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从 Guillauminia 和 Perrottetia 茎皮中分离和鉴定细胞毒性化合物。

Isolation and Characterization of Cytotoxic Compounds from Guill. and Perr. Stem Bark.

机构信息

Department of Pharmacognosy and Drug Development, University of Ilorin, Ilorin, Nigeria.

Department of Pharmacognosy, University of Ibadan, Ibadan, Nigeria.

出版信息

Anticancer Agents Med Chem. 2024;24(17):1295-1304. doi: 10.2174/0118715206317259240722113046.

Abstract

INTRODUCTION

Globally, about 8.2 million cancer-related deaths are recorded annually. Sadly, most of the deaths result from the toxicity of most chemotherapeutic agents. Hence, there are growing demands for chemotherapeutic agents with high specificity and selectivity. This study was designed to assess the cytotoxic potential of and isolate cytotoxic compounds with better selectivity profiles.

METHODS

Detarium microcarpum Stem bark (DMS) was collected and authenticated at the Forest Herbarium Ibadan (FHI), and a voucher (FHI-111954) was issued. Dried DMS was pulverized and extracted into 70% methanol. The extract was partitioned into hexane, dichloromethane, and ethyl acetate fractions. The cytotoxicities of the extract, fractions, and isolated compounds were determined. The cytotoxicity of the isolated compounds was tested against different cell lines, including human breast (AU565 and MDA MB231), oral adenosquamous (CAL27), and cervical (HeLa) cancer cells, as well as healthy (3T3) non-cancer cells.

RESULTS

Methyl gallate, eriodictyol, quercetin, quebrachitol, catechin, catechin gallate, and gallic acid, isolated from dichloromethane and ethyl acetate fractions, displayed weak cytotoxicity against breast (AU565 and MDAMD- 231) and cervical (HeLa) cancer cell lines. Interestingly, all the compounds, except gallic acid (48.91±4.51% inhibition), displayed potent cytotoxicity on oral cancer cells. Methyl gallate and quercetin displayed the highest activity, with IC values of 89.57±1.98μM and 78.19±1.49μM, respectively. Interestingly, all the compounds were not toxic to healthy non-cancer (3T3) cells.

CONCLUSION

The compounds displayed anticancer activity specific to oral cancer cells and were highly selective for cancer cells without causing significant toxicity to healthy non-cancer cells.

摘要

简介

全球每年记录约 820 万例与癌症相关的死亡。可悲的是,大多数死亡是由大多数化疗药物的毒性引起的。因此,人们对具有高特异性和选择性的化疗药物的需求日益增长。本研究旨在评估 和分离具有更好选择性特征的细胞毒性化合物。

方法

采集和鉴定 Detarium microcarpum Stem bark(DMS)在森林标本馆伊巴丹(FHI),并出具凭证(FHI-111954)。DMS 干燥后粉碎并提取 70%甲醇。提取物分为正己烷、二氯甲烷和乙酸乙酯馏分。测定提取物、馏分和分离化合物的细胞毒性。分离化合物的细胞毒性针对不同的细胞系进行测试,包括人乳腺癌(AU565 和 MDA MB231)、口腔腺鳞癌(CAL27)和宫颈癌(HeLa)细胞,以及健康(3T3)非癌细胞。

结果

从二氯甲烷和乙酸乙酯馏分中分离出的没食子酸甲酯、桔皮素、槲皮素、奎尼醇、儿茶素、儿茶素没食子酸酯和没食子酸对乳腺癌(AU565 和 MDAMD-231)和宫颈癌(HeLa)细胞系表现出微弱的细胞毒性。有趣的是,除了没食子酸(48.91±4.51%抑制)外,所有化合物对口腔癌细胞均表现出强大的细胞毒性。没食子酸甲酯和槲皮素表现出最高的活性,IC 值分别为 89.57±1.98μM 和 78.19±1.49μM。有趣的是,所有化合物对健康非癌细胞(3T3)均无毒性。

结论

这些化合物对口腔癌细胞表现出抗癌活性,并且对癌细胞具有高度选择性,而对健康非癌细胞没有显著毒性。

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