贯叶金丝桃素

贯叶金丝桃素用途

Hyperforin是一种瞬时受体典型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还显示出多种药理活性,包括抗抑郁、抗肿瘤、抗痴呆和抗糖尿病。Hyperforin调节γδT细胞分泌IL-17α,改善咪喹莫特(HY-B0180)诱导的银屑病样小鼠模型[1][2][3][4][5]。

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贯叶金丝桃素名称

[ CAS 号 ]:
11079-53-1

[ 中文名 ]:
贯叶金丝桃素

[ 英文名 ]:
Hyperforin

[英文别名 ]:

Hyperforin
MFCD01861497

贯叶金丝桃素生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

信号通路 >> 跨膜转运 >> TRP频道

研究领域 >> 炎症/免疫

研究领域 >> 神经疾病

[ 靶点 ]

TRPC6[1]

[体外研究]

Hyperforin公司具有多向作用机制。它阻断配体门控 (GABA、NMDA)和安帕受体) 和电压门控通道(Ca2+、K+、Na+)的电导[2]。 Hyperforin(0.1,1,10μM；2小时)降低体外培养的小鼠脾 γδT细胞中白介素-17A的表达和分泌[3]。 Hyperforin(0.1,1,10μM；2小时)抑制肿瘤坏死因子-α刺激的 HaCaT公司细胞中地图和状态3通路的磷酸化[3]。 Hyperforin(IC50=3.7μmol/L)抑制 HDMEC公司微血管管的形成和增殖,呈剂量依赖性,无毒性作用[4]。 Western印迹分析[3]细胞系：HaCaT细胞浓度：0.1、1、10μM；含或不含10,20 ng/mL TNF-α孵育时间：2小时结果：减少p-p38,p-ERK,p-JNK和p-STAT3的表达,尤其是在10μM剂量下。

[体内研究]

Hyperforin(5 mg/kg；腹腔注射; 每天 1.次, 共 7.天) 能够改善咪喹莫特(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]。动物模型：IMQ诱导的银屑病样小鼠模型[3]剂量：5mg/kg给药：腹腔注射；结果：在整个治疗期间,皮肤损伤显著改善,皮肤炎症严重程度评分降低。抑制皮肤损伤中CD3+T细胞的浸润并下调Il1、Il6、Il23、Il17a、Il22、抗菌肽(AMP)的表达。

[参考文献]

[1]. Heiser JH, et al. TRPC6 channel-mediated neurite outgrowth in PC12 cells and hippocampal neurons involves activation of RAS/MEK/ERK, PI3K, and CAMKIV signaling. J Neurochem. 2013 Nov;127(3):303-13.

[2]. Pochwat B, et al. Hyperforin Potentiates Antidepressant-Like Activity of Lanicemine in Mice. Front Mol Neurosci. 2018 Dec 12;11:456.

[3]. Zhang S, et al. Hyperforin Ameliorates Imiquimod-Induced Psoriasis-Like Murine Skin Inflammation by Modulating IL-17A-Producing γδ T Cells. Front Immunol. 2021 May 5;12:635076.

[4]. Adam P, et al. Biosynthesis of hyperforin in Hypericum perforatum. J Med Chem. 2002 Oct 10;45(21):4786-93.

[5]. Li XX, et al. Hyperforin: A natural lead compound with multiple pharmacological activities. Phytochemistry. 2023 Feb;206:113526.

贯叶金丝桃素物理化学性质

[ 密度 ]:
1.0±0.1 g/cm3

[ 沸点 ]:
616.8±55.0 °C at 760 mmHg

[ 熔点 ]:
79-80ºC

[ 分子式 ]:
C₃₅H₅₂O₄

[ 分子量 ]:
536.785

[ 闪点 ]:
340.9±28.0 °C

[ 精确质量 ]:
536.386536

[ PSA ]:
71.44000

[ LogP ]:
12.30

[ 外观性状 ]:
白色至灰白色粉末

[ 蒸汽压 ]:
0.0±4.0 mmHg at 25°C

[ 折射率 ]:
1.518

[ 储存条件 ]:
-20°C，密闭，干燥

贯叶金丝桃素安全信息

[ 符号 ]:

GHS02, GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H301 + H311 + H331-H370

[ 警示性声明 ]:
P210-P280-P302 + P352 + P312-P304 + P340 + P312-P370 + P378-P403 + P235

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
F,T

[ 风险声明 (欧洲) ]:
11-23/24/25-39/23/24/25

[ 安全声明 (欧洲) ]:
7-16-36/37-45

[ 危险品运输编码 ]:
UN1230 - class 3 - PG 2 - Methanol

[ WGK德国 ]:
3

[ 海关编码 ]:
29144000

贯叶金丝桃素文献

Plant flavonol isorhamnetin attenuates chemically induced inflammatory bowel disease via a PXR-dependent pathway.

J. Nutr. Biochem. 25(9) , 923-33, (2014)

Isorhamnetin is an O-methylated flavonol present in fruit and vegetables. We recently reported the identification of isorhamnetin as an activator of the human pregnane X receptor (PXR), a known target...

Phytochemical analysis and in vitro biological activity of three Hypericum species from the Canary Islands (Hypericum reflexum, Hypericum canariense and Hypericum grandifolium).

Fitoterapia 100 , 95-109, (2015)

In the present work we carried out a phytochemical and biological investigation on three Hypericum species, i.e. Hypericum reflexum, Hypericum canariense and Hypericum grandifolium, from the Canary Is...

Human UGT1A4 and UGT1A3 conjugate 25-hydroxyvitamin D3: metabolite structure, kinetics, inducibility, and interindividual variability.

Endocrinology 155(6) , 2052-63, (2014)

25-Hydroxyvitamin D3 (25OHD3) is used as a clinical biomarker for assessment of vitamin D status. Blood levels of 25OHD3 represent a balance between its formation rate and clearance by several oxidati...

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