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从巴基斯坦土生土长的 Trigonella foenum-graecum L. cv. Desi 的叶子中分离生物碱和糖苷类成分,用于评估抗前列腺素作为非甾体抗炎药的替代品。

Isolation of alkaloidal and glycosidal fractions from leaves of Trigonella foenum-graecum L. cv. Desi indigenous to Pakistan for antiprostaglandin evaluation as substitute of nonsteroidal anti-inflammatory drugs.

机构信息

Department of Pharmacology and Toxicology, University of Veterinary and Animal Sciences, Lahore, 54000, Pakistan.

Department of Pharmacology and Toxicology, University of Veterinary and Animal Sciences, Lahore, 54000, Pakistan.

出版信息

J Ethnopharmacol. 2023 Dec 5;317:116730. doi: 10.1016/j.jep.2023.116730. Epub 2023 Jun 17.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Trigonella foenum graecum (fenugreek) has been in use for a long time as a traditional medicine and natural food additive. The reported gastro-protective property makes it unique among other herbs. Seeds and leaves have been shown to exert significant antiatherogenic, antidiabetic, antianorexic, antioxidant, anticarcinogenic, antihyperlipidemic, galactogogue and anti-inflammatory effects in several animal and human models. But its use as a substitute for ulcerative nonsteroidal anti-inflammatory drugs needs to be confirmed.

AIM OF THE STUDY

Nonsteroidal anti-inflammatory drugs (NSAIDs) are in common use in treating inflammation associated with a variety of ailments, fever and pain such as menstrual cramps, back pain, arthritic pain and headaches. Their toxicity profile includes the risk of severe gastro-intestinal adverse events like increased bleeding tendency, ulceration, perforation, etc. Conventional NSAIDs have also been reported to reduce the glomerular filtration rate (GFR) by affecting afferent arterioles in nephrons. Exacerbated potassium levels were noted in patients using NSAIDs concomitantly with antihypertensive drugs belonging to the angiotensin converting enzyme (ACE) inhibitor or angiotensin receptor blocker (ARB) classes. In this context, the need of the hour is to discover and isolate new compounds from the reported medicinal plants for evaluation of antiprostaglandin potential and safety profile in terms of the hepato-renal system. These compounds may be used as substitutes for NSAIDs in the future management of inflammation and pain with therapeutic equivalency and organ safety. In this scenario, the present study aimed to assess the antiprostaglandin potential of alkaloidal and glycosidal fractions from the leaves of Trigonella foenum-graecum L. cv. Desi variety, indigenous to Pakistan, in albino mice along with safety profile. The herb has been used as folk medicine since ancient times for treating inflammation and pain.

MATERIAL AND METHODS

Alkaloidal and glycosidal fractions were separated from a methanol extract of leaves of the fenugreek Desi variety. After separation of fractions, their subsiding effects on carrageenan-induced inflammation, air pouch exudate prostaglandin-E2 levels, Brewer's yeast induced pyrexia and acetic acid induced abdominal constrictions were assessed in adult male albino mice. The safety profile of fractions was assessed by measuring their effects on mice sera hepato-renal biomarkers.

RESULT

Alkaloidal fraction of T. foenum Desi variety was found to be significantly effective in reducing inflammation, air pouch exudate PGE2 levels, fever (≤37 °C) and pain by inhibiting writhes (up to 96.58%) Gradual inhibition of paw edema was observed 1-6 h post-dose, with maximum reduction percentages of 62.82% and 62.57% for 100 mg and 200 mg, respectively. Both fractions did not disturb the normal physiology of the hepato-renal system by showing normal biomarker values.

CONCLUSION

In summary, the results demonstrate the potent antiprostaglandin potential of the alkaloidal fraction of gastroprotective fenugreek "Desi" leaves with hepato-renal system safety and hence justify its use as a substitute for ulcerative nonsteroidal anti-inflammatory drugs.

摘要

民族药理学相关性

葫芦巴(胡芦巴)作为传统药物和天然食品添加剂已有很长的使用历史。其报道的胃保护特性使它在其他草药中独具特色。种子和叶子已被证明在几种动物和人类模型中具有显著的抗动脉粥样硬化、抗糖尿病、抗厌食、抗氧化、抗癌、抗高血脂、催乳和抗炎作用。但它作为溃疡性非甾体抗炎药替代品的用途仍需进一步证实。

研究目的

非甾体抗炎药(NSAIDs)常用于治疗与多种疾病相关的炎症、发热和疼痛,如痛经、背痛、关节炎疼痛和头痛。它们的毒性谱包括增加出血倾向、溃疡、穿孔等严重胃肠不良反应的风险。常规 NSAIDs 还被报道通过影响肾单位中的入球小动脉来降低肾小球滤过率(GFR)。同时使用 NSAIDs 和属于血管紧张素转换酶(ACE)抑制剂或血管紧张素受体阻滞剂(ARB)类别的降压药的患者血钾水平会升高。在这种情况下,当务之急是从已报道的药用植物中发现和分离新的化合物,以评估其抗前列腺素的潜力和肝肾功能安全性。这些化合物未来可能会替代 NSAIDs 用于炎症和疼痛的治疗,具有治疗等效性和器官安全性。在这种情况下,本研究旨在评估巴基斯坦本土的胡芦巴 Desi 品种叶中的生物碱和糖苷类成分在白化小鼠体内的抗前列腺素潜力及其安全性。这种草药自古以来一直被用作民间药物,用于治疗炎症和疼痛。

材料和方法

从胡芦巴 Desi 品种的甲醇提取物中分离出生物碱和糖苷类成分。分离出各成分后,评估其对角叉菜胶诱导的炎症、气囊渗出液前列腺素 E2 水平、啤酒酵母诱导的发热和醋酸诱导的腹部收缩的抑制作用。通过测量各成分对小鼠血清肝肾功能生物标志物的影响来评估其安全性。

结果

胡芦巴 Desi 品种的生物碱类成分在抑制扭体(最高可达 96.58%)方面表现出显著的抗炎、气囊渗出液 PGE2 水平降低、退热(≤37°C)和止痛作用。在 1-6 小时内逐渐抑制爪肿胀,100mg 和 200mg 剂量的最大减少百分比分别为 62.82%和 62.57%。各成分均未通过显示正常的生物标志物值而干扰肝肾功能的正常生理机能。

结论

综上所述,结果表明,具有胃保护作用的胡芦巴“Desi”叶的生物碱类成分具有较强的抗前列腺素作用,且对肝肾功能安全,因此可以作为溃疡性非甾体抗炎药的替代品。

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