Phytochemical profiling and therapeutic potential of Baliospermum montanum: A promising inhibitor of COX-2/15-LOX enzymes and NO production in LPS-stimulated RAW 264.7 macrophages

IF 1.9 4区 医学 Q3 INTEGRATIVE & COMPLEMENTARY MEDICINE
Anithakumari Aswathy Krishna , Beena Levakumar Abhirami , Abdul Rahim Muhammed Jasim , Sulochana Priya , Alaganandam Kumaran
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引用次数: 0

Abstract

Introduction

Baliospermum montanum (BM) is traditionally used to treat various ailments such as inflammation, rheumatoid arthritis, pain, etc. The root part of BM is well documented for its anti-inflammatory activity. However, the present study evaluates the multitargeted anti-inflammatory activity of the less explored BM leaf part. This is the first study investigating the COX-2, 15-LOX dual inhibiting potential and NO production inhibition of BM leaf extracts, fractions and compounds.

Methods

The BM leaf's water, ethanol, and hydroethanolic extracts were evaluated for anti-inflammatory activity by assessing the inhibition of COX-2, 15-LOX, and NO production. Additionally, the antioxidant potential of the extracts was determined through DPPH, ABTS, and FRAP assays. The most active ethanol extract was fractionated into 12 fractions and tested for anti-inflammatory, antioxidant, phenol and flavonoid content. Compounds were isolated from the most active fractions and identified using NMR techniques. The isolated compounds were checked for their anti-inflammatory activity. In addition, HPLC analysis of ethanol extract, fractions, and isolated compounds was carried out.

Results

The ethanol extract exhibited higher inhibition of COX-2, 15-LOX enzymes and NO production (IC50 35.75 ± 1.95 μg/mL) in LPS-treated RAW 264.7 cells. It also showed higher antioxidant activity. Following the fractionation of the ethanol extract using different solvents, only the ethyl acetate fractions demonstrated inhibition of COX-2, 15-LOX enzymes, and NO production. The ethyl acetate and acetone fractions are excellent sources of antioxidants, phenolic and flavonoid compounds. An effort to find the active principles from these ethyl acetate fractions resulted in the isolation and identification of four potent anti-inflammatory agents, namely, (-)-epiafzelechin, afzelechin-(4α→8)-afzelechin, afzelechin-(4α→8)-epiafzelechin and β-sitosterol-d-glycoside. The first three compounds were reported for the first time from this plant and afzelechin-(4α→8)-afzelechin was found to be a potent inhibitor of the COX-2/15 LOX enzyme as well as NO production (IC50 = 5.9 ± 1.09 µM).

Conclusion

Based on these findings, we conclude that ethanol extract, fractions, and isolated compounds exert anti-inflammatory activity through multiple therapeutic mechanisms. The present study scientifically supports the traditional use of plant BM for treating inflammation and other related disorders.

万年青的植物化学成分分析和治疗潜力:LPS 刺激的 RAW 264.7 巨噬细胞中 COX-2/15-LOX 酶和 NO 生成的有效抑制剂
导言孟加拉草(Baliospermum montanum,BM)传统上用于治疗各种疾病,如炎症、类风湿性关节炎、疼痛等。文冠果的根部具有抗炎活性,这一点已得到充分证明。然而,本研究评估了探索较少的 BM 叶部分的多靶点抗炎活性。这是首次研究 BM 叶提取物、馏分和化合物的 COX-2、15-LOX 双重抑制潜力和 NO 生成抑制作用。此外,还通过 DPPH、ABTS 和 FRAP 试验测定了提取物的抗氧化潜力。最有活性的乙醇提取物被分成 12 个馏分,并进行了抗炎、抗氧化、酚和类黄酮含量测试。从最具活性的馏分中分离出化合物,并使用核磁共振技术进行鉴定。对分离出的化合物进行了抗炎活性检测。结果乙醇提取物对 LPS 处理的 RAW 264.7 细胞中 COX-2、15-LOX 酶和 NO 的产生有较高的抑制作用(IC50 35.75 ± 1.95 μg/mL)。它还显示出较高的抗氧化活性。使用不同溶剂对乙醇提取物进行分馏后,只有乙酸乙酯馏分显示出对 COX-2、15-LOX 酶和 NO 生成的抑制作用。乙酸乙酯和丙酮馏分是抗氧化剂、酚类和类黄酮化合物的极佳来源。为了从这些乙酸乙酯馏分中找到活性成分,我们分离并鉴定了四种强效抗炎剂,即 (-)-epiafzelechin 、afzelechin-(4α→8)-afzelechin 、afzelechin-(4α→8)-epiafzelechin 和 β-谷甾醇-d-糖苷。前三种化合物是首次从该植物中发现的,而阿夫儿茶素-(4α→8)-阿夫儿茶素是 COX-2/15 LOX 酶和 NO 生成的强效抑制剂(IC50 = 5.9 ± 1.09 µM)。本研究为传统上使用植物 BM 治疗炎症和其他相关疾病提供了科学依据。
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来源期刊
European Journal of Integrative Medicine
European Journal of Integrative Medicine INTEGRATIVE & COMPLEMENTARY MEDICINE-
CiteScore
4.70
自引率
4.00%
发文量
102
审稿时长
33 days
期刊介绍: The European Journal of Integrative Medicine (EuJIM) considers manuscripts from a wide range of complementary and integrative health care disciplines, with a particular focus on whole systems approaches, public health, self management and traditional medical systems. The journal strives to connect conventional medicine and evidence based complementary medicine. We encourage submissions reporting research with relevance for integrative clinical practice and interprofessional education. EuJIM aims to be of interest to both conventional and integrative audiences, including healthcare practitioners, researchers, health care organisations, educationalists, and all those who seek objective and critical information on integrative medicine. To achieve this aim EuJIM provides an innovative international and interdisciplinary platform linking researchers and clinicians. The journal focuses primarily on original research articles including systematic reviews, randomized controlled trials, other clinical studies, qualitative, observational and epidemiological studies. In addition we welcome short reviews, opinion articles and contributions relating to health services and policy, health economics and psychology.
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