深海牛蒡根提取物次级代谢产物的药代动力学、药物相似性、抗菌抗氧化活性及计算机分子对接研究

Getachew Tegegn, Y. Melaku, Milkyas ENDALE ANNİSA, R. Eswaramoorthy
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引用次数: 1

摘要

深海Crinum Abyssinium和Caltrophis procera传统上用于治疗不同的疾病,如高血压、糖尿病、乙型肝炎、皮肤感染、抗癌、哮喘、发烧和腹泻。通过1H NMR、13C NMR和DEPT-135光谱对化合物的结构进行了表征。化合物1-3在本文中首次报道来自深海C。深海藻DCM/MeOH(1:1)和MeOH根提取物对金黄色葡萄球菌和铜绿假单胞菌表现出显著的抑制活性,平均抑制区分别为16.67±1.20和16.33±0.33mm。化合物4和5对大肠杆菌显示出有希望的活性,平均抑制区为17.7 0.8和17.7 1.2毫米。DPPH活性测定结果表明,深海藻DCM:MeOH(1:1)和MeOH根提取物对DPPH自由基的抑制作用为52.86 0.24%和45.6 0.11%,而化合物5显示出85.7%的抑制作用。药物相似性分析表明,化合物2-4满足Lipinski的五项规则,没有任何违规行为。化合物2和6对大肠杆菌DNA旋转酶B的结合亲和力分别为−6.0和−6.7 kcal/mol,而化合物3和5对人过氧化物酶5的结合亲和力则分别为−5.0和−5.0 kcal/mol。因此,体外抗菌、清除自由基的活性以及分子对接分析表明,深海藻提取物和化合物2、5、6和3、5可分别被认为是有前途的抗菌剂和自由基清除剂。
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Pharmacokinetics, drug-likeness, antibacterial and antioxidant activity of secondary metabolites from the roots extracts of Crinum abyssinicum and Calotropis procera and in silico molecular docking study
Crinum abyssinicum and Calotropis procera were traditionally used for the treatment of different diseases such as hypertension, diabetes, hepatitis B, skin infection, anticancer, asthma, fever, and diarrhea. The structures of the compounds were characterized by 1H NMR, 13C NMR, and DEPT-135 spectra. Compounds 1-3 were reported herein for the first time from the species of C. abyssinicum. The DCM/MeOH (1:1) and MeOH roots extracts of C. abyssinicum showed significant inhibitory activity against S. aureus and P. aeruginosa with a mean inhibition zone of 16.67 ± 1.20 and 16.33 ± 0.33 mm, respectively. Compounds 4 and 5 showed promising activity against E. coli with a mean inhibition zone of 17.7  0.8 and 17.7  1.2 mm, respectively. The results of DPPH activity showed the DCM: MeOH (1:1) and MeOH roots extracts of C. abyssinicum inhibited the DPPH radical by 52.86  0.24 % and 45.6  0.11 %, respectively, whereas compound 5 displayed 85.7 % of inhibition. The drug-likeness analysis showed that compounds 2-4 satisfy Lipinski’s rule of five with zero violations. Compounds 2, and 6 showed binding affinities of −6.0, and −6.7 kcal/mol against E. coli DNA gyrase B, respectively, while 3 and 5 showed −5.0 and −5.0 kcal/mol, respectively against human peroxiredoxin 5. Therefore, the in vitro antibacterial, radical scavenging activity along with the molecular docking analysis suggest the potential use of the extracts of C. abyssinicum and compounds 2, 5, 6, and 3, 5 can be considered as promising antibacterial agents and free radical scavengers, respectively.
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来源期刊
International Journal of Secondary Metabolite
International Journal of Secondary Metabolite Biochemistry, Genetics and Molecular Biology-Biotechnology
CiteScore
1.40
自引率
0.00%
发文量
28
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