化学信息：

中文名	穿心莲内酯
英文名	Andrographolide
中文别名	-
英文别名	Andrographis
来源	穿心莲Andrographis paniculata (Burm. f.) Nees
化合物类型	萜类(Terpenoids)>二萜>二萜内酯
化学式	C20H30O5
分子量	350.45
CAS号	5508-58-7
纯度	98%, HPLC
溶剂/溶解度	Water: < 0.1 mg/ml (insoluble); DMSO: 50 mg/ml (142.67 mM)
溶液配制	5mg加入1.43ml DMSO，或者每3.50mg加入1ml DMSO，配制成10mM溶液。

生物信息

产品描述	Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.
信号通路	-
靶点	p50	-	-	-	-
IC50	NF-κB	-	-	-	-
体外研究	Andrographolide (AP) concentration-dependently suppresses receptor activator of nuclear factor kappa B ligand (RANKL)-mediated osteoclast differentiation and bone resorption in vitro and reduces the expression of osteoclast-specific markers. Andrographolide attenuates inflammation by inhibition of TNFα-induced NF-κB activation through covalent modification of reduced Cys62 of p50, without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide also inhibits the ERK/MAPK signalling pathway without affecting p38 or JNK signalling. Andrographolide inhibits osteoclast differentiation of RAW 264.7 cells in a concentration-dependent manner. Andrographolide suppresses osteoclast formation in a concentration-dependent manner without any obvious cytotoxic effects, in both BMMs and RAW 264.7 cells. Andrographolide treatment substantially reduces the area of bone resorption. Only approximately 30% of the bone resorption observed in the control group is achieved after treatment with 2.5 μM Andrographolide. Osteoclastic bone resorption is almost completely inhibited after treatment with 10 μM Andrographolide.
体内研究	Treatment with Andrographolide (5 or 30 mg/kg) reduces the extent of bone loss induced by LPS. Moreover, Andrographolide slightly increases the BMD and cortex thickness compared to LPS treatment. Histological examination confirms the protective effects of Andrographolide on LPS-induced bone loss. LPS injection leads to inflammatory bone erosion and increased numbers of TRAP-positive osteoclasts.
临床实验	NCT03134443: Acute Tonsillitis, Phase 4; NCT03132623: Acute Bronchitis, Phase 4; NCT03132610: Acute Exacerbation of Chronic Bronchitis, Phase 4.

参考文献：

1.Zhai ZJ, et al. Br J Pharmacol. 2014,171(3):663-75.

2.Gupta S, et al. Arch Virol. 2017,162(3):611-623.

包装清单：

产品编号	产品名称	包装
SM5168-10mM	穿心莲内酯(98%, HPLC)	10mM×0.2ml
SM5168-25mg	穿心莲内酯(98%, HPLC)	25mg
SM5168-100mg	穿心莲内酯(98%, HPLC)	100mg
－	说明书	1份

保存条件：

-20℃保存，至少一年有效。固体粉末4℃保存，至少一个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。

注意事项：

本产品可能对人体有一定的毒害作用，请注意适当防护，以避免直接接触人体或吸入体内。

本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。

为了您的安全和健康，请穿实验服并戴一次性手套操作。

使用说明：
1.收到产品后请立即按照说明书推荐的条件保存。使用前可以在2,000-10,000g离心数秒，以使液体或粉末充分沉降至管底后再开盖使用。
2.对于10mM溶液，可直接稀释使用。对于固体，请根据本产品的溶解性及实验目的选择相应溶剂配制成高浓度的储备液(母液)后使用。
3.具体的最佳工作浓度请参考本说明书中的体外、体内研究结果或其它相关文献，或者根据实验目的，以及所培养的特定细胞和组织，通过实验进行摸索和优化。
4.不同实验动物依据体表面积的等效剂量转换表请参考如下网页：
https://www.beyotime.com/support/animal-dose.htm