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首次报道从两种植物中分离出的化合物:植物源生物活性代谢产物及其药用潜力。

First-time report on compound isolation from two species: vegetable-derived bioactive metabolites and their medicinal potential.

作者信息

Alam Safaet, Richi Fahmida Tasnim, Emon Nazim Uddin, Chowdhury Abu Asad, Hasan Choudhury Mahmood, Haque Mohammad Rashedul

机构信息

Chemical Research Division, BCSIR Dhaka Laboratories, Bangladesh Council of Scientific and Industrial Research (BCSIR), Dhaka, Bangladesh.

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Dhaka, Dhaka, Bangladesh.

出版信息

Front Pharmacol. 2024 Dec 4;15:1474706. doi: 10.3389/fphar.2024.1474706. eCollection 2024.

DOI:10.3389/fphar.2024.1474706
PMID:39697535
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11652197/
Abstract

BACKGROUND

Schott and Hook.f. are two commonly found vegetable species of the genus , found mainly in the Asian region.

OBJECTIVES

The objective of this study was to isolate bioactive phytochemicals from and and elucidate their structure employing the NMR technique followed by bioactivity evaluation.

METHODOLOGY

Column chromatography was utilized to isolate phytochemicals, followed by NMR analysis for characterization. An analgesic test was performed through an acetic acid-induced writhing test, an anti-inflammatory test was performed through a formalin-induced licking test, and an antidiarrheal test was performed through a castor oil-induced diarrhea model. The antimicrobial test was executed through the disc diffusion method. Computer-aided simulation was also implemented to validate the wet laboratory results.

RESULTS

Six compounds from and were isolated and characterized from the dichloromethane (DCM)-soluble fractions of the methanolic extracts of these two species. Three of the compounds were from and proposed as penduletin , a mixture of α-amyrin , β-amyrin , and monoglyceride of stearic acid while the remaining three compounds were from and proposed as penduletin (which was also isolated from ), 7,8-(3″,3″-dimethyl-pyrano)-4'-hydroxy flavonol , and lastly a mixture of 7,8-(3″,3″-dimethyl-pyrano)-4'-hydroxy flavonol and 4',7,8-trihydroxy flavonol . These compounds showed promising zones of inhibition against Gram-positive and Gram-negative bacteria and fungi. In the antidiarrheal test, demonstrated the highest reduction in castor oil-induced diarrhea (44.44%) at a dose of 20 mg/kg compared to loperamide's 77.78% reduction. However, the analgesic assessment showed a noteworthy inhibition of acetic acid-induced writhing by and (56.52%) at a dose of 20 mg/kg compared to the 76.09% by diclofenac sodium. In comparison, showed pronounced anti-inflammatory action by 68.15% and 52.06% reduction, respectively, in the early and later phases compared to the ibuprofen's outcomes of 73.54% and 74.68%. Plausible targets such as dihydrofolate reductase (DHFR) for antimicrobial, kappa opioid receptor (KOR) for antidiarrheal, and cyclooxygenase 2 (COX-2) for anti-inflammatory and analgesic activities showed a noteworthy binding affinity with isolated compounds, and ADME/T studies displayed these phytochemicals' drug-likeness profiles.

CONCLUSION

To the best of our knowledge, this is the first report on compound isolation from these plants, which demands further extensive research for more absolute findings.

摘要

背景

肖特氏属植物和胡克氏属植物是该属中两种常见的蔬菜物种,主要分布在亚洲地区。

目的

本研究的目的是从肖特氏属植物和胡克氏属植物中分离生物活性植物化学物质,采用核磁共振技术阐明其结构,随后进行生物活性评估。

方法

利用柱色谱法分离植物化学物质,然后通过核磁共振分析进行表征。通过醋酸诱导扭体试验进行镇痛试验,通过福尔马林诱导舔足试验进行抗炎试验,通过蓖麻油诱导腹泻模型进行止泻试验。通过纸片扩散法进行抗菌试验。还实施了计算机辅助模拟以验证湿实验室结果。

结果

从这两个物种甲醇提取物的二氯甲烷(DCM)可溶部分中分离并鉴定出六种来自肖特氏属植物和胡克氏属植物的化合物。其中三种化合物来自肖特氏属植物,被鉴定为penduletin 、α-香树脂醇 、β-香树脂醇 和硬脂酸甘油单酯 的混合物,而其余三种化合物来自胡克氏属植物,被鉴定为penduletin (也从肖特氏属植物中分离得到)、7,8-(3″,3″-二甲基-吡喃)-4'-羟基黄酮醇 ,最后是7,8-(3″,3″-二甲基-吡喃)-4'-羟基黄酮醇 和4',7,8-三羟基黄酮醇 的混合物。这些化合物对革兰氏阳性菌、革兰氏阴性菌和真菌显示出有前景的抑制圈。在止泻试验中,与洛哌丁胺77.78%的止泻率相比,肖特氏属植物提取物在20mg/kg剂量下对蓖麻油诱导的腹泻的止泻率最高(44.44%)。然而,镇痛评估显示,与双氯芬酸钠76.09%的镇痛率相比,肖特氏属植物提取物和胡克氏属植物提取物在20mg/kg剂量下对醋酸诱导扭体的抑制率显著(56.52%)。相比之下,与布洛芬在早期和后期分别为73.54%和74.68%的抗炎效果相比,胡克氏属植物提取物在早期和后期分别显示出68.15%和52.06%的显著抗炎作用。抗菌的可能靶点如二氢叶酸还原酶(DHFR)、止泻的κ阿片受体(KOR)以及抗炎和镇痛活性的环氧合酶2(COX-2)与分离出的化合物显示出显著的结合亲和力,并且ADME/T研究显示了这些植物化学物质的类药性质。

结论

据我们所知,这是关于从这些植物中分离化合物的首次报道,需要进一步广泛研究以获得更确凿的结果。

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