Unusual N-acetoxymethyl derivatives of flindersine and acridone alkaloids from Kenyan Vepris glandulosa and V. hanangensis var unifoliata and their inhibitory effects against HIV 1 reverse transcriptase

IF 3.3 Q2 MULTIDISCIPLINARY SCIENCES

Scientific African Pub Date : 2025-09-17 DOI:10.1016/j.sciaf.2025.e02981

Carlotta Zamboni , Fatima Iganya Suleiman , Eduard Mas-Claret , Sajni Shah , Martin Cheek , Quentin Luke , Sani M. Isyaka , Moses K. Langat

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Abstract

The leaves of Vepris glandulosa gave ten compounds, nine known, flindersine (1a), 7-methoxyflindersine (1b), 7-prenyloxyflindersine (3), toddaliopsin C (4), xanthoxoline (5), arborinine (6), lupeol, sitosterol and pheophytin a, and one previously undescribed compound N-acetoxymethyl-7-methoxyflindersine (2). The leaves of Vepris hanangensis var. unifoliata gave eleven compounds, eight known, 7-methoxyflindersine (1b), 7-prenyloxyflindersine (3), toddaliopsin C (4), xanthoxoline (5) arborinine (6), lupeol, sitosterol and pheophytin a, and three previously undescribed compounds N-acetoxymethyl-7-methoxyflindersine (2), 8-carboxygeranioloxyflindersine (7) and 8-carboxygeranioloxy-N-methylflindersine (8). Compounds 1a, 1b, 2-8 were analysed for their in silico inhibitory effect against HIV-1 reverse transcriptase and compounds 1b, 2, 7 and 8 were analysed for their in vitro inhibitory effects against HIV-1 reverse transcriptase.

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肯尼亚野田螺和野田螺中少见的氟林德苷和吖啶酮生物碱n -乙酰氧基衍生物及其对HIV - 1逆转录酶的抑制作用

芦笋叶中含有10种化合物，其中9种已知，分别为：flindersin （1a）、7-甲氧基flindersin （1b）、7-prenyloxyflindersin(3)、totolaliopsin C(4)、xanthoxoline(5)、虫苷(6)、lupeol、谷甾醇和pheophytin a，以及1种先前未描述的化合物n -acetoxymethyl-7-甲氧基flindersin(2)。从单叶紫荆叶中分离出了11个已知化合物，其中8个为7-甲氧基flindersin （1b）、7-丙基氧基flindersin(3)、桃油苷C(4)、黄嘌呤(5)、虫苷(6)、lupeol、谷甾醇和pheophytin a，以及3个此前未被发现的化合物n -乙酰氧基甲基-7-甲氧基flindersin(2)、8-羧基香叶油氧基- n -甲基flindersin(7)和8-羧基香叶油氧基- n -甲基flindersin(8)。分析了化合物1a、1b、2-8对HIV-1逆转录酶的体外抑制作用，分析了化合物1b、2、7和8对HIV-1逆转录酶的体外抑制作用。

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