Isolation, identification and antiviral activities of metabolites of calycosin-7-O-beta-D-glucopyranoside

	Isolation, identification and antiviral activities of metabolites of calycosin-7-O-beta-D-glucopyranoside
	Chen LY 1; Li ZX 1; Tang YH 1; Cui XL 3; Luo RH 2; Guo SS 3; Zheng YT2; Huang CG1; zhengyt@mail.kiz.ac.cn ; cghsimm@126.com
	2011
发表期刊	JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
卷号	56 期号:2 页码:382-389
合作性质	其它
摘要	In vivo and in vitro metabolites of calycosin-7-O-beta-D-glucopyranoside in rats were identified using a specific and sensitive high performance liquid chromatography-tandem mass spectrometry (HPLC-MS(n)) method. The parent compound and twelve metabolites were found in rat urine after oral administration of calycosin-7-O-beta-D-glucopyranoside. The parent compound and six metabolites were detected in rat plasma. In heart, liver, spleen, lung and kidney samples, respectively, six, eight, seven, nine and nine metabolites were identified, in addition to the parent compound. Three metabolites, but no trace of parent drug, were found in the rat intestinal flora incubation mixture and feces, which demonstrated cleavage of the glycosidic bond of the parent compound in intestines. The main phase I metabolic pathways of calycosin-7-O-beta-D-glucopyranoside in rats were deglycosylation, dehydroxylation and demethylation reactions; phase II metabolism included sulfation, methylation, glucuronidation and glycosylation (probably). Furthermore, two metabolites commonly found in rat urine, plasma and tissues were isolated from feces and characterized by NMR. The antiviral activities of the metabolite calycosin against coxsackie virus B(3) (CVB(3)) and human immunodeficiency virus (HIV) were remarkably stronger than those of calycosin-7-O-beta-D-glucopyranoside.
关键词	Calycosin-7-o-beta-d-glucopyranoside Metabolites Antiviral Activity
资助者	This work was supported by the National Science & Technol- ogy Major Project “Key New Drug Creation and Manufacturing Program”, China (Grant no. 2009ZX09301-001; 2009ZX09308-005; 2009ZX09501-030; 2009ZX09103-334; 2009ZX09301-005-007; 2009ZX09501-029). ; This work was supported by the National Science & Technol- ogy Major Project “Key New Drug Creation and Manufacturing Program”, China (Grant no. 2009ZX09301-001; 2009ZX09308-005; 2009ZX09501-030; 2009ZX09103-334; 2009ZX09301-005-007; 2009ZX09501-029). ; This work was supported by the National Science & Technol- ogy Major Project “Key New Drug Creation and Manufacturing Program”, China (Grant no. 2009ZX09301-001; 2009ZX09308-005; 2009ZX09501-030; 2009ZX09103-334; 2009ZX09301-005-007; 2009ZX09501-029). ; This work was supported by the National Science & Technol- ogy Major Project “Key New Drug Creation and Manufacturing Program”, China (Grant no. 2009ZX09301-001; 2009ZX09308-005; 2009ZX09501-030; 2009ZX09103-334; 2009ZX09301-005-007; 2009ZX09501-029).
收录类别	SCI
语种	英语
资助者	This work was supported by the National Science & Technol- ogy Major Project “Key New Drug Creation and Manufacturing Program”, China (Grant no. 2009ZX09301-001; 2009ZX09308-005; 2009ZX09501-030; 2009ZX09103-334; 2009ZX09301-005-007; 2009ZX09501-029). ; This work was supported by the National Science & Technol- ogy Major Project “Key New Drug Creation and Manufacturing Program”, China (Grant no. 2009ZX09301-001; 2009ZX09308-005; 2009ZX09501-030; 2009ZX09103-334; 2009ZX09301-005-007; 2009ZX09501-029). ; This work was supported by the National Science & Technol- ogy Major Project “Key New Drug Creation and Manufacturing Program”, China (Grant no. 2009ZX09301-001; 2009ZX09308-005; 2009ZX09501-030; 2009ZX09103-334; 2009ZX09301-005-007; 2009ZX09501-029). ; This work was supported by the National Science & Technol- ogy Major Project “Key New Drug Creation and Manufacturing Program”, China (Grant no. 2009ZX09301-001; 2009ZX09308-005; 2009ZX09501-030; 2009ZX09103-334; 2009ZX09301-005-007; 2009ZX09501-029).
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/353002/6631
专题	科研部门_分子免疫药理学（郑永唐）科研部门_动物模型与人类重大疾病机理重点实验室
通讯作者	zhengyt@mail.kiz.ac.cn; cghsimm@126.com
作者单位	1.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 501 Haike Rd., Pudong, 201203 Shanghai, China 2.Key Laboratory of Animal Models and Human Disease Mechanisms, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China 3.Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, China
推荐引用方式 GB/T 7714	Chen LY,Li ZX,Tang YH,et al. Isolation, identification and antiviral activities of metabolites of calycosin-7-O-beta-D-glucopyranoside[J]. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,2011,56(2):382-389.
APA	Chen LY.,Li ZX.,Tang YH.,Cui XL.,Luo RH.,...&cghsimm@126.com.(2011).Isolation, identification and antiviral activities of metabolites of calycosin-7-O-beta-D-glucopyranoside.JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,56(2),382-389.
MLA	Chen LY,et al."Isolation, identification and antiviral activities of metabolites of calycosin-7-O-beta-D-glucopyranoside".JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS 56.2(2011):382-389.

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