Antiproliferative activities of phytochemicals isolated from the leaves of Dolichos kilimandischaricus (Harms) ex Taub. (Fabaceae) on Jurkat and HL-60 leukemic cells.

IF 3.4 2区 医学 Q1 INTEGRATIVE & COMPLEMENTARY MEDICINE
Simbarashe Sithole, Paul Mushonga, Matthias Heydenreich, Cephas Mawere, Stanley Mukanganyama
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引用次数: 0

Abstract

Background: Natural plant products represent one of the most productive sources of innovative lead drugs for the treatment of a wide range of ailments. Dolichos kilimandischaricus (Harms) ex Taub. (Fabaceae) root extracts have been traditionally used for the treatment of HPV-related cancers. The extracts from the plant have been previously shown to have antiproliferative effects on cancer cell lines. This study aimed to isolate, purify, and analyze the phytochemicals from the leaves of D. kilimandischaricus.

Methods: Phytochemicals in the ethanol leaf extract were separated by column chromatography on silica gel. The structures of the compounds were elucidated using spectroscopic techniques, then compared with the reported spectral data. Cytotoxicity of the phytochemicals on HL-60 and Jurkat cells was assessed by the sulphorhodamine B (SRB) assay with chlorambucil as a positive control. Docking simulations were used to further understand the binding preferences of the isolated compounds.

Results: The isolated compounds were identified as 3β-stigmasterol (1) and α-spinasterol (2). The results showed that both compounds were more potent against HL-60 cells than Jurkat cells, with IC50 values of 9.49 and 8.66 µg/mL, respectively. The two compounds function as 1HJC and 6VG8 inhibitors, according to the docking results, with the highest negative molecular binding affinities shown for both ligands against 1HJC.

Conclusions: Therefore, this study has identified some of the phytochemicals that may be responsible for the antiproliferative activity in D. kilimandischaricus. These phytochemicals may provide leads in the development of compounds for treating cancer and related neoplastic diseases.

Clinical trial number: Not applicable.

kilimandischaricus (Harms) ex Taub的叶片中分离的植物化学物质的抗增殖活性。(豆科)对Jurkat和HL-60白血病细胞的作用。
背景:天然植物产品是治疗多种疾病的创新先导药物的最具生产力的来源之一。《乞力曼卸charicus》(哈姆斯)ex Taub。(豆科)根提取物传统上用于治疗hpv相关癌症。这种植物的提取物先前已被证明对癌细胞系具有抗增殖作用。本研究旨在分离、纯化和分析乞力曼discharicus叶片中的植物化学物质。方法:采用硅胶柱层析法分离乙醇叶提取物中的植物化学成分。利用光谱技术对化合物的结构进行了分析,并与已有的光谱数据进行了比较。以氯苯为阳性对照,采用磺胺B (sulphorhodamine B, SRB)法评价植物化学物质对HL-60和Jurkat细胞的细胞毒性。对接模拟用于进一步了解分离化合物的结合偏好。结果:分离得到的化合物鉴定为3β-豆甾醇(1)和α-spinasterol(2)。结果表明,两种化合物对HL-60细胞的IC50值分别为9.49µg/mL和8.66µg/mL,均优于Jurkat细胞。对接结果显示,这两种化合物分别作为1HJC和6VG8抑制剂,两种配体对1HJC的负分子结合亲和度最高。结论:本研究确定了一些可能与kilimandischaricus抗增殖活性有关的植物化学物质。这些植物化学物质可能为开发治疗癌症和相关肿瘤疾病的化合物提供线索。临床试验号:不适用。
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来源期刊
BMC Complementary Medicine and Therapies
BMC Complementary Medicine and Therapies INTEGRATIVE & COMPLEMENTARY MEDICINE-
CiteScore
6.10
自引率
2.60%
发文量
300
审稿时长
19 weeks
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