Fermentation alters the bioactive properties of kaempferol derived from horse gram extract

Q3 Pharmacology, Toxicology and Pharmaceutics Phytomedicine Plus Pub Date : 2024-10-03 DOI:10.1016/j.phyplu.2024.100647
Amber Rizwan , Husna Shaikh , Insha Latief , Waseem Ali , Adil Parvez , Kunal Malik , Sonam Grover , Humaira Farooqi
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Abstract

Introduction

This study investigates the therapeutic potential of kaempferol, a metabolite from horse gram seeds, by comparing extracts from non-fermented and fermented sources. Kaempferol is known for its ability to interact with tumour suppressor genes, notably p53, and for its higher binding stability than conventional vinblastine.

Hypothesis

It is hypothesised that kaempferol extracted from fermented horse gram seeds will have superior anti-leukaemic properties compared to kaempferol from non-fermented seeds due to the higher yield and improved stability observed under fermentation conditions.

Methods

The study compared the efficacy of kaempferol from non-fermented and fermented horse gram seeds using different experimental approaches. Affinity to p53 and other target proteins (BAK, BAX), cell viability and apoptosis assays in HL-60 cells, as well as hematologic and histopathology analyses, were performed to evaluate therapeutic efficacy.

Results

Kaempferol, the active compound extracted from horse gram seeds, showed a significantly stronger affinity for tumour suppressor genes (p53) than the standard vinblastine across all target proteins (BAK, BAX). Kaempferol demonstrated greater stability in binding to P53 genes than vinblastine. The yield of kaempferol, the active ingredient of horse gram, increased by more than 50 % under fermentation conditions. Kaempferol curtailed viability and enhanced apoptosis in HL-60 cells more than vinblastine. Kaempferol, obtained from fermented seeds, markedly reduces red and white blood cell levels, such as lymphocytes, neutrophils, monocytes, and myeloblast cells, compared to vinblastine—no alteration in basophils and eosinophils. The histopathological alterations in the liver, spleen, and bone marrow caused by ENU were also reduced by kaempferol extract from horse gram. Kaempferol from fermented seeds was more effective than that obtained under non-fermented conditions.

Conclusion

The findings suggest that kaempferol obtained from fermented horse gram possesses more antileukaemia potential, showing more therapeutic potency than extract obtained from non-fermented horse gram. Studies indicate that fermentation factors influence the production of kaempferol and its therapeutic efficacy.

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发酵改变了从马齿苋提取物中提取的山奈酚的生物活性特性
引言本研究通过比较非发酵来源和发酵来源的提取物,探讨了山奈酚的治疗潜力,山奈酚是从马齿苋种子中提取的一种代谢物。假设由于发酵条件下山奈酚的产量更高且稳定性更好,因此与未发酵的山奈酚相比,从发酵的马齿苋种子中提取的山奈酚具有更优越的抗白血病特性。结果在所有靶蛋白(BAK、BAX)中,从马齿苋种子中提取的活性化合物山奈酚对肿瘤抑制基因(p53)的亲和力明显强于标准的长春新碱。与长春新碱相比,山奈酚与 P53 基因结合的稳定性更高。在发酵条件下,山奈酚(马钱子的活性成分)的产量增加了 50%以上。与长春新碱相比,山奈酚能更有效地抑制 HL-60 细胞的存活率并增强其凋亡。与长春新碱相比,从发酵种子中提取的山奈酚能明显降低红细胞和白细胞的含量,如淋巴细胞、中性粒细胞、单核细胞和骨髓母细胞,但对嗜碱性粒细胞和嗜酸性粒细胞没有影响。从马齿苋中提取的山奈酚也减少了 ENU 对肝脏、脾脏和骨髓造成的组织病理学改变。结论:研究结果表明,从发酵马齿笕中提取的山奈酚具有更强的抗白血病潜力,比从非发酵马齿笕中提取的山奈酚更有疗效。研究表明,发酵因素会影响山奈酚的产生及其治疗效果。
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来源期刊
Phytomedicine Plus
Phytomedicine Plus Medicine-Complementary and Alternative Medicine
CiteScore
3.70
自引率
0.00%
发文量
178
审稿时长
81 days
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