Phytochemical Research Laboratory, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Dhaka, Dhaka 1000, Bangladesh.
Department Pharmacy, University of Asia Pacific, Dhaka 1205, Bangladesh.
Molecules. 2022 Jun 22;27(13):4024. doi: 10.3390/molecules27134024.
The aim of the study was to conduct phytochemical and pharmacological investigations of Wrightia coccinea (Roxb. ex Hornem.) Sims via several in vitro, in vivo, and in silico models. A total of four compounds were identified and isolated from the methanol extract of the bark and the methanol extract of the seed pulp of W. coccinea through successive chromatographic techniques and were characterized as 3β-acetyloxy-olean-12-en-28-ol (1), wrightiadione (2), 22β-hydroxylupeol (3), and β-sitosterol (4) by spectroscopic analysis. The aqueous fraction of the bark and chloroform fraction of the fruits provided the most potent antioxidant capacity (IC50 = 7.22 and 4.5 µg/mL, respectively) in DPPH free radical scavenging assay compared with the standard ascorbic acid (IC50 = 17.45 µg/mL). The methanol bark extract and the methanol fruit coat extract exerted anti-diarrheal activity by inhibiting 74.55 ± 0.67% and 77.78 ± 1.5% (mean ± SEM) of the diarrheal episode in mice, respectively, after four hours of loading the samples. In the hypoglycemic test, the methanol bark extract and the methanol fruit coat extract (400 mg/kg) produced a significant (p < 0.05) reduction in the blood glucose level in mice. Both doses of the plant extracts (200 mg/kg and 400 mg/kg) used in the study induced a significant (p < 0.05) increase in pain reaction time. The in vitro and in vivo findings were supported by the computational studies. The isolated compounds exhibited higher binding affinity compared with the standard drugs towards the active binding sites of glutathione reductase, epidermal growth factor receptor (EGFR), kappa opioid receptor, glucose transporter 3 (GLUT 3), Mu opioid receptor, and cyclooxygenase 2 (COX-2) proteins due to their potent antioxidant, cytotoxic, anti-diarrheal, hypoglycemic, and central and peripheral analgesic properties, respectively. The current findings concluded that W. coccinea might be a potential natural source for managing oxidative stress, diarrhea, hyperglycemia, and pain. Further studies are warranted for extensively phytochemical screening and establishing exact mechanisms of action.
本研究旨在通过多种体外、体内和计算模型对 Wrightia coccinea (Roxb. ex Hornem.) Sims 进行植物化学和药理学研究。通过连续的色谱技术，从 Wrightia coccinea 的树皮甲醇提取物和种子浆甲醇提取物中鉴定并分离出四种化合物，并通过光谱分析鉴定为 3β-乙酰氧基-齐墩果-12-烯-28-醇（1）、wrightiadione（2）、22β-羟基羽扇豆醇（3）和 β-谷甾醇（4）。与标准抗坏血酸（IC50 = 17.45 µg/mL）相比，树皮的水提部分和果实的氯仿部分在 DPPH 自由基清除测定中提供了最强的抗氧化能力（IC50 = 7.22 和 4.5 µg/mL）。甲醇树皮提取物和甲醇果实外皮提取物在 4 小时后分别抑制了 74.55 ± 0.67%和 77.78 ± 1.5%（平均值 ± SEM）的腹泻发作，表现出抗腹泻活性。在降血糖试验中，甲醇树皮提取物和甲醇果实外皮提取物（400 mg/kg）使小鼠的血糖水平显著降低（p < 0.05）。研究中使用的两种植物提取物（200 mg/kg 和 400 mg/kg）均能显著（p < 0.05）增加疼痛反应时间。体外和体内发现得到了计算研究的支持。与标准药物相比，分离出的化合物对谷胱甘肽还原酶、表皮生长因子受体（EGFR）、κ 阿片受体、葡萄糖转运蛋白 3（GLUT 3）、μ 阿片受体和环加氧酶 2（COX-2）蛋白的活性结合部位表现出更高的结合亲和力，这是由于它们具有抗氧化、细胞毒性、抗腹泻、降血糖以及中枢和外周镇痛作用。目前的研究结果表明，Wrightia coccinea 可能是一种管理氧化应激、腹泻、高血糖和疼痛的潜在天然来源。需要进一步研究以广泛进行植物化学筛选并确定确切的作用机制。
