具有细胞毒性和抗炎活性的植物化学物质。

Phytochemicals from with potent cytotoxic and anti-inflammatory activities.

机构信息

HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.

Dr. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi, Pakistan.

出版信息

Nat Prod Res. 2022 Mar;36(6):1587-1592. doi: 10.1080/14786419.2021.1886101. Epub 2021 Feb 14.

DOI:10.1080/14786419.2021.1886101

PMID:33583281

Abstract

Six natural products () were isolated from the fresh leaves of including ursolic acid (, ursolic acid-γ-lactone (, 27----coumaroyl ursolic acid (, 23-hydroxy ursolic acid (, uvaol ( and ursolic aldehyde (. Their structure elucidation was done by modern spectroscopic techniques including H-NMR, C-NMR and comparison with reported data. All compounds were known, while were isolated for the first time from the genus . Isolated compounds were screened for their cytotoxic MTT assay and anti-inflammatory potential luminol-enhanced chem-iluminescence assay. Compounds and showed potent activity against lung cancer cell line (NCI-H460), and showed potent anti-inflammatory activity against reactive oxygen species production from human whole blood phagocytes. Compound displayed good selective cytotoxicity against NCI-H460 and did not provoke cytotoxicity against normal cell line upto 250 μM. Compounds were identified as potential anti-cancer drug leads.

摘要

从新鲜的叶片中分离得到 6 种天然产物，包括熊果酸（，熊果酸-γ-内酯（，27----咖啡酰基熊果酸（，23-羟基熊果酸（，齐墩果酸（和熊果酸醛（。通过现代光谱技术（包括 H-NMR、C-NMR 和与报道数据的比较）对其结构进行了鉴定。所有化合物均为已知化合物，而化合物是首次从该属中分离得到的。对分离得到的化合物进行了细胞毒性（MTT 法）和抗炎活性（发光增强化学发光法）的筛选。化合物和对肺癌细胞系（NCI-H460）表现出较强的活性，化合物对人全血吞噬细胞产生的活性氧具有较强的抗炎活性。化合物对 NCI-H460 具有良好的选择性细胞毒性，在 250 μM 浓度下对正常细胞系没有引起细胞毒性。化合物被鉴定为有潜力的抗癌药物先导化合物。