RSC Advances
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2017
·Vol. 7
·期 28
·17289-17296
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IF 3.108
Yu Chen,Fei Gan,Shan Jin,Hui Liu,Shijun Wu,Wenting Yang,Guangzhong Yang
Garcinia xanthochymus is a tropical fruit yielding tree native to South East Asia. Its fruit is used to treat bilious conditions, diarrhea and dysentery. In this study, three new adamantyl derivatives, two new rearranged benzophenones, named as garcixanthochymones A–E (1–5), together with 12 known compounds including 7 xanthones (6–12) and 5 flavonoids (13–17) were isolated from the fruits of G. xanthochymus. Their structures were elucidated by detailed spectroscopic analyses. All isolated compounds were evaluated for their anti-proliferative activities against four human tumor cells (HepG2, A549, SGC7901, MCF-7). Adamantyl derivatives (1–3) and rearranged benzophenones (4–5) displayed potential inhibitory activity against four human cancer cell lines with IC50 values of 5.16–16.45 μM. These data suggested that the extracts of the fruits of G. xanthochymus are potent candidates for cancer prevention.
研究领域:
植物化学
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药理学
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肿瘤学
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产品关联
DOI
高影响因子
JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES
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2014
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IF 2.694
Yunfang Li,Yu Chen,Chuying Xiao,Dan Chen,Yuxiu Xiao,Zhinan Mei
α-Amylase inhibitors play an important role in management of diabetes and obesity. In order to rapidly discover potent α-amylase inhibitors from medicinal plants, a ligands-screening method based on enzyme-immobilized magnetic nanoparticles integrated with HPLC was developed. Amine-terminated magnetic nanoparticles were prepared for the immobilization of α-amylase. Based on the affinity theory, the α-amylase-coated magnetic nanoparticles were employed to fish out the ligands from the extracts of Garcinia xanthochymus , and the elutes were examined by HPLC. As a result, three ligands were screened out. Isolation and identification were carried out subsequently. By analyzing the UV, MS and NMR spectra, they were identified as three biflavonoids including GB2a glucoside (2), GB2a (3) and fukugetin (4). The IC 50 values of the three compounds were also determined. The results suggest the proposed approach is efficient and accurate, and has great potential in rapid discovery of drug candidates from medical plants.
研究领域:
药理学
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生物化学
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药物发现
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DOI
PubMed
高影响因子
Food & Function
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2020
·Vol. 11
·期 12
·10568-10579
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IF 4.171
Jing Xu,Shan Jin,Fei Gan,Hui Xiong,Zhinan Mei,Yu Chen,Guangzhong Yang
The fruits of Garcinia xanthochymus can be eaten raw or processed into jams, preserves and vinegar. They provide not only vitamin and protein nutrients, but also pharmacologically active compounds, among which polycyclic polyprenylated acylphloroglucinols (PPAPs) are a major class. According to the literature, PPAPs exhibited good anti-cancer effects. This study investigated the antitumor effects and the underlying mechanism of S1 (the regioisomeric mixture of xanthochymol and guttiferone E) and S2 (the regioisomeric mixture of isoxanthochymol and cycloxanthochymol) isolated from the fruits of G. xanthochymus. In an H22 allograft mouse model, S1 and S2 could suppress the liver tumor growth and phosphorylation of STAT3. Computational modeling showed that S1 and S2 could form hydrogen bonds with the SH2 domain of STAT3. In HepG2 and MCF-7 cell lines, S1 and S2 downregulated the expression of p-STAT3Tyr705. Moreover, S1 and S2 inhibited the phosphorylation of JAK2 and Src, which are the upstream kinases of STAT3, and the expression of various STAT3-regulated genes, including anti-apoptotic (Bcl-XL, Mcl-1 and survivin), proliferative (cyclin D1) and angiogenic (VEGF) genes. As a result, S1 and S2 arrested the cell cycle and induced cell apoptosis, which were proved by the activation of cleaved caspase-3 and caspase-8. These results demonstrated that S1 and S2 from G. xanthochymus exhibited antitumor effects through the inactivation of STAT3, and could be promising candidates for cancer treatment.
