Pharmacological Activity of Sea Buckthorn Leaves: In silico and In vivo

N. A. Kovaleva, O. V. Trineeva, A. V. Buzlama, A. Y. Kuznetsov
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Abstract

Introduction. Sea buckthorn leaves are a promising object for the development of new medicinal herbal preparations due to an extensive list of biologically active substances (tannins, flavonoids, organic acids, etc.). However, despite the active study of biologically active substances of buckthorn buckthorn leaves, their use in medicine is limited to obtaining an antiviral drug "Hyporamine" containing a dry purified extract from the leaves of this plant.Aim. The aim of the work is to predict the pharmacological and toxic effects of decoction from buckthorn leaves in silico and to evaluate its anti-inflammatory activity in vivo in preclinical studies.Materials and methods. With the help of the PASS-online Internet resource, the prediction of promising pharmacological and possible toxic effects for the main biologically active substances of the phenolic complex of sea buckthorn leaves in silico was carried out. In preclinical studies in vivo (white outbred conventional male rats, 21 individuals, 210–240 g, 3 groups of 7 individuals each) on a model of formalin paw edema of rats (3.0 % aqueous formalin solution, 0.1 ml subplantarly), the anti-inflammatory activity of decoction of sea buckthorn leaves was evaluated. Animals of the experimental groups were administered: a comparison drug – an infusion of chamomile flowers or a decoction of sea buckthorn leaves at a dose of 10 ml/kg intragastrically daily for 7 days.Results and discussion. The analysis and systematization of data on the most likely pharmacological effects of the main biologically active substances of sea buckthorn leaves in silico using the PASS-online platform allow us to consider the most promising study of anti-inflammatory, hepatoprotective, cardioprotective, antibacterial, antifungal and antiviral activity, which opens up prospects for further preclinical and clinical studies in order to expand the list of indications for the use of extracts from the leaves of sea buckthorn. The prediction of the toxic effects of the main biologically active substances of sea buckthorn leaves showed that the smallest number of probable toxic effects is predicted for narcissin and quercetin, the largest for the substance strictinin I (including neurotoxicity, hematotoxicity, negative effects on the cardiovascular system, gastrointestinal toxicity, reproductive toxicity and carcinogenicity), which requires confirmations in preclinical toxicological studies. In preclinical studies in vivo on a model of rat paw edema, it was proved that a decoction of sea buckthorn leaves with a short-term oral course application of 7 days at a dose of 10 ml/kg (235 mg/kg based on the dry residue), it shows a sufficient anti-inflammatory effect, providing a significant, reliable decrease in the severity of rat paw edema, maximum 3 hours after phlogogen administration by 36.0 % compared with the control, which exceeds the effectiveness of the comparison drug (infusion of chamomile flowers).Conclusion. The main types of pharmacological activity (anti-inflammatory, hepatoprotective, cardioprotective, antibacterial, antifungal and antiviral) and toxic effects (neurotoxicity, hematotoxicity, negative effect on cardiovascular activity and gastrointestinal tract) have been established. Pronounced anti-inflammatory activity was reliably detected.
沙棘叶的体内和体外药理活性
介绍。沙棘叶中含有丰富的生物活性物质(单宁、黄酮类化合物、有机酸等),是开发新型中药制剂的理想对象。然而,尽管对沙棘叶的生物活性物质进行了积极的研究,但其在医学上的应用仅限于从这种植物的叶子中获得一种含有干燥纯化提取物的抗病毒药物“羟波拉明”。本研究的目的是在临床前研究中预测沙棘叶煎剂的药理和毒性作用,并评价其体内抗炎活性。材料和方法。借助PASS-online Internet资源,对沙棘叶酚类复合物的主要生物活性物质进行了有前景的药理学和可能的毒性预测。临床前研究(纯种白色常规雄性大鼠,21只,210 ~ 240 g, 3组,每组7只)建立大鼠福尔马林足跖水肿模型(3.0%福尔马林水溶液,足底0.1 ml),评价沙棘叶煎剂的抗炎作用。实验组动物分别给予对照药洋甘菊注射液或沙棘叶煎剂,剂量为10 ml/kg,每日灌胃,连用7天。结果和讨论。利用PASS-online平台对沙棘叶主要生物活性物质最可能的药理作用进行数据分析和系统整理,使我们能够考虑抗炎、保肝、保心、抗菌、抗真菌和抗病毒活性等最有前景的研究。这为进一步的临床前和临床研究开辟了前景,以扩大沙棘叶提取物的适应症。对沙棘叶主要生物活性物质的毒性作用预测表明,水仙桃素和槲皮素的可能毒性作用预测数量最少,而对沙棘素I的可能毒性作用预测数量最多(包括神经毒性、血液毒性、对心血管系统的负面影响、胃肠道毒性、生殖毒性和致癌性),这需要在临床前毒理学研究中加以证实。在大鼠足部水肿模型的体内临床前研究中,证明沙棘叶煎剂短期口服7天,剂量为10 ml/kg(根据干残量为235 mg/kg),具有足够的抗炎作用,在给药后最大3小时,与对照组相比,显著、可靠地减轻了大鼠足部水肿的严重程度,减少幅度为36.0%。超过对照药物(洋甘菊冲剂)的有效性。主要的药理作用类型(抗炎、保肝、保心、抗菌、抗真菌和抗病毒)和毒性作用(神经毒性、血液毒性、对心血管活动和胃肠道的负面影响)已经确定。明显的抗炎活性可靠地检测到。
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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