Torilin是一种睾酮5α还原酶抑制剂,它(IC50=31.7+/-4.23μM)对5α还原酶的抑制作用强于α-亚麻酸(IC50=160.3+/-24.62μM),但弱于非那雄胺(IC50=0.38+/-0.06μM)。Torilin具有免疫调节、肝脏保护和抗炎特性,它通过限制TAK1介导的MAP激酶和NF-βB活化来抑制炎症,它可以减轻关节炎的严重程度,改变dLN或关节中的白细胞活化,并恢复血清和脾细胞细胞因子失衡。托利林抑制α-黑素细胞刺激激素激活的B16黑色素瘤细胞中的黑色素生成,IC(50)值为25μM。Torilin对枯草芽孢杆菌ATCC 6633孢子和营养细胞表现出优异的抗菌活性。Torilin在体内和体外都具有强大的抗血管生成活性,它可能通过抑制肿瘤侵袭来抑制肿瘤发生,逆转癌细胞的多药耐药性,它可以增强阿霉素、长春碱、紫杉醇和秋水仙碱对多药耐药KB-V1和MCF7/ADR细胞的细胞毒性。
产品描述
Torilin is an inhibitor of testosterone 5 alpha-reductase, it (IC50 = 31.7 +/- 4.23 microM) shows a stronger inhibition of 5 alpha-reductase than alpha-linolenic acid (IC50 = 160.3 +/- 24.62 microM) but is weaker than finasteride (IC50 = 0.38 +/- 0.06 microM). Torilin has immunomodulatory, hepatoprotective, and anti-inflammatory properties, it inhibits inflammation by limiting TAK1-mediated MAP kinase and NF-IoB activation, it can attenuate arthritis severity, modify leukocyte activations in dLNs or joints, and restore serum and splenocyte cytokine imbalances. Torilin inhibits melanin production in alpha-melanocyte stimulating hormone-activated B16 melanoma cells, with an IC(50) value of 25 microM. Torilin shows excellent antimicrobial activity against Bacillus subtilis ATCC 6633 spores and vegetative cells. Torilin has a potent anti-angiogenic activity both in vivo and in vitro, and it may have a strong activity to suppress tumorigenesis by inhibition of tumor invasion, it reverses multidrug-resistance in cancer cells, it can potentiate the cytotoxicities of adriamycin, vinblastine, taxol and colchicine against multidrug-resistant KB-V1 and MCF7/ADR cells.
体外活性
Epidermal melanocytes synthesize melanin pigments and transfer them to keratinocytes, which is responsible for skin pigmentation. However, abnormal accumulation of melanin pigments causes hyperpigmentation disorders, which are substantially improved with treatment of tyrosinase inhibitor. In our ongoing study, Torilis japonica DC. (Umbelliferae) was found to inhibit melanin production. A goal of this study is to elucidate the hypopigmenting principle of T. japonica. METHODS AND RESULTS:A sesquiterpene structure of Torilin was isolated from the plant extracts via bioassay-guided phytochemical analysis. Torilin dose-dependently inhibited melanin production, with an IC(50) value of 25 microM, in alpha-melanocyte stimulating hormone (alpha-MSH)-activated B16 melanoma cells. Arbutin, a positive control of skin whitener, also inhibited alpha-MSH-induced melanin production with an IC(50) value of 170 microM. As to the mode of action, Torilin downregulated alpha-MSH-induced protein levels of tyrosinase without directly inhibiting catalytic activity of the enzyme. CONCLUSIONS: Taken together, this study shows that Torilin contributes to the hypopigmenting principle of T. japonica, and suggests its pharmacological potential in melanin-associated hyperpigmentation disorders[1].
Cas No.
13018-10-5
分子式
C22H32O5
分子量
376.49
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years