Phytochemical analysis of leaf extract of Piper nigrum and investigation of its biological activities.

IF 4.6 2区 医学 Q2 IMMUNOLOGY
Inflammopharmacology Pub Date : 2025-06-01 Epub Date: 2025-04-18 DOI:10.1007/s10787-025-01701-5
Pankaj Barman, Srija Hazarika, Kallol Roy, Ravindra K Rawal, Rituraj Konwar
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引用次数: 0

Abstract

Background: This study investigates the phytoconstituents of the less explored leaf of Piper nigrum, a common ethnomedicinal plant as an alternate source for multiple bioactivities.

Methods: Hydro-ethanolic (1:4) extract of Piper nigrum leaves (PNLE) prepared and profiled using liquid chromatography and mass spectrometry for identification of phytomolecules. Anti-oxidant activity, intracellular reactive oxygen species (ROS) expression, phagocytosis activity, and cytokine expression were estimated using cell-free and cell-based assays. Anti-cancer activity was determined with cancer cell viability, migration inhibition and colony-formation assay. Apoptosis and membrane depolarization assay were done using fluorescent microscopic staining methods while network pharmacology, and molecular docking analysis were done using open source and online tools.

Results: Major phytomolecules identified in PNLE were pentanamide N,N-didecyl, piperettine, curcumin, myristicin, pipernonaline, sesamin, and lupenone. PNLE exhibited anti-bacterial activity with higher activity against Gram-positive bacteria, Staphylococcus aureus. PNLE also showed anti-oxidant and anti-inflammatory activity through neutralization of free radicals; inhibition of intracellular ROS generation; inhibition of phagocytosis and reduction of cytokine (IL-6 and TNF-α) levels. PNLE showed anti-proliferative activity against human breast cancer cells (MDA-MB-231), rat mammary tumor cells (LA7), and mouse melanoma cells (B16-F10) with highest activity against MDA-MB-231 cells. The extract did not inhibit human kidney cells (HEK-293). Further, PNLE treatment significantly inhibited cell migration and colony formation of MDA-MB-231 cells. Fluorescent staining techniques confirmed induction of apoptosis in cancer cells by PNLE. Further, network pharmacology and molecular docking studies revealed that the identified PNLE phytomolecules share 97 targets of out of potential breast cancer and inflammation-related target genes with four best common target proteins among the top hub genes and sesamin showed the highest binding affinity with these important cellular targets.

Conclusions: Overall, the phytochemical profile of PNLE showed clear presence of important phytomolecules and their association with critical human cellular mechanistic pathways responsible for exhibited bioactivities. This study further establishes the leaf of P. nigrum as an additional anatomical plant part with potent medicinal properties and  as a potential renewable source for bioactive phyomolecules.

胡椒叶提取物的植物化学分析及其生物活性研究。
背景:本研究研究了胡椒叶的植物成分,胡椒是一种常见的民族药用植物,作为多种生物活性的替代来源。方法:制备红椒叶(PNLE)水乙醇(1:4)提取物,采用液相色谱和质谱法对其植物分子进行鉴定。抗氧化活性、细胞内活性氧(ROS)表达、吞噬活性和细胞因子表达通过无细胞和基于细胞的测定来估计。通过癌细胞活力、迁移抑制和集落形成实验测定其抗癌活性。细胞凋亡和膜去极化实验采用荧光显微染色法,网络药理学和分子对接分析采用开源和在线工具。结果:鉴定出的主要植物分子为戊酰胺N、N-二癸基、胡椒碱、姜黄素、肉豆蔻素、胡椒碱、芝麻素、豆烯酮。PNLE对革兰氏阳性菌金黄色葡萄球菌具有较高的抑菌活性。PNLE还通过中和自由基表现出抗氧化和抗炎活性;抑制细胞内ROS生成;抑制吞噬和降低细胞因子(IL-6和TNF-α)水平。PNLE对人乳腺癌细胞(MDA-MB-231)、大鼠乳腺肿瘤细胞(LA7)和小鼠黑色素瘤细胞(B16-F10)均有抑制增殖活性,其中对MDA-MB-231细胞的抑制活性最高。提取物对人肾细胞(HEK-293)无抑制作用。此外,PNLE处理显著抑制MDA-MB-231细胞的细胞迁移和集落形成。荧光染色技术证实PNLE诱导癌细胞凋亡。此外,网络药理学和分子对接研究表明,鉴定的PNLE植物分子在潜在的乳腺癌和炎症相关靶基因中共有97个靶点,在顶部枢纽基因中有4个最佳共同靶点蛋白,芝麻素与这些重要细胞靶点的结合亲和力最高。结论:总的来说,PNLE的植物化学特征显示了重要的植物分子的存在,以及它们与人类细胞机制通路的关联,这些通路负责表现出生物活性。本研究进一步确定了黑桫桫树的叶片作为一种额外的解剖植物部分,具有强大的药用特性和潜在的生物活性植物分子的可再生来源。
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
Inflammopharmacology
Inflammopharmacology IMMUNOLOGYTOXICOLOGY-TOXICOLOGY
CiteScore
8.00
自引率
3.40%
发文量
200
期刊介绍: Inflammopharmacology is the official publication of the Gastrointestinal Section of the International Union of Basic and Clinical Pharmacology (IUPHAR) and the Hungarian Experimental and Clinical Pharmacology Society (HECPS). Inflammopharmacology publishes papers on all aspects of inflammation and its pharmacological control emphasizing comparisons of (a) different inflammatory states, and (b) the actions, therapeutic efficacy and safety of drugs employed in the treatment of inflammatory conditions. The comparative aspects of the types of inflammatory conditions include gastrointestinal disease (e.g. ulcerative colitis, Crohn''s disease), parasitic diseases, toxicological manifestations of the effects of drugs and environmental agents, arthritic conditions, and inflammatory effects of injury or aging on skeletal muscle. The journal has seven main interest areas: -Drug-Disease Interactions - Conditional Pharmacology - i.e. where the condition (disease or stress state) influences the therapeutic response and side (adverse) effects from anti-inflammatory drugs. Mechanisms of drug-disease and drug disease interactions and the role of different stress states -Rheumatology - particular emphasis on methods of measurement of clinical response effects of new agents, adverse effects from anti-rheumatic drugs -Gastroenterology - with particular emphasis on animal and human models, mechanisms of mucosal inflammation and ulceration and effects of novel and established anti-ulcer, anti-inflammatory agents, or antiparasitic agents -Neuro-Inflammation and Pain - model systems, pharmacology of new analgesic agents and mechanisms of neuro-inflammation and pain -Novel drugs, natural products and nutraceuticals - and their effects on inflammatory processes, especially where there are indications of novel modes action compared with conventional drugs e.g. NSAIDs -Muscle-immune interactions during inflammation [...]
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