Bioassay-Guided Isolation and Structural Modification of the Anti-TB Resorcinols from Ardisia gigantifolia
Guan, Yi-Fu1,2; Song, Xun1,3; Qiu, Ming-Hua4; Luo, Shi-Hong4; Wang, Bao-Jie5; Nguyen Van Hung6; Cuong, Nguyen M.7; Soejarto, Djaja Doel8; Fong, Harry H. S.8; Franzblau, Scott G.5; Li, Sheng-Hong4; He, Zhen-Dan3; Zhang, Hong-Jie1
2016-08-01
Source PublicationCHEMICAL BIOLOGY & DRUG DESIGN
Volume88Issue:2Pages:293-301
AbstractTuberculosis (TB) is a highly contagious disease mainly caused by Mycobacterium tuberculosis H37RV. Antitubercular (anti-TB) bioassay-guided isolation of the CHCl3 extract of the leaves and stems of the medicinal plant Ardisia gigantifolia led to the isolation of two anti-TB 5-alkylresorcinols, 5-(8Z-heptadecenyl) resorcinol (1) and 5-(8Z-pentadecenyl) resorcinol (2). We further synthesized 15 derivatives based on these two natural products. These compounds (natural and synthetic) were evaluated for their anti-TB activity against Mycobacterium tuberculosis H37RV. Resorcinols 1 and 2 exhibited anti-TB activity with MIC values at 34.4 and 79.2 mu M in MABA assay, respectively, and 91.7 and 168.3 mu M in LORA assay, respectively. Among these derivatives, compound 8 was found to show improved anti-TB activity than its synthetic precursor (2) with MIC values at 42.0 mu M in MABA assay and 100.2 mu M in LORA assay. The active compounds should be regarded as new hits for further study as a novel class of anti-TB agents. The distinct structure-activity correlations of the parent compound were elucidated based on these derivatives.
KeywordArdisia Gigantifolia Isolation And Structure Identification Resorcinols Anti-tb Activity Mycobacterium Tuberculosis H37rv Structural Modification
DOI10.1111/cbdd.12756
Indexed BySCI
Language英语
WOS Research AreaBiochemistry & Molecular Biology ; Pharmacology & Pharmacy
WOS SubjectBiochemistry & Molecular Biology ; Chemistry, Medicinal
WOS IDWOS:000381035500013
Citation statistics
Document Type期刊论文
Identifierhttp://ir.kib.ac.cn/handle/151853/33597
Collection植物化学与西部植物资源持续利用国家重点实验室
Affiliation1.Hong Kong Baptist Univ, Sch Chinese Med, Hong Kong, Hong Kong, Peoples R China
2.HKBU Inst Res & Continuing Educ, Shenzhen 518057, Peoples R China
3.Shenzhen Univ, Engn Lab Shenzhen Nat Small Mol Innovat Drugs, Key Lab Novel Hlth Care Prod, Dept Pharm,Sch Med, Shenzhen 518060, Peoples R China
4.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources West Ch, Kunming 650201, Yunnan, Peoples R China
5.Univ Illinois, Coll Pharm, Inst TB Res, 833 South Wood St, Chicago, IL 60612 USA
6.Vietnam Acad Sci & Technol, Inst Marine Biochem, 18 Hoang Quoc Viet Rd, Hanoi, Vietnam
7.Cuc Phuong Natl Pk, Nho Quan Dist, Ninh Binh Provi, Vietnam
8.Univ Illinois, Coll Pharm, Dept Med Chem & Pharmacognosy, 833 South Wood St, Chicago, IL 60612 USA
Recommended Citation
GB/T 7714
Guan, Yi-Fu,Song, Xun,Qiu, Ming-Hua,et al. Bioassay-Guided Isolation and Structural Modification of the Anti-TB Resorcinols from Ardisia gigantifolia[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2016,88(2):293-301.
APA Guan, Yi-Fu.,Song, Xun.,Qiu, Ming-Hua.,Luo, Shi-Hong.,Wang, Bao-Jie.,...&Zhang, Hong-Jie.(2016).Bioassay-Guided Isolation and Structural Modification of the Anti-TB Resorcinols from Ardisia gigantifolia.CHEMICAL BIOLOGY & DRUG DESIGN,88(2),293-301.
MLA Guan, Yi-Fu,et al."Bioassay-Guided Isolation and Structural Modification of the Anti-TB Resorcinols from Ardisia gigantifolia".CHEMICAL BIOLOGY & DRUG DESIGN 88.2(2016):293-301.
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