Artesunate | CAS:88495-63-0 | Manufacturer ChemFaces

Artesunate

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Description:

Artesunate is a part of the artemisinin group of agents with an IC50 of < 5 μM for small cell lung carcinoma cell line H69. It is a potential inhibitor of STAT-3 and exhibits selective cytotoxicity of cancer cells over normal cells in vitro; A potent inhibitor of EXP1.Artesunate has anti-inflammatory activity, can prevent neuroinflammation in BV2 microglia by interfering with NF-κB and p38 MAPK signalling.

Targets:

In vitro:

Curr Top Med Chem . 2016;16(22):2453-63.

Artesunate as an Anti-Cancer Agent Targets Stat-3 and Favorably Suppresses Hepatocellular Carcinoma[Pubmed: 26873192]

Abstract Background: Aberrant signal transducer and activator of transcription 3 (STAT-3) molecular signaling elicit hepatocellular carcinoma (HCC) in humans. Therefore, targeting STAT-3 is considered as an attractive option towards suppression of HCC in humans. Objective: Our objective is to identify a potential small molecule inhibitor that can specifically target STAT-3 and suppress HCC. Methods: In this study, we analyze a group of sesquiterpene lactone (STL) candidates that has been recently reported in preclinical trials against cancer by a unified computational and experimental approach. Results: Our virtual analysis of the STL candidates revealed Artesunate (ATS) as the best potential inhibitor of STAT-3 with comparable potency to specific inhibitor S3I-201. We also observed that ATS inhibited IL-6 driven STAT-3-DNA binding activity with comparable potency to S3I-201 in a cell free system. Furthermore ATS was observed to interfere with STAT-3 dimerization and suppression of both constitutive and IL-6 inducible STAT-3 in vitro. Nevertheless, we also observed that ATS modulated STAT-3 dependent targets (procaspase-3, Bcl-xl and survivin) favoring occurrence of apoptosis in vitro. Overall, the putative inhibition of STAT-3 by ATS suggested its capacity to interfere with STAT-3 dimerization by binding to the SH2 domain of STAT-3 monomer. It resulted in suppression of STAT-3 and also favored promotion of in vitro cells towards apoptosis. Consequently, ATS also exhibited selective cytotoxicity of cancer cells over normal cells in vitro. Conclusion: All the above observations substantiated by unified computational and in vitro experimental approaches suggested its potential role as a therapeutic anti-cancer agent against HCC.

In vivo:

Mutat Res Genet Toxicol Environ Mutagen. 2015 Jan 1;777:1-6.

The antimalarial agent artesunate causes sperm DNA damage and hepatic antioxidant defense in mice.[Pubmed: 25726169]

Artesunate is an artemisinin derivative effective against multidrug resistant malaria.
METHODS AND RESULTS:
We analyzed the effects of Artesunate 40 mg/kg b.w. as a single dose (ART1) or 13.3mg/kg b.w. for 3 days at 24h intervals (ART2) on mice spermatozoa at morphological and molecular level, and hepatic antioxidant status following 24h and 35 days following exposures in vivo. Artesunate significantly reduced epididymal sperm count and increased the frequency of sperms with abnormal head morphology following 24h of exposure. Comet assay analysis revealed significant increase in DNA strand breaks in spermatozoa evidenced by about 3-fold increase in comet tail DNA and up to 10-fold increase in Olive tail moment following 35 days of Artesunate treatment. The damage index was significantly higher in the treated groups (40.27 ± 6.62 and 37.07 ± 5.35 for ART1 and ART2 respectively) as compared to the control group (16.13 ± 3.21) indicating the genotoxic effect of Artesunate. The significant reduction in GSH, SOD and increase in lipid peroxidation indicate involvement of oxidative mechanisms in Artesunate induced toxicity in mice.
CONCLUSIONS:
The present study suggests that Artesunate has the potential to breach the testis-blood barrier and cause toxicity to male germ cells which may have implications in male reproductive toxicity.

Br J Clin Pharmacol. 2015 Apr 15.

Opposite malaria and pregnancy effect on oral bioavailability of artesunate - a population pharmacokinetic evaluation.[Pubmed: 25877779]

To compare the pharmacokinetic properties of Artesunate and dihydroartemisinin in the same women: i) pregnant with acute uncomplicated malaria on day 1 and 2, ii) pregnant with convalescent malaria on day 7 and iii) in a healthy state 3 months post-partum on day 1, 2 and 7.
METHODS AND RESULTS:
Nonlinear mixed-effects modelling was used to compare plasma concentration-time profiles of Artesunate and dihydroartemisinin over 7 days of treatment following oral and intravenous Artesunate administration to pregnant women with uncomplicated Plasmodium falciparum malaria during their second or third trimesters of pregnancy. The same women were restudied three months after delivery when fully recovered. Non-compartmental results of the same study have been published previously.Twenty pregnant patients on the Thailand-Myanmar border were studied and 15 volunteered to be restudied three months post-partum. Malaria and pregnancy had no effect on the pharmacokinetic properties of Artesunate or dihydroartemisinin after intravenous Artesunate administration. However, malaria and pregnancy had opposite effects on the absorption of orally administered Artesunate. Malaria increased the absolute oral bioavailability of Artesunate by 87%, presumably by inhibiting first-pass effect, whereas pregnancy decreased oral bioavailability by 23%.
CONCLUSIONS:
The population pharmacokinetic analysis demonstrated opposite effects of malaria and pregnancy on the bioavailability of orally administered Artesunate. Lower drug exposures during the second and third trimesters of pregnancy may contribute to lower cure rates and thus the development of drug resistance. Dose optimisation studies are required for Artesunate containing ACTs in later pregnancy.

