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    Artesunate
    Information
    CAS No. 88495-63-0 Price $30 / 20mg
    Catalog No.CFN90313Purity>=98%
    Molecular Weight384.42Type of CompoundSesquiterpenoids
    FormulaC19H28O8Physical DescriptionPowder
    Download Manual    COA    MSDSSimilar structuralComparison (Web)
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    Biological Activity
    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: NF-kB | p38MAPK | IFN-γ | IL Receptor | PGE | COX | TNF-α | IkB | TGF-β/Smad | gp120/CD4 | Antifection | IKK
    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.
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    Recently, ChemFaces products have been cited in many studies from excellent and top scientific journals

    Cell. 2018 Jan 11;172(1-2):249-261.e12.
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    Calculate Dilution Ratios(Only for Reference)
    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
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    Protocol
    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.