IA1300 青蒿琥酯 抑制剂/拮抗剂/激动剂 索莱宝

使用本产品的案例（仅供参考）

In Vitro

Cell（ARPE-19，0~200μM Artesunate,0~72h）

The cells were cultured to 80% ? 90% fusion degree, starved overnight in serum-free medium, and replaced with DMEM / F12 containing 1% FBS,Different concentrations of artesunate (Solarbio) (0,50,100,150,200μM)Cell proliferation and migration were detected at different time points (0, 24, 48 and 72h).   TGF was used-βThe degree of EMT was detected after 48 hours of pretreatment with artesunate.

来源文献：Wang ZY, Zhang Y, Chen J, Wu LD, Chen ML, Chen CM, Xu QH. Artesunate inhibits the development of PVR by suppressing the TGF-β/Smad signaling pathway. Exp Eye Res. 2021 Dec;213:108859. doi: 10.1016/j.exer.2021.108859. Epub 2021 Nov 23. PMID: 34822854.

In Vivo

Mice（Young (4 month) mice：30μg/g Artesunate，1次/天，16天，口服；Aged (20 month) mice：30μg/g Artesunate，1次/2天，口服）

Young (4 month) mice were randomly divided into 3 groups (n=5): Vehicle, Tm and Tm+Artesunate. The mice were orally administrated with Artesunate (Solarbio, China, 30 μg/g, dissolved in 5 % NaHCO3) for successive 16 days.    Body weight was measured every day. Tm (6 μg/g) was intraperitoneally administrated 15 h before sacrifice.    FD-4 was administrated 3 h before sacrifice for the evaluation of intestinal permeability. Colon length was measured and mucosa tissues were removed for subsequent experiments.

Aged (20 month) mice were randomly divided into 2 groups (n=5): Vehicle and Artesunate. The mice were orally administrated with Artesunate (30 μg/g) every other day for a total of 25 doses.    Body weight was measured every 2 days. Length of colon was measured at sampling time and FD-4 leakage were measured. Colon mucosa tissues were removed for subsequent experiments.

来源文献：Chen H, Sun HM, Wu B, Sun TY, Han LZ, Wang G, Shang YF, Yang S, Zhou DS. Artesunate delays the dysfunction of age-related intestinal epithelial barrier by mitigating endoplasmic reticulum stress/unfolded protein response. Mech Ageing Dev. 2023 Mar;210:111760. doi: 10.1016/j.mad.2022.111760. Epub 2022 Dec 5. PMID: 36476344.

Rabbit（2-2.5kg Adult pigmented rabbits, 20μg/mL Artesunate, 注射于玻璃体）

Twelve adult pigmented rabbits were selected, each weighing about 2-2.5kg, After extracted 0.2ml vitreous,12 traumatic PVR model rabbits were prepared by intravitreal injection of 0.1ml platelet rich plasma and 0.1mlPBS.   They were randomly divided into blank group, control group (0.1mlprp +0.1mlpbs) and experimental group: (0.1mlPRP + 0.1mL 20μg/ml artesunate).    In the control group, 0.1mL platelet-rich plasma and 0.1mL PBS were injected into the vitreous cavity at the same time. In the experimental group, 0.1mL platelet rich plasma and 0.1ml artesunate (20μg/ml) were injected into the vitreous cavity at the same time. Fundus photography and B ultrasound machine were used to observe the proliferation of the vitreous and retina at different periods. The expression of Vim, Smad3 and PSmad3 in vitreous retinal hyperplasia was detected by Western blotting 28 days after surgery, and the retinal tissue structure of each group was observed by frozen section.

来源文献：Wang ZY, Zhang Y, Chen J, Wu LD, Chen ML, Chen CM, Xu QH. Artesunate inhibits the development of PVR by suppressing the TGF-β/Smad signaling pathway. Exp Eye Res. 2021 Dec;213:108859. doi: 10.1016/j.exer.2021.108859. Epub 2021 Nov 23. PMID: 34822854.

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标题:Artesunate protects against ocular fibrosis by suppressing fibroblast activation and inducing mitochondria-dependent ferroptosis

成员:Jingyuan Liu, Zheng Pan, Boding Tong, Cong Wang, Jia Yang, Jingling Zou, Jikuan Jiang, Lusi Zhang, Bing Jiang

论文因子:5.834 发表期刊:FASEB JOURNAL pmid:37159329

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标题:Artesunate delays the dysfunction of age-related intestinal epithelial barrier by mitigating endoplasmic reticulum stress/unfolded protein response

成员:Chen H. Sun HM. Wu B. Sun TY. Han LZ. Wang G. Shan

论文因子:5.013 发表期刊:Mech Ageing Dev pmid:36476344

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标题:Artesunate inhibits the development of PVR by suppressing the TGF-β/Smad signaling pathway

成员:Wang ZY. Zhang Y. Chen J. Wu LD. Chen ML. Chen CM.

论文因子:3.161 发表期刊:Exp Eye Res pmid:34822854

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标题:Artesunate inhibits the development of PVR by suppressing the TGF-β/Smad signaling pathway

成员:Wang ZY. Zhang Y. Chen J. Wu LD. Chen ML. Chen CM.