Artesunate Description

Source:	The herbs of Artemisia annua L.
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Storage:	Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C). Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
After receiving:	The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.

Kinase Assay:

Bioorg Med Chem. 2014 Sep 1;22(17):4726-34.

A semi-synthetic derivative of artemisinin, artesunate inhibits prostaglandin E2 production in LPS/IFNγ-activated BV2 microglia.[Pubmed: 25074847]

Artesunate is a semi-synthetic derivative of artemisinin used to treat malaria, and has been shown to possess anti-inflammatory activity.
METHODS AND RESULTS:
In this study, we have investigated the effect of Artesunate on PGE2 production/COX-2 protein expression in LPS+IFNγ-activated BV2 microglia. To further understand the mechanism of action of this compound, we investigated its interference with NF-κB and p38 MAPK signalling pathways. PGE2 production was determined using EIA, while protein expressions of inflammatory targets like COX-2, mPGES-1, IκB, p38 and MAPKAPK2 were evaluated using western blot. An NF-κB-bearing luciferase reporter gene assay was used to test the effect of Artesunate on NF-κB-mediated pro-inflammatory gene expression in HEK293 cells stimulated with TNFα (1ng/ml). Artesunate (2 and 4μM), significantly (p <0.01) suppressed PGE2 production in LPS+IFNγ-activated BV2 microglia. This effect was found to be mediated via reduction in COX-2 and mPGES-1 proteins. Artesunate also produced significant inhibition of TNFα and IL-6 production in activated BV2 microglia. Further investigations showed that Artesunate (0.5-4μM) significantly (p <0.001) reduced NF-κB-driven luciferase expression, and inhibited IκB phosphorylation and degradation, through inhibition of IKK. Artesunate inhibited phosphorylation of p38 MAPK and its substrate MAPKAPK2 following stimulation of microglia with LPS+IFNγ.
CONCLUSIONS:
Taken together, we have shown that Artesunate prevents neuroinflammation in BV2 microglia by interfering with NF-κB and p38 MAPK signalling.

Cell Research:

Int Immunopharmacol. 2015 Jul;27(1):110-21.

Artesunate down-regulates immunosuppression from colorectal cancer Colon26 and RKO cells in vitro by decreasing transforming growth factor β1 and interleukin-10.[Pubmed: 25978851]

Immunosuppression is the main source of ineffective treatment on tumor, and the study aimed to investigate the effect of Artesunate on tumor immunosuppression.
METHODS AND RESULTS:
Supernatants of re-cultivated murine colorectal cancer cell Colon26 and human colorectal cancer cell RKO after pre-treatment with or without Artesunate were enrolled. After pretreatment with Artesunate, immunosuppression from the two cells was down-regulated significantly (all P<0.05), and the concentrations of TGF-β1 and IL-10 decreased greatly (all P<0.001). There were positive correlations between the down-regulation of immunosuppression and the decrease in TGF-β1 or IL-10. Their combined potency attributed to decreased TGF-β1 and IL-10 with respect to the down-regulating effect of Artesunate on immunosuppression of NK killing, lymphocyte proliferation and expressions of IL-2Rα and CD3ε(+)ζ(+), was about 60%-90%.
CONCLUSIONS:
The present analysis provides clues that Artesunate reverses the immunosuppression from Colon26 and RKO colorectal cancer cells by decreasing TGF-β1 and IL-10. This is probably one of the anti-tumor mechanisms of Artesunate.

Product Name	Artesunate
Price:	$30 / 20mg
CAS No.:	88495-63-0
Catalog No.:	CFN90313
Molecular Formula:	C₁₉H₂₈O₈
Molecular Weight:	384.42 g/mol
Purity:	>=98%
Type of Compound:	Sesquiterpenoids
Physical Desc.:	Powder
Source:	The herbs of Artemisia annua L.
Solvent:	Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc.
Download:	COA MSDS SDF Manual
Similar structural:	Comparison (Web) (SDF)
Guestbook:

	1 mg	5 mg	10 mg	20 mg	25 mg
1 mM	2.6013 mL	13.0066 mL	26.0132 mL	52.0264 mL	65.033 mL
5 mM	0.5203 mL	2.6013 mL	5.2026 mL	10.4053 mL	13.0066 mL
10 mM	0.2601 mL	1.3007 mL	2.6013 mL	5.2026 mL	6.5033 mL
50 mM	0.052 mL	0.2601 mL	0.5203 mL	1.0405 mL	1.3007 mL
100 mM	0.026 mL	0.1301 mL	0.2601 mL	0.5203 mL	0.6503 mL

CFN97212	Deoxyartemisinin	72826-63-2	266.3	C₁₅H₂₂O₄
CFN99507	Dihydroartemisinin	71939-50-9	284.35	C₁₅H₂₄O₅
CFN99184	Artemether	71963-77-4	298.38	C₁₆H₂₆O₅
CFN99011	Artemisinin	63968-64-9	282.3	C₁₅H₂₂O₅
CFN90485	alpha-Dihydroartemisinin	81496-81-3	284.34	C₁₅H₂₄O₅
CFN90313	Artesunate	88495-63-0	384.42	C₁₉H₂₈O₈