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辣木中槲皮素-3-O-葡萄糖苷和4-(β-D-吡喃葡萄糖基-1→4-α-L-鼠李糖吡喃糖氧基)-苄基异硫氰酸酯的细胞毒性、抗氧化及凋亡研究

Cytotoxicity, Antioxidant and Apoptosis Studies of Quercetin-3-O Glucoside and 4-(β-D-Glucopyranosyl-1→4-α-L-Rhamnopyranosyloxy)-Benzyl Isothiocyanate from Moringa oleifera.

作者信息

Maiyo Fiona C, Moodley Roshila, Singh Moganavelli

机构信息

Non-Viral Gene Delivery Laboratory, Discipline of Biochemistry, School of Life Sciences, University of KwaZulu-Natal, Durban 4000, South Africa.

出版信息

Anticancer Agents Med Chem. 2016;16(5):648-56. doi: 10.2174/1871520615666151002110424.

DOI:10.2174/1871520615666151002110424
PMID:26428271
Abstract

Moringa oleifera, from the family Moringaceae, is used as a source of vegetable and herbal medicine and in the treatment of various cancers in many African countries, including Kenya. The present study involved the phytochemical analyses of the crude extracts of M.oleifera and biological activities (antioxidant, cytotoxicity and induction of apoptosis in-vitro) of selected isolated compounds. The compounds isolated from the leaves and seeds of the plant were quercetin-3-O-glucoside (1), 4-(β-D-glucopyranosyl-1→4-α-L-rhamnopyranosyloxy)-benzyl isothiocyanate (2), lutein (3), and sitosterol (4). Antioxidant activity of compound 1 was significant when compared to that of the control, while compound 2 showed moderate activity. The cytotoxicity of compounds 1 and 2 were tested in three cell lines, viz. liver hepatocellular carcinoma (HepG2), colon carcinoma (Caco-2) and a non-cancer cell line Human Embryonic Kidney (HEK293), using the MTT cell viability assay and compared against a standard anticancer drug, 5-fluorouracil. Apoptosis studies were carried out using the acridine orange/ethidium bromide dual staining method. The isolated compounds showed selective in vitro cytotoxic and apoptotic activity against human cancer and non-cancer cell lines, respectively. Compound 1 showed significant cytotoxicity against the Caco-2 cell line with an IC50 of 79 μg mL(-1) and moderate cytotoxicity against the HepG2 cell line with an IC50 of 150 μg mL(-1), while compound 2 showed significant cytotoxicity against the Caco- 2 and HepG2 cell lines with an IC50 of 45 μg mL(-1) and 60 μg mL(-1), respectively. Comparatively both compounds showed much lower cytotoxicity against the HEK293 cell line with IC50 values of 186 μg mL(-1) and 224 μg mL(-1), respectively.

摘要

辣木属辣木科植物,在包括肯尼亚在内的许多非洲国家,它被用作蔬菜和草药的来源,并用于治疗各种癌症。本研究涉及辣木粗提物的植物化学分析以及所选分离化合物的生物活性(抗氧化、细胞毒性和体外诱导凋亡)。从该植物的叶子和种子中分离出的化合物有槲皮素 - 3 - O - 葡萄糖苷(1)、4 -(β - D - 吡喃葡萄糖基 - 1→4 - α - L - 鼠李糖吡喃糖氧基)- 苄基异硫氰酸酯(2)、叶黄素(3)和甾醇(4)。与对照相比,化合物1的抗氧化活性显著,而化合物2表现出中等活性。使用MTT细胞活力测定法在三种细胞系中测试了化合物1和2的细胞毒性,这三种细胞系分别是肝癌细胞系(HepG2)、结肠癌细胞系(Caco - 2)和非癌细胞系人胚肾细胞系(HEK293),并与标准抗癌药物5 - 氟尿嘧啶进行比较。使用吖啶橙/溴化乙锭双重染色法进行凋亡研究。分离出的化合物分别对人癌细胞系和非癌细胞系显示出选择性的体外细胞毒性和凋亡活性。化合物1对Caco - 2细胞系显示出显著的细胞毒性,IC50为79 μg mL(-1),对HepG2细胞系显示出中等细胞毒性,IC50为150 μg mL(-1),而化合物2对Caco - 2和HepG2细胞系分别显示出显著的细胞毒性,IC50分别为45 μg mL(-1)和60 μg mL(-1)。相比之下,两种化合物对HEK293细胞系的细胞毒性要低得多,IC50值分别为186 μg mL(-1)和224 μg mL(-1)。

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