Lupeol: A Triterpenoid Isolated from the Stem Bark of Hymenocardia Acida (tul.) Exhibits a van der Waal Antagonism on the Alpha Subunit of Gastric H+K+Atpase - A Promising Antiulcer Principle.

IF 1.7 Q3 PHARMACOLOGY & PHARMACY

Drug Research Pub Date : 2023-10-01 Epub Date: 2023-08-25 DOI:10.1055/a-2132-6475

Adedokun Oluwasegun, Ume Ogochukwu, Ojukwu Ugochukwu, Ismail Mussaddiq, Ayinde Bunyamin

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Abstract

Background: Hymenocardia acida (HA) is one of the numerous medicinal plants in Nigeria with ethnomedicinal history of usage in the treatment of ulcer. The study aimed at isolating antiulcer principle(s) from the stem bark of HA as well as the mechanism of action determination.

Methods: Antiulcer screenings of the crude extract, aqueous fraction, and bulked VLC fractions were performed using in vivo and in vitro models. Docking was carried out by using PyRx.

Results: Crude extract (HA; 1 mg/mL) and the aqueous fraction of H. acida (HAA; 1 mg/mL) showed an acid neutralizing capacity (MEq) of 0.3948 and 0.4035, respectively which is significantly different from 0.431 MEq showed by negative control (distilled water) at p<0.05. BVLC 3 (1 mg/mL) showed a significant value of 0.4049 MEq. However, HA showed a dose-dependent decrease in activity across doses examined, with 100 mg/kg showing an ulcer index of 10.00±2.89 (61.50%) and cimetidine (positive control; 100 mg/kg), also showed the highest ulcer index of 3.67±0.88 (85.9%), which is significantly different from ulcer index of 26.00±6.35 (0.00%) p<0.05 observed in the negative control (5% dimethylsulphoxide). The highest ulcer index of 8.00±1.32 (65.10%) was noted in BVLC 3. Bioactive BVLC 3, resulted in an isolated compound (BF3B2A). The compound was suggested to be lupeol, with a docking score of -7.7. It showed a van der Waal interaction with some key amino acid residues in the vonoprazan binding site.

Conclusion: The experimental studies justify the ethnomedicinal claim of usage among locals.

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Lupeol：一种从膜翅目（tul.）茎皮中分离的三萜类化合物，对胃H+K+Atpase的α亚基表现出范德华拮抗作用，这是一种有前景的抗溃疡原理。

背景：膜壳菌酸（HA）是尼日利亚众多的药用植物之一，有治疗溃疡的民族医药史。本研究旨在从HA茎皮中分离出抗溃疡的原理，并测定其作用机制。方法：使用体内和体外模型对粗提取物、水性组分和膨胀VLC组分进行抗溃疡筛选。使用PyRx进行对接。结果：粗提物（HA；1 mg/mL）和H.acida的水性部分（HAA；1 mg/mL）显示的酸中和能力（MEq）分别为0.3948和0.4035，与阴性对照（蒸馏水）在pps时显示的0.431MEq显著不同。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Drug Research PHARMACOLOGY & PHARMACY-

CiteScore

3.50

自引率

0.00%

发文量

期刊介绍： Drug Research (formerly Arzneimittelforschung) is an international peer-reviewed journal with expedited processing times presenting the very latest research results related to novel and established drug molecules and the evaluation of new drug development. A key focus of the publication is translational medicine and the application of biological discoveries in the development of drugs for use in the clinical environment. Articles and experimental data from across the field of drug research address not only the issue of drug discovery, but also the mathematical and statistical methods for evaluating results from industrial investigations and clinical trials. Publishing twelve times a year, Drug Research includes original research articles as well as reviews, commentaries and short communications in the following areas: analytics applied to clinical trials chemistry and biochemistry clinical and experimental pharmacology drug interactions efficacy testing pharmacodynamics pharmacokinetics teratology toxicology.