Department of Pharmaceutics and Biopharmaceutics, Philipps-University of Marburg, Marburg, Germany.
Merck KGaA, BU Performance Materials, Darmstadt, Germany.
J Ethnopharmacol. 2021 Apr 24;270:113741. doi: 10.1016/j.jep.2020.113741. Epub 2021 Jan 13.
Waltheria Indica L. is traditionally used in Africa, South America and Hawaii to treat pain, anemia, diarrhea, epilepsy and inflammatory related diseases.
This study aimed to identify extraction parameters to maximize tiliroside yield and to quantitative secondary metabolite composition of Waltheria Indica under various extraction conditions. The extracts were tested for COX-2 inhibition and their activity correlated with the type and quantity of the secondary metabolites. Insight was gained about how extraction parameters influence the extract composition and thus the COX-2 enzymatic inhibitory activity.
Powdered leaves of Waltheria Indica were extracted using water, methanol, ethyl acetate and ethanol at different temperatures. Tiliroside was identified by HPLC-HRMS n and quantified using a tiliroside standard. The compound groups of the secondary metabolites were quantified by spectrometric methods. Inhibitory potential of different Waltheria extracts against the COX-2 enzyme was determined using a fluorometric COX-2 inhibition assay.
The molecule, tiliroside, exhibited a COX-2 inhibition of 10.4% starting at a concentration of 15 μM and increased in a dose dependent manner up to 51.2% at 150 μM. The ethanolic extract at 30 °C and the ethyl acetate extract at 90 °C inhibited COX-2 with 37.7% and 38.9%, while the methanolic and aqueous extract showed a lower inhibition of 21.9% and 9.2% respectively. The results concerning phenol, alkaloid and tiliroside concentration in the extracts showed no dependence on COX-2 inhibition. The extracts demonstrated a direct correlation of COX-2 inhibitory activity with their triterpenoid-/steroidal-saponin concentration. COX-2 inhibition increased linearly with the concentration of the saponins.
The data suggest that Waltheria Indica extracts inhibit the key inflammatory enzyme, COX-2, as a function of triterpenoid- and steroidal-saponin concentration and support the known efficacy of extracted Waltheria Indica leaves as a traditional treatment against inflammation related diseases.
瓦勒西亚因迪卡 L. 在非洲、南美洲和夏威夷被传统用于治疗疼痛、贫血、腹泻、癫痫和炎症相关疾病。
本研究旨在确定提取参数，以最大限度地提高Tiliroside 的产量，并在各种提取条件下定量测定瓦勒西亚因迪卡的次生代谢产物组成。测试提取物对 COX-2 的抑制作用，并将其活性与次生代谢产物的类型和数量相关联。深入了解提取参数如何影响提取物的组成，从而影响 COX-2 酶的抑制活性。
用不同温度的水、甲醇、乙酸乙酯和乙醇提取瓦勒西亚因迪卡的粉末状叶子。通过 HPLC-HRMS n 鉴定Tiliroside，并使用 Tiliroside 标准定量。通过光谱方法定量测定次生代谢产物的化合物组。用荧光 COX-2 抑制测定法测定不同瓦勒西亚提取物对 COX-2 酶的抑制潜力。
该分子 Tiliroside 从 15 μM 的浓度开始对 COX-2 抑制 10.4%，并呈剂量依赖性增加至 150 μM 时的 51.2%。30°C 的乙醇提取物和 90°C 的乙酸乙酯提取物对 COX-2 的抑制率分别为 37.7%和 38.9%，而甲醇和水提取物的抑制率较低，分别为 21.9%和 9.2%。关于提取物中苯酚、生物碱和 Tiliroside 浓度的结果表明，它们与 COX-2 抑制无关。提取物表现出与三萜/甾体皂苷浓度直接相关的 COX-2 抑制活性。COX-2 抑制作用随皂苷浓度的增加呈线性增加。
数据表明，瓦勒西亚因迪卡提取物抑制关键炎症酶 COX-2，其功能与三萜和甾体皂苷浓度有关，并支持已提取的瓦勒西亚因迪卡叶作为传统治疗炎症相关疾病的功效。
