壳聚糖负载龙葵碱糖生物碱的作用。叶提取物的抗炎和体外抗癌作用。

IF 1.8 Q3 PHARMACOLOGY & PHARMACY Turkish Journal of Pharmaceutical Sciences Pub Date : 2023-08-22 DOI:10.4274/tjps.galenos.2022.03837
Cletus Anes Ukwubile, Emmanuel Oise Ikpefan, Ademola Clement Famurewa
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引用次数: 2

摘要

目的:药用龙葵。通常“非洲龙葵”或“越橘”是一种植物,其叶子被尼日利亚和喀麦隆的部落分别用来制作流行的“Kombi”和“Njama Njama”汤。本研究旨在评价黄芩叶粗甲醇提取物的抗炎和抗癌活性。材料与方法:采用角叉菜胶诱导小鼠浮肿的方法,检测植物提取物对MCF-7和HMVII细胞系的抗炎活性和体外抗癌活性,并采用流式细胞术分别进行3-(4,5-二甲基噻唑-2-基)-2,5-二苯基- 2h -溴化四氮唑、跨井迁移和侵袭实验以及细胞凋亡研究等细胞毒性试验。结果:生物引导分离得到白色结晶化合物3-硝基二苯并呋喃(C12H7NO3, m/z;213.19 g/mol, m.p;181.49°C)。1H-NMR在δ (ppm) 2.8 ~ 4.3处显示7个碳信号,包括2个双线和5个单线;13C-NMR在δ (ppm) 120 ~ 195处显示12个碳信号,主要是甲基碳。所有测试样品在卡拉胶诱导的小鼠中显示出剂量依赖性的抗炎活性。分离得到的茄碱和壳聚糖负载药物对MCF-7和HMVII细胞的抑制浓度分别为8.52、0.82和22.1 μg/mL,抑制浓度分别为4.54、0.08和12.1 μg/mL,而阳性对照阿霉素对MCF-7和HMVII细胞的抑制浓度分别为0.02和0.06 μg/mL。在本研究中,龙葵碱的选择性指数最低,因此缺乏对Vero E6细胞系癌细胞和正常细胞的区分能力。壳聚糖负载药物加速细胞早期凋亡和持续细胞晚期凋亡,并显著改善细胞的选择性指标。结论:本研究结果进一步肯定了壳聚糖纳米颗粒作为抗癌药物载体的应用前景。
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Role of Chitosan-Loaded Solanine Glycoalkaloid from Solanum scabrum Mill. Leaf Extract as Anti-Inflammatory and In Vitro Anticancer Agents.

Objectives: Solanum scabrum Mill. commonly "African nightshade" or "huckleberry" is a plant, whose leaves are used by tribes in Nigeria and Cameroon for making the popular "Kombi" and "Njama Njama" soups, respectively. This study aimed to evaluate the anti-inflammatory and anticancer activities of the leaf crude methanol extract from S. scabrum.

Materials and methods: Fractions of the plant were tested for anti-inflammatory potential and in vitro anticancer activity on MCF-7 and HMVII cell lines by carrageenan-induced oedema in mice, and cytotoxicity assays such as 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide, transwell migration and invasion assays, and apoptosis study by flow cytometry, respectively.

Results: Bioguided isolation yielded a white crystalline compound 3-nitro dibenzofuran (C12H7NO3, m/z; 213.19 g/mol, m.p.; 181.49 °C). 1H-NMR showed seven signals at δ (ppm) 2.8-4.3 consisting of two doublets and five singlets, while 13C-NMR revealed twelve carbons, which are majorly methyl carbons at δ (ppm) between 120 and 195. All tested samples demonstrated dose-dependent anti-inflammatory activity in carrageenan-induced mice. The isolated compound, i.e. solanine, and chitosan-loaded drugs showed significant inhibitory activity on the cell lines with inhibitory concentration 50 (IC50) values of 8.52, 0.82, and 22.1 μg/mL, respectively on MCF-7 cell line and 4.54, 0.08, and 12.1 μg/mL, respectively, on HMVII cell line, while doxorubicin (adriamycin) positive control, had IC50 values of 0.02 and 0.06 μg/mL, respectively, on MCF-7 and HMVII cancer cells. Selectivity index of solanine was the lowest in the study, hence, it lacks the ability to differentiate between cancerous and normal cell Vero E6 cell lines. Chitosan-loaded drugs quicken early apoptosis and sustained late apoptosis in cells with much improved selective indices.

Conclusion: The results obtained from this study further affirmed the use of chitosan nanoparticles as carriers for anticancer drugs.

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