Description |
Hyperforin is a transient 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, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model[1][2][3][4][5].
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Target |
TRPC6[1]
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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.
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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.
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Density | 1.0±0.1 g/cm3 |
Boiling Point | 616.8±55.0 °C at 760 mmHg |
Flash Point | 340.9±28.0 °C |
Exact Mass | 536.386536 |
PSA | 71.44000 |
LogP | 12.30 |
Vapour Pressure | 0.0±4.0 mmHg at 25°C |