Quinine Sulfate is the Sulfate salt of Quinine, a naturally occurring alkaloid originally isolated from the bark of the cinchona tree in 1820. Bark extracts have been used for malaria since 1632 (Sullivan, 2011) and Quinine was the very first antimalarial discovered over 400 years ago. It is a stereoisomer of quinidine which contains an aromatic quinoline and a bicyclic quinuclidine. The compound can also be used to study the metabolism of hemozoin in malarial parasites. Quinine can be used in food science testing as a bitterness reference standard. A potassium channel blocker, Quinine can be incorporated into testing studies investigating the toxicity of heme complexes.
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| Mechanism of Action | Quinine Sulfate inhibits the mitochondrial ATP-regulated potassium channel. |
| Molecular Formula | C20H24N2O2 ∙ 0.5H2O4S ∙H20 |
| Microbiology Applications | Plasmodium falciparaum, the most dangerous malaria parasite, has become resistant to Quinine, thus studies are ongoing for additional natural products with development potential as antimalarial agents. |
| Eukaryotic Cell Culture Applications |
Quinine can be used as a positive control for in vitro phototoxicity testing with cellular models. The 3T3 neutral red uptake phototoxicity testing with HaCaT human keratinocyte cell line and UVA/UVB radiation is based on the 3T3 neutral red uptake phototoxicity test (NRU PT) for pharmaceutical formulation testing protocols (Maciel et al, 2022). Cytotoxicity is evaluated considering the reduction in vital dye (ie neutral red) uptake by damaged or dead cells. Aptamers are nucleic acid structures that form binding pockets for their target ligands, and have applications in synthetic biology and gene therapy. Many naturally occuring RNA aptamers are components of roboswitches (noncoding RNA gene regulatory devices containing an expression platform). Quinine Hydrochloride can be used in aptamer engineering. Researchers developed a 'Graftamer' approach, an experimental platform exploring the architecture of a natural riboswitch to enhance in vitro aptamer selection. Authors discovered aptamers for Quinine that seem to maintain the structural features of the natural guanine riboswitch aptamer. Quinine aptamers were grafted onto this platform and found these aptamers function in cells (Mohsen et al, 2023). |
| References |
Holfels E et al (1994) In vitro effects of artemisinin ether, cycloguanil hydrochloride (alone and in combination with sulfadiazine), quinine sulfate, mefloquine, primaquine phosphate, trifluoperazine hydrochloride, and verapamil on Toxoplasma gondii. Antimicrob. Agents Chemother. 38 (6):1392–1396 PMID 8092843 Kingston DGI, Cassera, MB (2022). Antimalarial Natural Products. In: Kinghorn, A.D., Falk, H., Gibbons, S., Asakawa, Y., Liu, JK., Dirsch, V.M. (eds) Antimalarial Natural Products. Progress in the chemistry of organic natural products, Vol 117. Springer, Cham. Maciel B et al (2019) Implementation of an in vitro methodology for phototoxicity evaluation in a human keratinocyte cell line. Toxicol In Vitro. 61:104618 PMID 31381965 Mohsen MG, Midy MK, Balaji A, Breaker RR (2023) Exploiting natural riboswitches for aptamer engineering and validation. Nucleic Acids Res. 51(2):966-981 PMID 36617976 |