论文因子:3.161 发表期刊:Exp Eye Res pmid:34822854

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标题:Artesunate inhibits proliferation and migration of RPE cells and TGF-β2 mediated epithelial mesenchymal transition by suppressing PI3K/AKT pathway

成员:Wang ZY; Zhang Y; Wu LD; Chen J; Chen ML; Chen CM; Xu QH

论文因子:1.4 发表期刊:International Journal of Ophthalmology pmid:35186677

基本信息
CAS	No.88495-63-0
中文名称	青蒿琥酯
英文名称	Artesunate
别名	WR-256283
分子式	C19H28O8
分子量	384.42
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
EC	EINECS 618-170-5
MDL	MFCD00866204
SMILES	O=C(O[C@H]1[C@H](C)[C@]2([H])CC[C@@H](C)[C@]3([H])CC[C@@](O4)(C)OO[C@]32[C@]4([H])O1)CCC(O)=O
InChIKey	FIHJKUPKCHIPAT-AHIGJZGOSA-N
InChI	InChI=1S/C19H28O8/c1-10-4-5-13-11(2)16(23-15(22)7-6-14(20)21)24-17-19(13)12(10)8-9-18(3,25-17)26-27-19/h10-13,16-17H,4-9H2,1-3H3,(H,20,21)/t10-,11-,12+,13+,16-,17-,18-,19-/m1/s1
PubChem CID	6917864
靶点	STAT3;EXP1
通路	JAK/STAT Signaling
背景说明	Artesunate是 STAT-3 和EXP1 的抑制剂。
生物活性	Artesunate 是 STAT-3 和输出蛋白 1 (EXP1) 的抑制剂。[1-3]
In Vitro	青蒿琥酯是STAT-3 [1]和输出蛋白1(EXP1)的抑制剂[2]。青蒿琥酯治疗24小时导致两种细胞系中活性氧(ROS)水平以剂量依赖性方式显著增加。此外，蛋白质印迹显示，当用更高剂量范围的青蒿琥酯处理癌细胞24小时时，γ-H2AX的水平显著升高。青蒿琥酯还显示出对A2780和HO8910细胞中RAD51水平的时间依赖性影响。在两种类型的非恶性细胞，正常人成纤维细胞和永生化上皮细胞FTE-187中，青蒿琥酯不改变RAD51的水平。在A2780细胞中，RAD51 mRNA的水平确实通过添加青蒿琥酯而以剂量依赖性方式降低。相应地，青蒿琥酯显著抑制RAD51的启动子活性。相比之下，H8910细胞中的RAD51 mRNA水平不受青蒿琥酯的影响[3]。
细胞实验	接受青蒿琥酯和顺铂联合治疗的组肿瘤生长明显减少(P <0.01)。相比之下，单独的青蒿琥酯对两种细胞系的肿瘤异种移植物的生长没有显着影响[3]。
细胞实验	A2780和HO8910细胞在RPMI 1640，DMEM中的正常人成纤维细胞(NHF)和M199中的FTE-187中培养，补充有10％胎牛血清，100单位/ mL青霉素和100mg/mL链霉素。将所有细胞在95％空气和5％CO 2的潮湿气氛中孵育。将青蒿琥酯以0，5，10，25或50μg/ mL的浓度应用于培养的细胞不同时期。确定青蒿琥酯处理后的活性氧(ROS)产生。简言之，将细胞加载5μM的CM-H2DCFDA，并在用青蒿琥酯处理后在37℃下孵育20分钟。使用保存液重悬细胞并用FACSCanto II分析。氧化的CM-H2DCFDA的峰值激发波长为490nm，发射为530nm [3]。
动物实验	使用4-6周龄雌性无胸腺裸鼠(BALB/c，nu/nu)。收获A2780和HO8910细胞并重悬于0.1ml PBS中，将5×10 6个细胞/0.2mL皮下注射到小鼠的左腹股沟区域。两周后，携带肿瘤的小鼠(A2780和HO8910约70mm3)随机分成4组。每天通过ip注射以单独50mg/kg的剂量施用青蒿琥酯，持续16天。每隔一天监测肿瘤生长。肿瘤体积由公式1/2a×b2确定，其中a是长直径(mm)，b是短直径(mm)[3]。
激酶实验	用青蒿琥酯处理24小时后，收获细胞并在1×细胞裂解缓冲液中裂解。通过SDS-PAGE分离15至25μg的总蛋白质并转移至聚偏二氟乙烯(PVDF)膜。在室温下用5％脱脂乳封闭膜1至2小时，然后用一抗探测并在4℃温育过夜。在用TBS-T充分洗涤后，将膜与合适的HRP缀合的二抗在室温下孵育1小时，然后通过Western ECL增强的鲁米诺试剂检测[3]。
数据来源文献	[1]. Ilamathi M， et al. Artesunate as an Anti-Cancer Agent Targets Stat-3 and Favorably Suppresses Hepatocellular Carcinoma. Curr Top Med Chem. 2016;16(22):2453-63. [2]. Lisewski AM， et al. Supergenomic network compression and the discovery of EXP1 as a glutathione transferase inhibited by artesunate. Cell. 2014 Aug 14;158(4):916-928. [3]. Wang B， et al. Artesunate sensitizes ovarian cancer cells to cisplatin by downregulating RAD51. Cancer Biol Ther. 2015;16(10):1548-56
单位	瓶