研究领域:
药理学
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肿瘤学
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分子生物学
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生物化学
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产品关联
DOI
PubMed
高影响因子
BIOORGANIC & MEDICINAL CHEMISTRY
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2017
·
IF 2.93
Yunfang Li,Ping Zhao,Yu Chen,Yanze Fu,Kuan Shi,Liu Liu,Hui Liu,Mingrui Xiong,Qing-Hua Liu,Guangzhong Yang,Yuxiu Xiao
Garcinia xanthochymus is a widely used folk medicine in southwestern China. Previous studies indicated it possesses potential anti-diabetic activities both in vitro (Fu et al., 2014; Nguyen et al., 2017) and in vivo (Shivanand et al., 2017). To discover bioactive ingredients from it and unveil their mechanism of action against diabetes, the present study was designed to isolate constituents from extract of G. xanthochymus , determine their structures, screen their activities and investigate mechanism of action of the active substances. Twenty compounds including a new depsidone named garciniadepsidone A ( 20 ) and 19 known xanthones were obtained. All of them were screened to discover the active compounds with anti-diabetic activities. Finally, three xanthones including 12 b -hydroxy-des- d -garcigerrin ( 5 ), 1,2,5,6-tretrahydroxy-4-(1,1-dimethyl-2-propenyl)-7-(3-methyl-2-butenyl) xanthone ( 13 ) and 1,5,6-trihydroxy-7,8-di(3-methyl-2-butenyl)-6′,6′-dimethylpyrano (2′,3′:3,4) xanthone ( 18 ) were found to be able to significantly stimulate the glucose uptake in the skeleton muscle cells. The effects of the three compounds were comparable to those of insulin and metformin . Based on molecular mechanistic study , it was found that both of compound 5 and 13 promoted glucose uptake by activating phosphatidylinositol-3 kinase (PI3K)/the serine/threonine kinase protein kinase B (PKB/Akt) signaling pathway and AMP-activated protein kinase (AMPK) signaling pathway, resulting in the translocation of GLUT4 in L6 myotubes without affecting the expression of GLUT4. Compound 5 and 13 have great potential to be developed as promising leads to target diabetes.
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DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
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2021
·Vol. 22
·期 19
·10365
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IF 5.924
Shan Jin,Wen Wang,Fei Gan,Wenli Xie,Jing Xu,Yu Chen,Zhinan Mei,Guangzhong Yang
Pharmacologic studies have revealed that polycyclic polyprenylated acylphloroglucinols (PPAPs) collectively exhibit a broad range of biological activities, including antineoplastic potential. Here, six new PPAPs, named garcixanthochymones F–K (3,5,7,8,11,and15), together with nine known analogues were isolated from the fruits ofGarcinia xanthochymus. Their structures were elucidated based on the spectroscopic data, including UV, HRESIMS, and NMR, and quantum chemical calculations. All the isolated PPAPs were tested for anti-proliferative activity against four human tumor cell lines, including SGC7901, A549, HepG2, and MCF-7. Most of the PPAPs possessed high anti-proliferative activity with IC50values in the range of 0.89 to 36.98 μM, and significant apoptosis was observed in MCF-7 cells exposed to compounds2and5. Besides, docking results showed that compounds2and5could strongly combine with the Src homology 2 (SH2) domain of STAT3 via hydrogen bond and hydrophobic interaction, which is one of the key oncogenes and crucial therapeutic targets. Furthermore, compounds2and5efficiently downregulated the expression of p-STAT3Tyr705and pivotal effector proteins involved in oncogenic signaling pathways of MCF-7 cells.Keywords:polycyclic polyprenylated acylphloroglucinols;Garcinia xanthochymus;anti-proliferative;STAT3;apoptosis
研究领域:
药理学
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肿瘤学
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化学
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产品关联
DOI
PubMed
高影响因子
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
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2019
·Vol. 20
·期 19
·4803
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IF 4.183
Shan Jin,Kuan Shi,Liu Liu,Yu Chen,Guangzhong Yang
Xanthones are important chemical constituents ofGarcinia xanthochymusand varied bioactivities including cytotoxicity. However, their anti-tumor mechanism has remained unknown. Here, we isolated and identified a new xanthone named garciniaxanthone I (1) and five known compounds from the bark ofG. xanthochymus. Their structures were elucidated by NMR analysis and HRESIMS. The anti-proliferation activities of all isolated compounds were evaluated on four human tumor cell lines (HepG2, A549, SGC7901, MCF-7). The results demonstrated that the anti-proliferation activity of xanthone was related to the number and location of prenyl groups. We further found that garciniaxanthone I (GXI) could induce HepG2 apoptosis and enhance the expression of cleaved caspase-8, caspase-9, and caspase-3. GXI could also increase Bax level and concurrently reduce the overexpression of Bcl-2, Bcl-XL, Mcl-1, and surviving in HepG2 cells. Moreover, GXI could inhibit cell migration of HepG2 cells by inhibiting the expressions of MMP-7 and MMP-9. In summary, our study suggests that GXI could induce HepG2 apoptosis via the mitochondrial pathway and might become a lead compound for liver cancer treatment.Keywords:xanthones;Garcinia xanthochymus;apoptosis;HepG2;caspase;Bcl-2 family;MMPs
研究领域:
药理学
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肿瘤学
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细胞生物学
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DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）