Cryptolepine is the major alkaloidal constituent of the West African climbing shrub Cryptolepis sanguinolenta, a species used in traditional medicine for the treatment of malaria and a number of other infectious diseases. Cryptolepine and a number of its synthetic analogues have been shown to have potent antiplasmodial activities using P. falciparum lactate dehydrogenase assay (PfLDH). Intraery...

Peptide-bond isosteres can enable a deep interrogation of the structure and function of a peptide or protein by amplifying or attenuating particular chemical properties. In this Minireview, the electronic, structural, and conformational attributes of four such isosteres-thioamides, esters, alkenes, and fluoroalkenes-are examined in detail. In particular, the ability of these isosteres to partak...

Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...

Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...

Topoisomerases have been shown to have roles in cancer progression. Here, we have examined the effect of cryptolepine, a plant alkaloid, on the growth of human non-melanoma skin cancer cells (NMSCC) and underlying mechanism of action. For this purpose SCC-13 and A431 cell lines were used as an in vitro model. Our study reveals that SCC-13 and A431 cells express higher levels as well as activity...

Cryptolepine is the major alkaloidal constituent of the West African climbing shrub Cryptolepis sanguinolenta, a species used in traditional medicine for the treatment of malaria and a number of other infectious diseases. Cryptolepine and a number of its synthetic analogues have been shown to have potent antiplasmodial activities using P. falciparum lactate dehydrogenase assay (PfLDH). Intraery...

Colorectal cancer (CRC) is the third most frequent and second leading cause of cancer-related deaths globally. Evidence shows that over 90% CRC cases are initiated by a deregulated Wingless Integrated Type-1 (WNT)/β-catenin signaling pathway. The WNT/β-catenin pathway also promotes cell proliferation, stemness, metastasis. Therefore, modulators may serve as promising regimens for CRC. This stud...

2 4. Kirby GC, Paine A, Warhurst DC, Noamesi BK, Phillipson JD. In vitro and in vivo antimalarial activity of cryptolepine, a plant-derived indoloquinoline. Phytother Res 1995; 9: 359-363 5. Noamesi BK, Paine A, Kirby GC, Warhurst DC, Phillipson JD. In vitro antimalarial activity of cryptolepine, an indoquinoline. Trans Roy Soc Trop Med Hyg 1991; 85:315 6. Boye GL. Studies on antimalarial actio...

RAFT polymerization was used to synthesize urea-bearing methyl methacrylate copolymers for binding carboxylate isosteres.