However, a short half-life, and poor water solubility and bioavailability limited further anticancer applications of artemisinins. Recent studies revealed that artemisinins also displayed antitumor, antidiabetic, antifungal, immunomodulatory, antiviral, anti-inflammatory and antibacterial activities. Artemisinin and its derivatives (artemisinins) have become the standard therapy for malaria. Therefore, there is an urgent need to develop more effective treatment options.Īrtemisinin, a sesquiterpene lactone containing an endoperoxide bridge, was originally isolated from the Chinese herb Qinghao ( Artemisia annua) as an effective antimalarial component. However, many patients are diagnosed at advanced stages and rely on non-surgical procedures, such as chemotherapy and radiation therapy, and the survival rate remains low. In the early stages, HCC can be treated with surgical procedures. Hepatocellular carcinoma (HCC) is the most common form and accounts for 80–90% of primary liver cancer. Thus, UDCMe-Z-DHA may be a potential drug candidate for hepatocellular carcinoma.Īccording to the International Agency for Research on Cancer, primary liver cancer is the sixth most common cancer in the world and the third leading cause of cancer death for both sexes in 2020. Compared to DHA, UDCMe-Z-DHA displayed much lower cytotoxicity toward normal cells. Mechanistic studies revealed that UDCMe-Z-DHA caused G0/G1 arrest and induced reactive oxygen species (ROS), mitochondrial membrane potential loss and autophagy, which may in turn lead to apoptosis. Time course experiments and stability in medium determined by cell viability assay as well as HPLC-MS/MS analysis revealed that UDCMe-Z-DHA was more stable than DHA, which in part accounted for the increased anticancer activity. We found that UDCMe-Z-DHA was even more potent than UDC-DHA in HepG2 cells with IC 50 of 1 μM. ![]() ![]() The objectives of this study were to evaluate the anticancer activity and investigate the molecular mechanisms of UDCMe-Z-DHA, a hybrid of ursodeoxycholic acid methyl ester and DHA via a triazole linkage. We synthesized a series of bile acid–dihydroartemisinin hybrids to improve its stability and anticancer activity and demonstrated that an ursodeoxycholic–DHA (UDC-DHA) hybrid was 10-fold more potent than DHA against HepG2 hepatocellular carcinoma cells. Dihydroartemisinin (DHA), an antimalarial drug, has been reported to exhibit anticancer activity but with a short half-life. patents that may apply, see bd.com/patents.Hepatocellular carcinoma is the third most common cause of cancer-related death according to the International Agency for Research on Cancer. Please refer to to access safety data sheets (SDS).We recommend use of BD Horizon Brilliant™ Stain Buffer in your experiments to help mitigate potential background. Human donor specific background has been observed in relation to the presence of anti-polyethylene glycol (PEG) antibodies, developed as a result of certain vaccines containing PEG, including some COVID-19 vaccines.For fluorochrome spectra and suitable instrument settings, please refer to our Multicolor Flow Cytometry web page at.Dilute azide compounds in running water before discarding to avoid accumulation of potentially explosive deposits in plumbing. Caution: Sodium azide yields highly toxic hydrazoic acid under acidic conditions.Please observe the following precautions: Absorption of visible light can significantly alter the energy transfer occurring in any tandem fluorochrome conjugate therefore, we recommend that special precautions be taken (such as wrapping vials, tubes, or racks in aluminum foil) to prevent exposure of conjugated reagents, including cells stained with those reagents, to room illumination.An isotype control should be used at the same concentration as the antibody of interest.We typically use 1 × 10^6 cells in a 100-µl experimental sample (a test). ![]() This reagent has been pre-diluted for use at the recommended Volume per Test. ![]() Please refer to for technical protocols.
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