地奥司明：从酢浆草科植物三叶草中分离纯化得到的一种矛头蝮蛇毒 PLAs 抑制剂，并对其进行了表征。

Diosmin: A Daboia russelii venom PLAs inhibitor- purified, and characterized from Oxalis corniculata L medicinal plant.

机构信息

Division of Biochemistry, School of Life Science, JSS Academy of Higher Education and Research, Mysore-15, India.

Department of Biochemistry, Adichunchanagiri Institute of Medical Sciences, Adichunchanagiri University, B. G. Nagara- 571448, Nagamangala (T), Mandya (D), Karnataka, India; Department of Biotechnology, Adichunchanagiri School of Natural Sciences, ACU-CRI, Adichunchanagiri University, B. G. Nagara- 571448, Nagamangala (T), Mandya (D), Karnataka, India.

出版信息

J Ethnopharmacol. 2024 Jan 10;318(Pt B):116977. doi: 10.1016/j.jep.2023.116977. Epub 2023 Aug 5.

DOI:10.1016/j.jep.2023.116977

PMID:37544341

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Oxalis corniculata L is a medicinal plant that belongs to the Oxalidaceae family. It is a little, slow-growing plant with a frail appearance typically found in mild temperate and tropical areas like Pakistan and India. This plant also includes many other bioactive substances, including alkaloids, flavonoids, terpenoids, cardiac glycosides, saponins, phlobatannins, and steroids.

AIM OF THE STUDY

To investigate the anti-inflammatory effects of Compound diosmin, which is derived from Oxalis corniculata L, on VRV-PL-5 and VRV-PL-8a isolated from Vipera russelli.

MATERIALS AND METHODS

Extraction, purification, and characterization of bioactive by TLC, HPTLC, FT-IR analysis, UV-Vis spectrophotometer, LC-MS/MS Analysis, NMR, XRD Analysis, In vitro evaluation, Circular dichroism spectroscopy, in vivo, and in silico studies.

RESULTS

In this study, the extract of Oxalis corniculata was evaluated for its in vitro and in vivo anti-inflammatory effect against PLA. The methanolic extract decreased hemolytic activity by about 60% at 1:75 w/w and neutralized the hemolytic activity completely at 1:100 w/w concentration. Diosmin inhibited VRV-PL-5 and VRV-PL-8a in a dose-dependent manner, with the extent of inhibition being about 56% for VRV-PL-5120 μM and VRV-PL-8a by 62% at the same concentration with IC concentrations of 87.08 μM for VRV-PL-5 and 82.08 μM for VRV-PL-8a, while at 75 μM. Diosmin inhibited the hemolytic activity of VRV-PL-5 by about 85%, and at the same concentration, VRV-PL-8a inhibited by about 75%. UV-CD spectra at the IC concentration of diosmin disrupted the secondary structure of VRV-PL-5 &VRV-PL-8a. In vivo, studies showed decreased myotoxicity and cardiotoxicity of the VRV-PL-5 &VRV-PL-8a, which was seen in the decrease in cytoplasmic markers LDH and CPK levels in the serum when incubated with diosmin. Furthermore, Histopathological studies of Muscles and lungs revealed that diosmin considerably protects against cellular abnormality caused by VRV-PL-5 & VRV-PL-8a. Molecular docking, MM/GBSA, and molecular dynamics simulation studies show that the diosmin is a potent inhibitor for VRV-PL-5 and VRV-PL-8a.

CONCLUSION

This study shows that diosmin is a potentially effective VRV-PL-5 and VRV-PL-8a.

摘要

民族药理学相关性

Oxalis corniculata L 是一种属于 Oxalidaceae 科的药用植物。它是一种生长缓慢的小型植物，外观脆弱，通常生长在温和的温带和热带地区，如巴基斯坦和印度。这种植物还包含许多其他生物活性物质，包括生物碱、类黄酮、萜类化合物、强心苷、皂苷、鞣花单宁和类固醇。

研究目的

研究来源于 Oxalis corniculata L 的复方橙皮苷对从 Vipera russelli 分离的 VRV-PL-5 和 VRV-PL-8a 的抗炎作用。

材料和方法

通过 TLC、HPTLC、FT-IR 分析、UV-Vis 分光光度计、LC-MS/MS 分析、NMR、XRD 分析、体外评估、圆二色光谱、体内和计算研究进行生物活性的提取、纯化和表征。

结果

在这项研究中，评估了 Oxalis corniculata 的提取物对 PLA 的体外和体内抗炎作用。在 1:75 w/w 时，甲醇提取物使溶血活性降低约 60%，在 1:100 w/w 浓度时完全中和溶血活性。地奥司明以剂量依赖的方式抑制 VRV-PL-5 和 VRV-PL-8a，在相同浓度下，VRV-PL-5 的抑制程度约为 56%，VRV-PL-8a 的抑制程度约为 62%，IC 浓度分别为 87.08 μM 和 82.08 μM，而在 75 μM 时，地奥司明抑制 VRV-PL-5 的溶血活性约为 85%，在相同浓度下，VRV-PL-8a 的抑制活性约为 75%。在 IC 浓度的地奥司明下，UV-CD 光谱破坏了 VRV-PL-5 和 VRV-PL-8a 的二级结构。在体内研究中，当与地奥司明孵育时，观察到 VRV-PL-5 和 VRV-PL-8a 的细胞毒性和肌毒性降低，血清中细胞质标志物 LDH 和 CPK 水平降低。此外，肌肉和肺部的组织病理学研究表明，地奥司明可显著防止 VRV-PL-5 和 VRV-PL-8a 引起的细胞异常。分子对接、MM/GBSA 和分子动力学模拟研究表明，地奥司明是 VRV-PL-5 和 VRV-PL-8a 的有效抑制剂。