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Bioactivity-based molecular networking-guided identification of guttiferone J from Garcinia cambogia as an anti-obesity candidate

文献类型：期刊论文

作者Feng, Zheling1; Chen, Jiali1; Chen, Cheng1; Feng, Lu2; Wang, Rui1; Zhu, Jianzhong1; Lou, Ruohan1; Liu, Jia2; Ye, Yang2; Lin, Ligen1,3,4,5
刊名BRITISH JOURNAL OF PHARMACOLOGY
出版日期2022-11-22
页码20
ISSN号0007-1188
关键词anti-obesity bioactivity-based molecular networking Garcinia cambogia guttiferone J sirtuin 3 white adipose tissue browning
DOI10.1111/bph.15979
通讯作者Lin, Ligen(ligenl@um.edu.mo)
英文摘要Background and PurposePharmacological intervention to induce browning of white adipose tissue provides a promising anti-obesity therapy. The fruits of Garcinia cambogia (Clusiaceae) have been widely applied to manage body weight; however, the chemical principles remain unclear. The current study aims to discover browning inducers from the fruits of G. cambogia and investigate the underlying mechanisms. Experimental ApproachThe bioactivity-based molecular networking and Oil Red O staining on 3T3-L1 and C3H10T1/2 adipocytes were applied for guided isolation. High-fat diet-induced obese mice were recruited to evaluate the anti-obesity activity. Key ResultsThe bioactivity-based molecular networking-guided isolation yielded several polycyclic polyprenylated acylphloroglucinols from the fruits of G. cambogia with lipid-lowering effect in adipocytes, including guttiferone J (GOJ), garcinol and 14-deoxygarcinol. As the most potent one, GOJ (10 mu M) reduced lipid accumulation by 70% and 76% in 3T3-L1 and C3H10T1/2 adipocytes, respectively. Furthermore, GOJ (2.5-10 mu M) increased the expression of the deacetylase sirtuin 3 (SIRT3) and activated it, which, in turn, reduced the acetylation level of PPAR gamma coactivator-1 alpha to boost mitochondrial biogenesis and promoted uncoupling protein 1 expression to enhance thermogenesis, resulting in browning of adipocytes. In high-fat diet-induced-obese mice, GOJ (10 and 20 mg center dot kg(-1)center dot day(-1) for 12 weeks) protected against adiposity, hyperlipidaemia, insulin resistance and liver lipotoxicity, through boosting SIRT3-mediated browning of inguinal adipose tissue. Conclusion and ImplicationsGOJ represents a new scaffold of thermogenic inducer, which is responsible for the anti-obesity property of G. cambogia and can be further developed as a candidate for treating obesity and its related disorders.
WOS关键词ADIPOSE-TISSUE ; CONCISE GUIDE ; NATURAL-PRODUCTS ; THERMOGENESIS ; EXPRESSION ; DISCOVERY ; AUTOPHAGY ; OBESITY ; SIRT3 ; CELL
资助项目Fundo para o Desenvolvimento das Ciencias e da Tecnologia[0064/2021/AGJ] ; National Natural Science Foundation of China[81872754] ; National Natural Science Foundation of China[82073715] ; Internal Research Grant of the State Key Laboratory of Quality Research in Chinese Medicine, University of Macau[QRCM-IRG2022-014] ; Open Research Fund of Chengdu University of Traditional Chinese Medicine Key Laboratory of Systematic Research of Distinctive Chinese Medicine Resources in Southwest China[2022GZ2011011] ; University of Macau[MYRG2021-00177-ICMS] ; University of Macau[MYRG2020-00091-ICMS]
WOS研究方向Pharmacology & Pharmacy
语种英语
出版者WILEY
WOS记录号WOS:000888142300001
源URL[http://119.78.100.183/handle/2S10ELR8/304530]  
专题新药研究国家重点实验室
通讯作者Lin, Ligen
作者单位1.Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Res Chinese Med, Macau, Macau, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Nat Prod Chem Dept, Shanghai, Peoples R China
3.Chinese Acad Sci, State Key Lab Drug Res, Shanghai, Peoples R China
4.Univ Macau, Fac Hlth Sci, Dept Pharmaceut Sci & Technol, Macau, Macau, Peoples R China
5.Univ Macau, Inst Chinese Med Sci, State Key Lab Qual Res Chinese Med, Ave Univ, Taipa 999078, Macau, Peoples R China
推荐引用方式
GB/T 7714		 Feng, Zheling,Chen, Jiali,Chen, Cheng,et al. Bioactivity-based molecular networking-guided identification of guttiferone J from Garcinia cambogia as an anti-obesity candidate[J]. BRITISH JOURNAL OF PHARMACOLOGY,2022:20.
APA Feng, Zheling.,Chen, Jiali.,Chen, Cheng.,Feng, Lu.,Wang, Rui.,...&Lin, Ligen.(2022).Bioactivity-based molecular networking-guided identification of guttiferone J from Garcinia cambogia as an anti-obesity candidate.BRITISH JOURNAL OF PHARMACOLOGY,20.
MLA Feng, Zheling,et al."Bioactivity-based molecular networking-guided identification of guttiferone J from Garcinia cambogia as an anti-obesity candidate".BRITISH JOURNAL OF PHARMACOLOGY (2022):20.

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来源：上海药物研究所

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