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Antimalarial and Other Antiparasitic Drugs
Published in Richard J. Sundberg, The Chemical Century, 2017
As evidence of malaria resistance accumulated, one approach was to use combinations of drugs such as sulfadoxine–pyrimethamine and atovaquone–proguanil.9 Although these treatments can be effective, they require adequate medical infrastructure. Several combinations of artemisinin derivatives are also available. The most widely used is artemether–lumefantrine. It is made by Novartis as Coartem and is part of WHO malaria control programs. Several other drug combinations are available.
Terpenoids Against Infectious Diseases
Published in Dijendra Nath Roy, Terpenoids Against Human Diseases, 2019
Sanhita Ghosh, Kamalika Roy, Chiranjib Pal
Artemisinin, another sesquiterpene lactone, contains a rare endoperoxide bridge that is essential for its anti-malarial activity. Artemisinin is derived from an ancient Chinese herbal remedy and has been isolated from Artemisia annua (sweet wormwood or “Qinghao”), a species of the Asteraceae family. This plant has been used in Chinese herbal medicine for over 200 years (Wang et al. 2005). The discovery of artemisinin dramatically changed the landscape regarding malaria and led to a paradigm shift in anti-malarial drug development. According to a recent World Health Organization report, 97 countries have ongoing malaria transmission, and an estimated 3.4 billion people are at risk of malaria, of whom ~1.2 billion are at high risk (Su and Miller 2015). The good news is that between 2000 and 2012, the malaria incidence rates were reduced by 25% globally, and the global malaria mortality rate was reduced by 42% during the same period (Su and Miller 2015). Many countries are now on track for declaring malaria-free status. According to a recent estimate, approximately 22% of the 663 million averted clinical cases were due to the use of artemisinin combination therapies (Su and Miller 2015). The 2015 Nobel Prize in Physiology or Medicine was conferred upon Professor Youyou Tu for her key contributions to the discovery of artemisinin, which has saved millions of lives and represents one of the significant contributions of China to global health (Su and Miller 2015). Artemisinin and its derivatives have played a key role in reducing malaria-related mortality. Since 1979, several derivatives of artemisinin have been synthesized. Artemisinin, artesunate (oral or parenteral), intramuscular artemether and dihydroartemisinin tablets have all proved to be highly effective, with numbers of successful clinical trials and medical uses. These drugs have now replaced chloroquine and quinine for the treatment of malaria (Li et al. 1994).
Artemisia integrifolia, A. capillaris Components, and Sesquiterpene Lactones
Published in Abu Zahrim Yaser, Poonam Khullar, A. K. Haghi, Green Materials and Environmental Chemistry, 2021
Francisco Torrens, Gloria Castellano
As a result of the Vietnam War, as the North Vietnamese forces were suffering heavily from malaria, they appealed to their ally, China, for help [11]. Many Chinese herbs were tested and attention was drawn to an ancient herbal remedy based on the plant Artemisia annua, which was used by Chinese herbalists for over 1000 years. Peasants in rural areas made a tea from it (via hot, not boiling, H2O) or chewed fresh plants mixed with brown sugar, as a way of treating fevers. A team led by Professor Tu Youyou obtained ART, the active ingredient, by low-temperature (LT) ether extraction; they found the formula C15H22O5 of the white crystals in 1972 and its structure was determined in 1976. The ART (cf. Figure 7.1a) presents relatively short-term potency; because of this, it is not a suitable prophylactic. It also suffers from a lack of H2O solubility. Semisynthetic ARTDs developed to improve its potency were soon in use as antimalarial drugs (e.g., artesunate, Figure 7.1b, artemether, Figure 7.1c). When Plasmodium parasites ingest hemoglobin (Hb) to extract protein for growth, heme groups are freed. Either Haem groups or free Fe2+ attack the peroxide group in ART, resulting in the generation of free radicals (FRs) that attack and kill Plasmodium deoxyribonucleic acid (DNA). The ART was suggested to inhibit enzyme Plasmodium falciparum PfATP6 that is involved in pumping Ca2+ into membrane organelles, which may be a means of its action. Concerns exist about the possible emergence of ART-resistant parasites, which is compounded by the widespread availability of fake ART medications, especially in Southeast Asia, and by people not completing their course of treatment. The ART combination therapy (ACT, via artemether-lumefantrine, artesunate-mefloquine, artesunate-amodiaquine, artesunate-sulphadoxine/pyrimethamine) was endorsed by the World Health Organization (WHO) as a frontline treatment for severe P. falciparum malaria.
Formulation development and characterization of lumefantrine nanosuspension for enhanced antimalarial activity
Published in Journal of Biomaterials Science, Polymer Edition, 2021
Ripalkumar Shah, Tejal Soni, Unnati Shah, B. N. Suhagia, M. N. Patel, Tejas Patel, Gamal A. Gabr, Bapi Gorain, Prashant Kesharwani
Malaria is a life-threatening disease caused by Plasmodium parasites, where the infected carriers, particularly female Anopheles mosquitoes, transmit the infection from person-to-person [1]. According to the estimation by World Health Organization (WHO), 228 million cases of malaria infections were made, where the death penalty was paid by 405,000 numbers of patients in 2018 [2]. This is a common disease in the developing countries and to prevent it, several measures are taken by the governing authorities. The control of this disease is possible with proper treatment following prompt diagnosis. Emergence of need for the treatment of the protozoa, there are several strategies available, from chloroquine to artemisinin-based combination therapies [3,4]. However, quinine categories are found to be unsuccessful due to the uneven dosage schedule and unsatisfactory bioavailability [5]. Additionally, combination of artemether and lumefantrine (LUF) are known to provide better control over the malarial condition [4].
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).