(1 → 4)-β-D-glucopyranoside (17), (25R)-5β-spirostan- 1β,3β-diol-3-O-β-D-glucopyranosyl-(1 → 6)-β-D-glucopyranoside (18), (25R)-5β- spirostan-1β,3β-diol-3-O-β-D-fructofuranosyl-(2 → 6)-β-D-glucopyranoside (19), 5β-spirost-25(27)-en-3β-ol-3-O-β-D-glucopyranosyl-(1 → 4)-β-D-glucopyranoside (20). The antiproliferative effects against seven human cancer cell lines and inhibitory activities on nitric oxide (NO) production induced by lipopolysaccharide (LPS) in a macrophage cell line RAW 264.7 were assayed for all the isolated compounds. Compounds 17, 19 and 21 exhibited potential antiproliferative activities against all of human cancer cell lines tested. Compounds 21 showed significant inhibition on NO production with IC50 values of 11.5 μM. These results showed that the spirostanol saponins isolated from the dried rhizomes of T. chinensis have potent antiproliferative and anti-inflammatory activities and T. chinensis might be used as anticancer and.anti-inflammatory supplement.

Durian, known as the king of fruits, is native to Southeast Asia and popular in many countries. Bioactivity-guided fractionation of the peel of durian was applied to determine its bioactive constituents. Four novel phenolics, along with 16 known, were purified and identified. Four novel phenolics were elucidated to be durianol A (1), durianol B (2), durianol C (3), and 5′-methoxy-7′-epi-jatrorin A (4), respectively. The antioxidant and NO inhibitory activities were evaluated for the isolated phenolics. Some phenolics showed significant antioxidant activity in the DPPH and superoxide anion radical scavenging capacity assay. Most of the phenolics revealed pronounced inhibitory effects on NO production in murine RAW 264.7 cells induced by LPS, which showed more potent NO inhibitory activity compared to indomethacin. The results strongly demonstrated that the phenolics may be partially responsible for durian’s NO inhibitory activity.

Ursolic acid (UA, 1), a major bioactive constituent of apple peels, exhibits a wide spectrum of biological activities, including antioxidant, antitumor, anti-inflammatory, and hypoglycemic properties. The bioconversion of 1 by Alternaria alternata was investigated, and 8 metabolites were isolated and identified. The chemical structures of these metabolites were found to be 2α,3β-dihydroxyurs-12-en-28-oic acid (corosolic acid, 2), urs-12-en-2α,3β,28-triol (3), 3β,23-dihydroxyurs-12-en-28-oic acid (4), 2α,3β,23-trihydroxyurs-12-en-28-oic acid (5), 2α,3β,23,24-tetrahydroxyurs-12-en-28-oic acid (6), 3β,28-dihydroxy-12-ursene (7), urs-12-en-3β-ol (8), and urs-12-en-2α,3β-diol (9), as determined through chemical and spectroscopic analyses. Among these metabolites, 2 was found to be the main bioconversion product, with a yield of 77.6%. The proposed biosynthetic pathways of UA by A. alternata were drawn and are presented in this paper. Metabolites 2, 5 and 6 showed potent antiproliferative activities against human breast cancer (MCF-7, MDA-MB-231), human colon cancer (Caco-2) and human liver cancer (HepG2) cell lines.

Genetic studies have shown the effects of various photoreceptors on early photomorphogenic processes, defining the precise time course of red (RL), far-red (FrL) and blue light (BL) action. In this study, the effect of green wavebands in conjunction with these responses is examined. Longer-term (end point; 24–96 h) analysis of hypocotyl elongation in enriched green environments shows an increase in growth compared to seedlings under blue, red or both together. The effect was only observed at lower fluence rates (

