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Africa
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Artemisia and Development of Drugs from Asteraceae
Published in Debarshi Kar Mahapatra, Swati Gokul Talele, Tatiana G. Volova, A. K. Haghi, Biologically Active Natural Products, 2020
Francisco Torrens, Gloria Castellano
Artemisinin was used in Chinese herbal medicine (CHM) for more than 2000 years. The small molecule artesunate, a derivative of Art, was used to treat various kinds of diseases ranging from malaria to RA. The findings broaden the potential application of artesunate, which attenuated subchondral bone deterioration (e.g., suppressing dramatic bone resorption) inhibiting hetero-topic bone formation via interrupting transforming growth factor (TGF)-β signaling and abrogating aberrant blood vessel formation in the subchondral bone in early-stage OA. Specifically, articular cartilage degeneration was alleviated, indicating that maintaining stabilization of subchondral bone microarchitecture in early OA was seen as an effective therapeutic approach. Several limitations were present in this study. Compared to oral administration, intraperitoneal injection is not a considerably more convenient route, especially for those who need to administer repeatedly medications. Although the molecular model indicates the artesunate-receptor activator of NF-κB (RANK) and -TGF-β receptor-I interactions, the effect needs to be further demonstrated by transgenic and knock-out/in models.
Click synthesis of new 7-chloroquinoline derivatives by using ultrasound irradiation and evaluation of their biological activity
Published in Green Chemistry Letters and Reviews, 2018
Asmaa Aboelnaga, Taghreed H. EL-Sayed
Quinolines and their derivatives are present in numerous natural products and have highly antimalaria, antiasthmatic, antiinflammatory, antibacterial and antihypersensitive activities (1). Few methods have been reported for the preparation of quinolines derivatives such as the Skraup, Doebner von Miller and Combes procedures (2, 3). Malaria is a contagious disease, caused by protozoa parasites from the genus Plasmodium that is transmitted by mosquitoes of the genus Anopheles. Plasmodium falciparum is responsible for the most lethal form of malaria (4). Chloroquine was the most effective antimalarial clinically used drug but parasite resistance led to its substitution by artemisinin and its semi-synthetic derivatives (artemether, artesunate) (5, 6). So, new drugs to treat malaria are critically required. Synthesis of molecular hybrids containing different moieties which are representatives of known or putative antimalarial compounds is presently being extensively explored. Recently, the synthesis of 1,2,3-triazoles by a process known as Cu-mediated click chemistry (7) has been explored to combine different molecules affording new analogs of chloroquine (8), chalcones (9), naphthoquinones (10) several other hybrid antimalarial molecules have been synthesized (11–13).
Design of artificial cells: artificial biochemical systems, their thermodynamics and kinetics properties
Published in Egyptian Journal of Basic and Applied Sciences, 2022
Adamu Yunusa Ugya, Lin Pohan, Qifeng Wang, Kamel Meguellati
Munshaw group work on a fully rational synthetic HCV subtype 1a virus (Bole1a) was designed by Bayesian phylogenetics, covariance analysis, and ancestral sequence reconstruction comprising mainly of 338 epitopes and envelope genes assembled and mediated in the entry into the target cells [60]. The intracellular incorporation of synthetic enhancers can help in the generation of viruses with novel properties and is also a good example cited in the construction of artificial cells [61]. Cottingham and his coworkers’ study is based on the clinically deployable viral vector by proof-of-concept experiments, modified Vaccinia virus Ankara bacterial artificial chromosomes (MVA-BCA), and it is found to be an effective new candidate for mutant and recombinant vaccines [62]. The construction of synthetic CMV promoters of all strengths was carried out by a 10-mer synthetic enhancer spacer [63]. A new approach for the treatment of DENV infection in humans is based on improving the nucleic acid inhibitors of the Dengue virus (DENV) by RNAi (RNA interference) based on multiple artificial microRNAs (amiRNAs) that target the conserved regions of the virus [64]. The few studies on artificial cells mimicking bacteria report the construction of Artesimisin artesunate (ARS), a synthetic tetraxane drug candidate (RKA182) and a trioxolane equivalent (FBEG100), which have been used as an efficient drug for the treatment of P. falciparum malaria [65]. Kissner and his group produced a synthetic dimeric BB-loop mimetic of MyD88 (EM-163) that inhibited pro-inflammatory signaling and was found to be toxic to Staphylococcal enterotoxin B therapeutically [66].