Adamu Isa I, Adebayo Salmon A, Al-Shahrani Mohammad S
Physiology Unit Department of Basic Medical Sciences, College of Medicine, University of Bisha, Bisha, 61922, Saudi Arabia.
Department of Human Physiology, Faculty of Medicine, Ahmadu Bello University, Zaria, Nigeria.
J Inflamm Res. 2020 Oct 23;13:765-772. doi: 10.2147/JIR.S271254. eCollection 2020.
Plant extracts are used to treat illnesses, promote health, and maintain general well-being in traditional medicine. Juss (Malvaceae) is one of the medicinal herbs that is used traditionally to treat chronic diseases and related pain because currently used anti-inflammatory drugs may cause severe side effects, and naturally occurring compounds with reduced cytotoxicity could be explored for therapeutic goals.
Dried leaf of was extracted with aqueous and organic solvents and partitioned based on polarity using solvent-solvent methods. The extracts were tested in anti-inflammatory assays against cyclooxygenases and lipoxygenase, and the safety profile was determined in a cell-based in-vitro assay.
The -hexane fraction of leaf extracts had significant activity against both COX-1 (IC =0.97±1.9 µg/mL) and COX-2 (IC =1.13±0.2 µg/mL) better than the indomethacin positive control (IC =1.3±0.6 and 1.52±0.2 µg/mL), respectively (p≤ 0.05). Also, all the extracts and fractions of tested inhibited the activity of 15-LOX (IC =12.48±2.9 to 29.43±9.9 µg/mL) better than the quercetin reference control (IC =61.82±5.5 µg/mL), with the butanol fraction demonstrating the best anti-15 LOX action (IC =12.48±2.9 µg/mL). Furthermore, all the extracts and fractions of had relatively lower cytotoxicity on vero monkey kidney cells (LD =30.56-479±0.07 µg/mL) compared to the doxorubicin positive control (LD =2.59 µg/mL), but the selectivity index (SI=1.04-1.89) determination suggested that some of the extracts may contain toxic constituents.
Organic extracts of the leaves of contained bioactive molecules with potent action on COX-2 and 15-LOX. Targeted high-resolution high-performance liquid chromatographic (HPLC) methods have streamlined and enhanced bioactive compound isolation and purification process. This allows for the separation of undesirable compounds that could cause metabolic cytotoxicity in the plant extract mixtures. The method could be used to develop an alternative therapeutic strategy to manage pain associated with chronic inflammation where the use of NSAID is problematic.
在传统医学中，植物提取物用于治疗疾病、促进健康和维持总体健康状况。朱槿（锦葵科）是传统上用于治疗慢性病及相关疼痛的草药之一，因为目前使用的抗炎药物可能会引起严重的副作用，而具有较低细胞毒性的天然化合物可用于治疗目的的探索。
用含水和有机溶剂提取朱槿的干燥叶片，并采用溶剂 - 溶剂法根据极性进行分离。对提取物进行抗环氧化酶和脂氧化酶的抗炎测定，并在基于细胞的体外测定中确定其安全性。
朱槿叶提取物的正己烷馏分对COX - 1（IC = 0.97±1.9μg/mL）和COX - 2（IC = 1.13±0.2μg/mL）均具有显著活性，分别优于吲哚美辛阳性对照（IC = 1.3±0.6和1.52±0.2μg/mL）（p≤0.05）。此外，所测试的朱槿的所有提取物和馏分对15 - LOX活性的抑制作用（IC = 12.48±2.9至29.43±9.9μg/mL）均优于槲皮素参考对照（IC = 61.82±5.5μg/mL），其中丁醇馏分表现出最佳的抗15 - LOX作用（IC = 12.48±2.9μg/mL）。此外，与阿霉素阳性对照（LD = 2.59μg/mL）相比，朱槿的所有提取物和馏分对非洲绿猴肾细胞的细胞毒性相对较低（LD = 30.56 - 479±0.07μg/mL），但选择性指数（SI = 1.04 - 1.89）的测定表明某些提取物可能含有有毒成分。
朱槿叶的有机提取物含有对COX - 2和15 - LOX具有强效作用的生物活性分子。靶向高分辨率高效液相色谱（HPLC）方法简化并增强了生物活性化合物的分离和纯化过程。这使得能够分离植物提取物混合物中可能导致代谢细胞毒性的不良化合物。该方法可用于开发一种替代治疗策略，以管理与慢性炎症相关的疼痛，在这种情况下使用非甾体抗炎药存在问题。