Andrographolide ( 1 ), a major labdane diterpenoidal constituent of a famous traditional Chinese of Andrographis paniculata , exhibits a wide spectrum of biological activities including antibacterial, anti-inflammatory, and antitumor properties. Bioconversion of andrographolide ( 1 ) by Aspergillus ochraceus (ATCC 1008) was investigated. Five bioconversion products were isolated and identified. Their structures were identified to be 8β-hydroxy-8(17)-dihydroandrographolide ( 2 ), 8β-hydroxy-8(17)-dihydro-14-deoxy-11,12-didehydroandrographolide ( 3 ), 8β-hydroxy-8(17)-dihydro-14-deoxy-11,12-didehydroandrographolide 19-oic acid ( 4 ), 14-deoxy-11,12-didehydroandrographolide ( 5 ), and 14-deoxy-11,12-didehydroandrographolide 19-oic acid ( 6 ). Metabolites 2 – 4 were novel compounds. The proposed biosynthetic pathways of andrographolide by A. ochraceus were drawn. Most bioconversion products showed potential cytotoxic activities against human breast cancer (MCF-7), human colon cancer (HCT-116) and leukemia (HL-60) cell lines.

A phytochemical study on the methanol extracts from the seeds of Peganum harmala L. led to a new quizonaline alkaloid (S)-vasicinone-1-O-β-d-glucopyranoside (1) and four known ones, (R)-vasicinone-1-O-β-d-glucopyranoside (2), (S)-vasicinone (3), vasicine (4), and deoxyvasicinone (5). Their structures were elucidated by spectroscopic analysis including IR, HR-ESI-MS, 1D and 2D NMR, and specific rotation as well as by comparison of the data with those in the literature. All of the alkaloids were screened for antiproliferative activity against human gastric cancer cells MCG-803 with MTT method. Compounds 1 and 3 exhibited moderate inhibitory activity.

Moderate consumption of red wine reduces the risk of heart disease and extends lifespan, which these healthy benefits are often attributed to its high antioxidant content. The relative contributions of wine polyphenols in healthy benefits were studied in this study. Among all wine polyphenols, caffeic acid was the richest one, while gallic acid showed the highest free radical scavenging activity. There was no significant difference between the prime red wine and the red wine adding 10-fold resveratrol on neuroprotective effects on SH-SY5Y cell line. The contribution percentage of resveratrol to the antioxidant activity of red wine was less than other tested polyphenols. It suggested that resveratrol may be negligible with respect to healthy benefits of red wine.

Acorns play an important role in human history and are a source of food and recipes for many cultures around the world. In this study, eleven oleanolic triterpenes, one of which was novel, were isolated from Chinese acorns (Quercus serrata var. brevipetiolata). The chemical structure of the novel triterpene, which was identified as 2α,3β,19α-trihydroxy-24-oxo-olean-12-en-28-oic acid (1), was established based on the interpretation of chemical and spectroscopic analyses, including IR, HR-ESI-MS, and NMR experiments (¹H, (13)C NMR, DEPT, ¹H-¹H COSY, HSQC, HMBC, and NOESY). All isolated compounds were tested for their inhibitory effects on LPS-induced nitric oxide (NO) production in RAW 264.7 macrophages. Compared with the positive control drug indomethacin (IC50 = 47.4 μM), compounds 1, 3, 6 and 8 exhibited remarkable anti-inflammatory activities with IC50 values of 5.4, 7.8, 4.0 and 8.9 μM, respectively. Besides, compounds 2, 4, 7 and 9 also showed moderate anti-inflammatory activities with IC50 values of 10.1, 13.0, 20.1 and 17.2 μM, respectively. Furthermore, Compound 1 could inhibit TNF-α-induced IL-6 and IL-8 production in MH7A cells.

