Introduction: Plant extracts are used to treat illnesses, promote health, and maintain general well-being in traditional medicine. Grewia mollis 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.
Materials and Methods: Dried leaf of G. mollis 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.
Results: The n-hexane fraction of G. mollis leaf extracts had significant activity against both COX-1 (IC₅₀ =0.97± 1.9 μg/mL) and COX-2 (IC₅₀ =1.13± 0.2 μg/mL) better than the indomethacin positive control (IC₅₀ =1.3± 0.6 and 1.52± 0.2 μg/mL), respectively (p≤ 0.05). Also, all the extracts and fractions of G. mollis tested inhibited the activity of 15-LOX (IC₅₀ =12.48± 2.9 to 29.43± 9.9 μg/mL) better than the quercetin reference control (IC₅₀ =61.82± 5.5 μg/mL), with the butanol fraction demonstrating the best anti-15 LOX action (IC₅₀ =12.48± 2.9 μg/mL). Furthermore, all the extracts and fractions of G. mollis had relatively lower cytotoxicity on vero monkey kidney cells (LD₅₀ =30.56– 479± 0.07 μg/mL) compared to the doxorubicin positive control (LD₅₀ =2.59 μg/mL), but the selectivity index (SI=1.04– 1.89) determination suggested that some of the extracts may contain toxic constituents.
Conclusion: Organic extracts of the leaves of Grewia mollis 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.

Keywords: Grewia mollis, anti-inflammatory, pain, plant extracts, COX, 15-LOX


中文翻译：

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Grewia mollis 叶提取物和馏分在体外显示出对促炎酶的良好抑制活性和较低的细胞毒性

简介：植物提取物在传统医学中用于治疗疾病、促进健康和维持整体健康。Grewia mollis Juss (Malvaceae) 是传统上用于治疗慢性疾病和相关疼痛的药草之一，因为目前使用的抗炎药可能会导致严重的副作用，并且可以探索具有降低细胞毒性的天然化合物来实现治疗目标。
材料与方法：G. mollis干叶用水性和有机溶剂萃取，并使用溶剂-溶剂方法根据极性进行分配。在针对环氧合酶和脂氧合酶的抗炎试验中对提取物进行了测试，并在基于细胞的体外试验中确定了安全性。
结果：毛茛叶提取物的正己烷部分对COX-1（IC ₅₀ =0.97±1.9 μg/mL）和COX-2（IC ₅₀ =1.13±0.2 μg/mL）均具有显着的抑制活性。消炎痛阳性对照 (IC ₅₀ =1.3± 0.6 和 1.52± 0.2 μg/mL)，分别 (p≤ 0.05)。此外，所测试的G. mollis的所有提取物和级分均抑制 15-LOX 的活性 (IC ₅₀=12.48± 2.9 至 29.43± 9.9 μg/mL) 优于槲皮素参考对照 (IC ₅₀ =61.82± 5.5 μg/mL)，丁醇部分表现出最佳的抗 15 LOX 作用 (IC ₅₀ =12.48± 2.9 μg /毫升）。此外，与多柔比星阳性对照 (LD ₅₀ =2.59 μg/ mL) 相比， G. mollis的所有提取物和级分对 vero 猴肾细胞的细胞毒性 (LD ₅₀ =30.56–479± 0.07 μg/mL)相对较低，但选择性指数 (SI=1.04–1.89) 测定表明某些提取物可能含有有毒成分。结论：小茴香叶的有机提取物
含有对 COX-2 和 15-LOX 有效的生物活性分子。有针对性的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。这允许分离可能导致植物提取物混合物中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，以管理与使用 NSAID 存在问题的慢性炎症相关的疼痛。

关键词： Grewia mollis，抗炎，疼痛，植物提取物，COX，15-LOX