摘要
Cissampelos属包括21种具有广泛的全球分布和各种药理活性如止痛和解热,抗炎,抗过敏,支气管扩张和免疫调节的物种。从该属中分离出几种具有不同生物活性的生物碱我们将突出解热活动,抗炎,抗过敏,支气管扩张和免疫调节活动。此外,我们应用与内部数据库的Cissampelos属的63次次级代谢物的小数据集的基于结构的虚拟筛选相关的基于配体的虚拟筛选,以选择具有潜在抗炎活性的化合物。对于抑制酶MAPKp38α,PKCβ,PKCθ和PKCζ,观察到hayatine(26),等位基因(30),pelosine(52),sepigeine(59)和warifteine(63)的亲和力。单独的香芹黄酮化合物(8)对PKCζ没有潜在的抑制活性或对PKCα的亲和力。该化合物可用作进一步研究具有潜在抗炎活性的结构的起点。
关键词: Cissampelos,抗炎活性,虚拟筛选,多靶标,次级代谢物,哮喘。
Current Medicinal Chemistry
Title:Secondary Metabolites from Cissampelos, A Possible Source for New Leads with Anti-Inflammatory Activity
Volume: 24 Issue: 16
关键词: Cissampelos,抗炎活性,虚拟筛选,多靶标,次级代谢物,哮喘。
摘要: The genus Cissampelos comprises of 21 species which have a wide global distribution and various pharmacological activities such as analgesic and antipyretic, antiinflammatory, anti-allergic, bronchodilation, and immunomodulation among others. Several compounds, mainly alkaloids with differing biological activities have been isolated from this genus. We will highlight antipyretic activities, anti-inflammatory, antiallergic, bronchodilatory, and immunomodulatory activities. In addition, we applied ligand-based-virtual screening associated with structure-based-virtual screening of a small dataset of 63 secondary metabolites from the Cissampelos genus of an in-house data bank, in order to select compounds with potential anti-inflammatory activity. Affinities were observed for hayatine (26), isochondrondendrine (30), pelosine (52), sepeerine (59), and warifteine (63) to the inhibiting enzymes MAPK p38 alpha, PKC beta, PKC theta and PKC zeta. The cissampeloflavone compound (8) alone showed no potential inhibitory activity for PKC zeta, or affinity for the PKC alpha. The compounds can be used as starting points for further studies on structures with potential anti-inflammatory activity.
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Cite this article as:
Secondary Metabolites from Cissampelos, A Possible Source for New Leads with Anti-Inflammatory Activity, Current Medicinal Chemistry 2017; 24 (16) . https://dx.doi.org/10.2174/0929867323666161227123411
DOI https://dx.doi.org/10.2174/0929867323666161227123411 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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