Carlotta Zamboni , Fatima Iganya Suleiman , Eduard Mas-Claret , Sajni Shah , Martin Cheek , Quentin Luke , Sani M. Isyaka , Moses K. Langat
{"title":"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","authors":"Carlotta Zamboni , Fatima Iganya Suleiman , Eduard Mas-Claret , Sajni Shah , Martin Cheek , Quentin Luke , Sani M. Isyaka , Moses K. Langat","doi":"10.1016/j.sciaf.2025.e02981","DOIUrl":null,"url":null,"abstract":"<div><div>The leaves of <em>Vepris glandulosa</em> gave ten compounds, nine known, flindersine (<strong>1a</strong>), 7-methoxyflindersine (<strong>1b</strong>), 7-prenyloxyflindersine (<strong>3</strong>), toddaliopsin C (<strong>4</strong>), xanthoxoline (<strong>5</strong>), arborinine (<strong>6</strong>), lupeol, sitosterol and pheophytin a, and one previously undescribed compound <em>N-</em>acetoxymethyl-7-methoxyflindersine (<strong>2</strong>). The leaves of <em>Vepris hanangensis</em> var. <em>unifoliata</em> gave eleven compounds, eight known, 7-methoxyflindersine (<strong>1b</strong>), 7-prenyloxyflindersine (<strong>3</strong>), toddaliopsin C (<strong>4</strong>), xanthoxoline (<strong>5</strong>) arborinine (<strong>6</strong>), lupeol, sitosterol and pheophytin a, and three previously undescribed compounds <em>N-</em>acetoxymethyl-7-methoxyflindersine (<strong>2</strong>), 8-carboxygeranioloxyflindersine (<strong>7</strong>) and 8-carboxygeranioloxy-N-methylflindersine (<strong>8</strong>). Compounds <strong>1a, 1b, 2</strong>-<strong>8</strong> were analysed for their <em>in silico</em> inhibitory effect against HIV-1 reverse transcriptase and compounds <strong>1b, 2, 7</strong> and <strong>8</strong> were analysed for their <em>in vitro</em> inhibitory effects against HIV-1 reverse transcriptase.</div></div>","PeriodicalId":21690,"journal":{"name":"Scientific African","volume":"30 ","pages":"Article e02981"},"PeriodicalIF":3.3000,"publicationDate":"2025-09-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"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\",\"authors\":\"Carlotta Zamboni , Fatima Iganya Suleiman , Eduard Mas-Claret , Sajni Shah , Martin Cheek , Quentin Luke , Sani M. Isyaka , Moses K. Langat\",\"doi\":\"10.1016/j.sciaf.2025.e02981\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>The leaves of <em>Vepris glandulosa</em> gave ten compounds, nine known, flindersine (<strong>1a</strong>), 7-methoxyflindersine (<strong>1b</strong>), 7-prenyloxyflindersine (<strong>3</strong>), toddaliopsin C (<strong>4</strong>), xanthoxoline (<strong>5</strong>), arborinine (<strong>6</strong>), lupeol, sitosterol and pheophytin a, and one previously undescribed compound <em>N-</em>acetoxymethyl-7-methoxyflindersine (<strong>2</strong>). The leaves of <em>Vepris hanangensis</em> var. <em>unifoliata</em> gave eleven compounds, eight known, 7-methoxyflindersine (<strong>1b</strong>), 7-prenyloxyflindersine (<strong>3</strong>), toddaliopsin C (<strong>4</strong>), xanthoxoline (<strong>5</strong>) arborinine (<strong>6</strong>), lupeol, sitosterol and pheophytin a, and three previously undescribed compounds <em>N-</em>acetoxymethyl-7-methoxyflindersine (<strong>2</strong>), 8-carboxygeranioloxyflindersine (<strong>7</strong>) and 8-carboxygeranioloxy-N-methylflindersine (<strong>8</strong>). Compounds <strong>1a, 1b, 2</strong>-<strong>8</strong> were analysed for their <em>in silico</em> inhibitory effect against HIV-1 reverse transcriptase and compounds <strong>1b, 2, 7</strong> and <strong>8</strong> were analysed for their <em>in vitro</em> inhibitory effects against HIV-1 reverse transcriptase.</div></div>\",\"PeriodicalId\":21690,\"journal\":{\"name\":\"Scientific African\",\"volume\":\"30 \",\"pages\":\"Article e02981\"},\"PeriodicalIF\":3.3000,\"publicationDate\":\"2025-09-17\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Scientific African\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S246822762500451X\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"MULTIDISCIPLINARY SCIENCES\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Scientific African","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S246822762500451X","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"MULTIDISCIPLINARY SCIENCES","Score":null,"Total":0}
引用次数: 0
摘要
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。
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
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.