A 70% ethanol extract of the roots of Livistona chinensis has been investigated, led to the isolation of 13 compounds, including a new ceramide, (2S,3S,4R,9Z)-2-[(2R)-2-hydroxytricosanoylamino]-9-octadecene-1,3,4-triol (2), a new glycosyl ceramide, 1-O-β- d -glucopyranosyl-(2S,3S,4R,9Z)-2-[(2R)-2-hydroxydocosanoylamino]-9-octadecene-1,3,4-triol (3), three new monoacylglycerols, 1-(34-hydroxytetratriacontanoyl)-sn-glycerol (9), 1-[nonadeca-(9Z,12Z)-dienoyl]-sn-glycerol (10), and 1-[12-hydroxypentatriaconta-(13E,15Z)-dienoyl]-sn-glycerol (11), a new diacylglycerol, 1-(heptadeca-6Z,9Z-dienoyl)-3-(octadeca-6Z,9Z,12Z-trienoyl)-sn-glycerol (12), as well as a new diacylglycerol aminoglycoside, 1-octadecanoyl-2-nonadecanoyl-3-O-(6-amino-6-deoxy)-β- d -glucopyranosyl-sn-glycerol (13). The structures of new compounds were elucidated, based on spectroscopic, zymologic and chemical methods. Among the compounds tested, compounds 3, 4 and 13 showed significantly antiproliferative effects against the human tumor cell lines (K562, HL-60, HepG2, and CNE-1) with the IC50 of 10–65 μM. To our knowledge, this is first report of the occurrence of ceramides and acylglycerols in the genus Livistona.

Various silver nanostructures with hollow interiors, including nanoscaled cubic or quasi-cubic boxes, tubes, triangular rings, trapeziform rings and hybrid structures composed of tubes and cubic boxes, were synthesized via an extremely simple route. The method involved the modification of the solid silver nanocrystals by dithiol, and subsequent dissolving of the interior metal and assembly of the outer surface. In the whole process, only one simple step of pretreatment was needed before the transformation from Ag solid nanostructures to their corresponding hollow nanostructures. According to the morphological, spectral and structural changes in the evolution from silver solid nanostructures to their corresponding hollow nanostructures, a layer-by-layer assembly mechanism was proposed. The method is believed to open up a simple and versatile route to the fabrication of metallic hollow nanostructures with various morphologies according to the starting templates.

This study investigated the antioxidant and cytotoxic activity of the phenolics isolated from the fruits of Livistona chinensis. Four new compounds, 1-{ω-isoferul[6- (4-hydroxybutyl)pentadecanoic acid]}-glycerol (1), E-[6′-(5″-hydroxypentyl)tricosyl]-4-hydroxy-3-methoxycinnamate (2), 2-(3′-hydroxy-5′-methoxyphenyl)-3-hydroxylmethyl-7-methoxy-2,3-dihydrobenzofuran-5- carboxylic acid (3), 7-hydroxy-5,4′-dimethoxy-2-arylbenzofuran (4), together with eleven known phenolics (5–15), were isolated and identified. Among these compounds, 1–4, 5-O-caffeoylshikimic acid (5), caffeic acid (7), and 3-O-caffeoylshikimic acid (8) showed potent antioxidant activity. 1–5, and 8 showed potent antiproliferative activities with IC50 values among 5–150 μM against HepG2 human liver cancer, HL-60 human myeloid leukemia, K562 human myeloid leukemia, and CNE-1 human nasopharyngeal carcinoma cell lines. On the basis of these findings, it could be proposed that the fruits of L. chinensis may serve as attractive mines of powerful anticancer and antioxidant agents for various purposes.

Phase change characteristics of hydrate salt were analyzed for a system consisting of three types of SiO2 nano-particles doped phase change materials (PCMs). By using the three nano-particles of Aerosol SiO2, RNS-A SiO2 and Liquid phase SiO2, the surface effect of the interaction between nano-particles and hydrate salts was investigated. The time-temperature curves and Differential Scanning Calorimeter (DSC) testing results showed that Aerosol SiO2 had the most effective and stable performance as the nucleators for hydrate salts. The analysis of FT-IR showed that there were strong characteristic hydroxyl bonds on the surface of Aerosol SiO2. And the designed hydroxyl controllable silica gel system could prove the effect of hydroxyl bonds on suppressing supercooling of hydrate salts. It was concluded that supercooling of hydrate salts could be easily suppressed by the nano-additives with high specific surface area and strong polar hydroxyls in the surface. The ion-exchange attraction between hydroxyls and hydrate salts might mainly result in the supersaturation of hydrate salts in the interface of nano-particles. And then the supercooling of hydrate salts could be suppressed. The theoretical analysing model based on interionic attraction is a novel approach for investigating the nucleation of hydrate salts. And this result might provide a potential low-cost approach for the applications of nano-additivs in building energy storage and coolant.