Preparative HPLC fractionation of Cinnamomum cassia Water Extract and their in-vitro Antimalarial Activities

Abstract

Due to the development of antimalarial resistance strains of Plasmodium falciparum, the search for new antimalarial drugs is immediately needed. Such drugs might work by obstructing the heme detoxification pathway in the malaria parasite, a vital requirement for parasite existence in host erythrocytes. The present study is aimed to investigate the antimalarial activity of four preparative HPLC fractions from Cinnamomum cassia water extract using semi-quantitative in vitro micro-assay that is based on the inhibition of ferriprotoporphyrin IX (FP) biomineralization. A reversed phase C18 inch preparative column and wateracetonitrile binary solvent mixture mobile phase were used to collect the fractions at 275 nm. UHPLC-MS revealed that the major compounds in water crude Cinnamomum cassia extract are coumarin and cinnamic acid. Containing coumarin as a major compound, fraction 2 showed superior efficacy compared to chloroquine and 2 -mercaptopyrimidine positive controls. Fraction 3 which contains cinnamic acid showed moderate activity, while fraction 4 was the least potent.

Phytochemical screening of Pomegranate juice, peels, leaves and membranes water extracts and their effect on β- hematin formation, a comparative study

“…The method of choice for extracting phytochemicals from food or natural herbs in our laboratory is infusion. [3][4][5][6][7][8][9][10][11] Since different preparations may exert different actions and safety profiles, we opt to use it the most popular and simple method. Infusion crude water extracts of pomegranate leaves, juice, peels and membranes were freshly prepared and directly analyzed using HPLC-PDA and the UV absorption was high at 350nm ( Figure 1).…”

“…During the past ten years, an extensive in-vitro β-hematin inhibition screening on edible food, wild natural plant extracts and/or pure isolates have been engaged in our laboratory. [3][4][5][6][7][8][9][10][11] The mechanism that links antimalarial effects with the ability to inhibit β-hematin formation has been thoroughly discussed. [3][4][5][6][7][8][9][10][11] Preparative chromatography and liquid chromatography coupled to mass spectrometer (LC-MS) were used to isolate and identify active phytochemicals present in these foods and/or natural herbs.…”

“…[3][4][5][6][7][8][9][10][11] The mechanism that links antimalarial effects with the ability to inhibit β-hematin formation has been thoroughly discussed. [3][4][5][6][7][8][9][10][11] Preparative chromatography and liquid chromatography coupled to mass spectrometer (LC-MS) were used to isolate and identify active phytochemicals present in these foods and/or natural herbs. Although encouraging results were achieved, the ability of the above-mentioned tests to predict activity against in-vivo human malaria has not yet been established.…”

Alkyl and Aryl Derivatives Based on p-Coumaric Acid Modification and Inhibitory Action against Leishmania braziliensis and Plasmodium falciparum

“…( Leishmania ) amazonensis affect more than 98 countries worldwide [ 11 , 12 ]. Caused by unicellular eukaryotic protozoans of the Plasmodium genus such as Plasmodium falciparum and Plasmodium vivax , leishmaniasis quickly develops into a very serious human infection that can cause death [ 13 , 14 , 15 ]. Approximately 12 million people are currently affected with the disease [ 16 ].…”

Hetaryl‐1,5 Benzodiazepines—Part I: Synthesis of 3‐pyrimidinyl‐ and Imidazolyl‐1,5‐benzodiazepines

“…Pyrimidines are reported to possess pharmacological activities, such as antineoplastic and anticancer agents , analgesic, anti‐pyretic , anti‐HIV , and anti‐tubercular , and are used as antibiotics . On the other hand, imidazoles possess significant medicinal applications, such as antibacterial and anti‐inflammatory activities , antifungal activity , antiparasitic activity , antiviral activity , and antidepressant activity . In view of the previous applications, and in continuation of our interest in synthesis of some fused and spiro‐1,5‐benzodiazepinones , we aimed to use 2‐oxo‐4‐phenyl‐2,3‐dihydro‐1 H ‐1,5‐benzodiazepin‐3‐ylimidothiocarbamate ( 2 ) and 1‐(2‐oxo‐4‐phenyl‐2,3‐dihydro‐1 H ‐1,5‐benzodiazepin‐3‐yl)guanidine ( 3 ) as building blocks for the synthesis of some new family of 3‐pyrimidinyl‐ and imidazolyl‐1,5‐benzodiazepines with the hope to possess better antimicrobial activity.…”