IT0640 知母皂苷BⅡ 抑制剂/拮抗剂/激动剂 索莱宝

Timosaponin BII 是一种抗氧化剂和抗炎化合物。

使用本产品的应用案例（仅供参考）

In Vitro

In Vitro Incubation of Timosaponin BII with Gut Microbiota

After 7 SD rats were sacrificed, the colon contents were collected and added to the sterilized anaerobic medium (Solarbio Life Sciences Co., Ltd., Beijing, China) at a ratio of 1.0 g:20 mL, and stirred gently. After filtering, the culture medium containing gut microbiota (mixed medium) was placed in a N2 atmosphere, and pre-incubated at 37 ?C for 60 min before use. Accurately weigh 1.0 mg of timosaponin BII and dissolve with methanol to obtain a solution of 1 mg/mL. The incubation system consists of 10 μL of timosaponin BII in methanol (1 mg/mL), and 990 μL of mixed medium. The incubation was conducted in a 37 ?C, 200 rpm shaking incubator. The incubation system must be maintained completed in an anaerobic environment during the experiment. In the first incubation experiment, the timosaponin BII and mixed medium were incubated for 0, 1, 2, 6, 12, and 24 h, respectively. In the second incubation experiment, the drugs and mixed medium were incubated for 0, 0.25, 0.5, 1, 1.5, and 2 h, respectively. In addition, the negative control group was introduced consisting of twice boiled mixed medium incubated with the same amount of timosaponin BII. The termination reaction was carried out by adding 3-fold volume of 100 ng/mL glipizide methanol solution (IS), shaking it evenly and then precipitating the protein. After each sample was centrifuged at 13,400× g rpm in a 4 ?C refrigerated centrifuge for 10 min, 10 μL of supernatant was injected for LC-MS/MS analysis, and 7 μL of supernatant was injected for LC/MS-Q-TOF analysis.

In Vitro Incubation of Timosaponin BII with Liver Microsomes and Liver Homogenate

The liver microsome incubation system was consisted of the following: 5 μL SD rat liver microsomes (20 mg/mL), 2 μL timosaponin BII (1 mM), 20 μL of NADPH, and 0.05 mM Tris/HCl (pH = 7.4), with a total volume of 200 μL. The incubation was conducted in a shaking incubator at 37 ?C and 800 rpm with supply of oxygen. After the incubation, 3-fold volume of glipizide methanol solution (IS, 100 ng/mL) was added to the incubation system and mixed to stop the reaction at 0, 0.25, 0.5, 1, 1, 5, and 2 h. After centrifugation at 13,400× g rpm in a refrigerated centrifuge at 4 ?C for 10 min, 10 μL of the supernatant was injected for LC-MS/MS analysis.

Liver homogenate was prepared by homogenizing freshly collected SD rat livers and adding ice-cold normal saline with weight/volume = 1:3. The liver homogenate incubation system was consisted as follows: 2 μL timosaponin BII (1 mM), 198 μL of freshly prepared liver homogenate, with a total volume of 200 μL.

Incubation was conducted in a shaking incubator at 37 ?C and 800 rpm with supply of oxygen. After the incubation, 3-fold volume of glipizide methanol solution (IS, 100 ng/mL) was added to the incubation system and mixed to stop the reaction at 0, 0.25, 0.5, 1, 1, 5, and 2 h. After centrifugation at 13,400× g rpm in a refrigerated centrifuge at 4 ?C for 10 min, 10 μL of the supernatant was injected for LC-MS/MS analysis.

来源文献：Dong GM, Yu H, Pan LB, Ma SR, Xu H, Zhang ZW, Han P, Fu J, Yang XY, Keranmu A, Niu HT, Jiang JD, Wang Y. Biotransformation of Timosaponin BII into Seven Characteristic Metabolites by the Gut Microbiota. Molecules. 2021 Jun 24;26(13):3861. doi: 10.3390/molecules26133861. PMID: 34202717; PMCID: PMC8270264.

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标题:Timosaponin B-II alleviates osteoarthritis-related inflammation and extracellular matrix degradation through inhibition of mitogen-activated protein kinases and nuclear factor-κB pathways in vitro

成员:Xinwei Liu, Dulei Xiang, Wenming Jin, Gen Zhao, Han Li, Bing Xie, Xiaochuan Gu

论文因子:6.832 发表期刊:Bioengineered pmid:35094658

【本资料源自公开渠道，如需（此处）屏蔽，请联系删除】

标题:Biotransformation of Timosaponin BII into Seven Characteristic Metabolites by the Gut Microbiota.

成员:Dong GM, Yu H, Pan LB, Ma SR, Xu H, Zhang ZW, Han

论文因子:4.148 发表期刊:Molecules. pmid:34202717

基本信息
CAS	No.136656-07-0
中文名称	知母皂苷BⅡ
英文名称	Timosaponin BⅡ
别名	;知母皂苷B2;知母皂苷BII;知母皂苷BⅡ;
分子式	C45H76O19
分子量	921.07
溶解性	Soluble in DMSO
纯度	HPLC≥98%
外观(性状)	White to off-white Solid
储存条件	Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
MDL	MFCD30179489
SMILES	C[C@@]1([C@]([C@@H]2C)([H])[C@](O[C@]2(O)CC[C@H](C)CO[C@@H]([C@@H]([C@@H](O)[C@@H]3O)O)O[C@@H]3CO)([H])C4)[C@]4([H])[C@@](CC[C@@]5([H])[C@@]6(CC[C@H](O[C@@](O[C@H](CO)[C@H](O)[C@@H]7O)([H])[C@@H]7O[C@]([C@@H]([C@@H](O)[C@@H]8O)O)([H])O[C@@H]8CO)C5)C)([H])[C@]6([H])CC1
靶点	Others
通路	Others
背景说明	Timosaponin BII 是一种抗氧化剂和抗炎化合物。
生物活性	Timosaponin BII 是一种抗氧化剂和抗炎化合物。[1-2]
In Vitro	Timosaponin BII是一种从Zhi Mu中分离出的甾体糖苷，被发现具有抑制HL-60(白血病)，Hela(子宫颈)，HepG2和Bel-7402(肝脏)，HT-29(结肠)增殖的抑制活性，和MDA-MB-468(乳腺)人癌细胞系在HL-60细胞中的IC50值为15.5μg/ mL [1]。
细胞实验	模型组和载体对照组中的大鼠视网膜表现出BACE1表达的明显上调。同时，丙二醛(MDA)，Aβ1-40和β-CTF的水平增加。然而，当与媒介物对照组相比时，Timosaponin-BII处理组中的视网膜显示出显著更少的BACE1并且累积更少的Aβ1-40或β-CTF。它还显示MDA水平显著降低和部分凝血活酶时间延长[2]。
数据来源文献	[1]. Guo J， et al. Cytotoxic activities of chemical constituents from rhizomes of Anemarrhena asphodeloides and their analogues. Arch Pharm Res. 2015;38(5):598-603. [2]. Huang JF， et al. Timosaponin-BII inhibits the up-regulation of BACE1 induced by ferric chloride in rat retina. BMC Complement Altern Med. 2012 Oct 22;12:189.
单位	瓶