Hyperforin 是瞬时受体典型 6 (TRPC6) 通道激活剂。Hyperforin 通过激活 Ca2+传导非选择性典型 TRPC6 通道来调节 Ca2+水平。Hyperforin 还表现出多种药理活性,包括抗抑郁、抗肿瘤、抗痴呆、抗糖尿病等。Hyperforin 调节 γδ T 细胞分泌 IL-17α,改善
Imiquimod (HY-B0180) 诱导的银屑病样小鼠皮肤炎症。
生物活性 | Hyperforin is atransient receptor canonical 6 (TRPC6)channels activator. Hyperforin modulates Ca2+levels by activating Ca2+-conducting non-selective canonical TRPC6 channels. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improvesImiquimod(HY-B0180)-induced psoriasis-like mice model[1][2][3][4][5]. |
IC50& Target | |
体外研究 (In Vitro) | Hyperforin 具有多向作用机制。它阻断配体门控 (GABA、NMDA 和 AMPA 受体) 和电压门控通道(Ca2+, K+, Na+) 的电导[2]。 Hyperforin (0.1, 1,10 μM; 2 h) 降低体外培养的小鼠脾 γδ T 细胞中 IL-17A 的表达和分泌[3]。 Hyperforin (0.1, 1,10 μM; 2 h) 抑制 TNF-α 刺激的 HaCaT 细胞中 MAPK 和 STAT3 通路的磷酸化[3]。 Hyperforin (IC50=3.7 μmol/L) 抑制 HDMEC 微血管管的形成和增殖,呈剂量依赖性,无毒性作用[4]。
Western Blot Analysis[3] Cell Line: | HaCaT cells | Concentration: | 0.1, 1, 10 μM; with or without 10, 20 ng/mL TNF-α | Incubation Time: | 2 hours | Result: | Reduced the expressions of p-p38, p-ERK, p-JNK, and p-STAT3, especially at the dosage of 10 μM. |
|
体内研究 (In Vivo) | Hyperforin (5 mg/kg; 腹腔注射; 每天 1 次, 共 7 天) 能够改善Imiquimod(HY-B0180) 诱导的小鼠银屑病皮损情况,抑制炎症细胞浸润和炎症因子释放[3]。
Animal Model: | IMQ-induced psoriasis-like mice model[3] | Dosage: | 5 mg/kg | Administration: | Intraperitoneal injection; once daily for 7 days | Result: | Significantly ameliorated skin lesion throughout the treatment period, demonstrated by the reduced severity score of skin inflammation. Suppressed infiltration of CD3+ T cells and downregulated expression of Il1, Il6, Il23, Il17a, Il22, antimicrobial peptides (AMPs) in the skin lesion. |
|
分子量 | |
Formula | |
CAS 号 | |
结构分类 | |
来源 | - Plants
- Guttiferae
- Hyperlcurn perforatumL.
|
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |