Department of Analytical Chemistry, Faculty of Pharmacy, Bezmialem Vakif University, Istanbul, Turkey.
Forensic Toxicology Laboratories, Institute of Forensic Sciences, Istanbul-Cerrahpasa University, Istanbul, Turkey.
Pharm Biol. 2020 Dec;58(1):925-931. doi: 10.1080/13880209.2020.1814356.
L. (Capparaceae) is grown worldwide. Caper has been used in traditional medicine to treat various diseases including rheumatism, kidney, liver, stomach, as well as headache and toothache.
To isolate and elucidate of the secondary metabolites of the extracts which are responsible for their anti-inflammatory activities.
Buds, fruits, flowers, leaves and stems of Desf. was dried, cut to pieces, then ground separately. From their dichloromethane/hexane (1:1) extracts, eight compounds were isolated and their structures were elucidated by NMR, mass spectroscopic techniques. The effects of compounds on the expression of inflammatory cytokines in SH-SY5Y cell lines were examined by qRT-PCR ranging from 4 to 96 µM. Cell viability was expressed as a percentage of the control, untreated cells.
This is a first report on isolation of triterpenoids and steroids from with anti-inflammatory activity. One new triterpenoid ester olean-12-en-3β,28-diol, 3β-pentacosanoate () and two new natural steroids 5α,6α-epoxycholestan-3β-ol () and 5β,6β-epoxycholestan-3β-ol () were elucidated besides known compounds; oleanolic acid (), ursolic acid (), β-sitosterol (), stigmast-5,22-dien-3β-myristate () and bismethyl-octylphthalate (). mRNA expression levels as EC of all the tested seven genes were decreased, particularly CXCL9 (19.36-fold), CXCL10 (8.14-fold), and TNF (18.69) by the treatment of 26 µM of compound on SH-SY5Y cells.
Triterpenoids and steroids isolated from were found to be moderate-strong anti-inflammatory compounds. Particularly, compounds and were found to be promising therapeutic agents in the treatment of inflammatory and autoimmune diseases.
L.（山柑科）在世界各地都有种植。该植物的花蕾、果实、花朵、叶子和茎已被用于传统医学，以治疗各种疾病，包括风湿、肾脏、肝脏、胃部疾病，以及头痛和牙痛。
分离并阐明其提取物中负责抗炎活性的次生代谢产物。
将 Desf.的花蕾、果实、花朵、叶子和茎干燥、切成小块，然后分别粉碎。从它们的二氯甲烷/正己烷（1:1）提取物中分离出 8 种化合物，并通过 NMR、质谱技术阐明其结构。通过 qRT-PCR 检测化合物在 SH-SY5Y 细胞系中对炎症细胞因子表达的影响，浓度范围为 4 至 96μM。细胞活力以未经处理的对照细胞的百分比表示。
这是首次从抗炎活性的 中分离出三萜类和甾体类化合物的报道。一种新的三萜酯olean-12-en-3β,28-diol, 3β-pentacosanoate ()和两种新的天然甾体化合物 5α,6α-epoxycholestan-3β-ol ()和 5β,6β-epoxycholestan-3β-ol ()被阐明，除了已知化合物外；齐墩果酸（oleanolic acid ()）、熊果酸（ursolic acid ()）、β-谷甾醇（β-sitosterol ()）、豆甾-5,22-二烯-3β-豆蔻酸酯（stigmast-5,22-dien-3β-myristate ()）和邻苯二甲酸双辛酯（bismethyl-octylphthalate ()）。用 26μM 的化合物 处理 SH-SY5Y 细胞后，所有七种测试基因的 mRNA 表达水平均降低，特别是 CXCL9（19.36 倍）、CXCL10（8.14 倍）和 TNF（18.69 倍）。
从 中分离出的三萜类和甾体类化合物被发现是具有中等强度的抗炎化合物。特别是，化合物 和 被发现是治疗炎症和自身免疫性疾病的有前途的治疗剂。
