Coptisine, a natural alkaloid from <i>Coptidis Rhizoma</i>, inhibits plasmodium falciparum dihydroorotate dehydrogenase

Li, Lang; Hu, Qian; Wang, Jing‐Yuan; Liu, Zehui; Huang, Jin; Lü, Weiqiang; Huang, Ying

doi:10.1111/cbdd.13197

Cited by 19 publications

(8 citation statements)

References 46 publications

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“…The mechanisms of action of most isolated compounds from the medicinal plants are unclear and/or were only studied in vitro against P. falciparum . This is the case of Coptisine, isolated from Coptis japonica , which exhibits its activity by inhibiting P. falciparum dihydroorotate dehydrogenase, an enzyme required for the synthesis of pyrimidine in the parasite ( Lang et al, 2018 ). The authors reported that the kinetic parameters obtained revealed that coptisine was an uncompetitive inhibitor of the enzyme.…”

Section: Resultsmentioning

confidence: 99%

Studies on Activities and Chemical Characterization of Medicinal Plants in Search for New Antimalarials: A Ten Year Review on Ethnopharmacology

et al. 2021

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Malaria is an endemic disease that affected 229 million people and caused 409 thousand deaths, in 2019. Disease control is based on early diagnosis and specific treatment with antimalarial drugs since no effective vaccines are commercially available to prevent the disease. Drug chemotherapy has a strong historical link to the use of traditional plant infusions and other natural products in various cultures. The research based on such knowledge has yielded two drugs in medicine: the alkaloid quinine from Cinchona species, native in the Amazon highland rain forest in South America, and artemisinin from Artemisia annua, a species from the millenary Chinese medicine. The artemisinin-based combination therapies (ACTs), proven to be highly effective against malaria parasites, and considered as “the last bullet to fight drug-resistant malaria parasites,” have limited use now due to the emergence of multidrug resistance. In addition, the limited number of therapeutic options makes urgent the development of new antimalarial drugs. This review focuses on the antimalarial activities of 90 plant species obtained from a search using Pubmed database with keywords “antimalarials,” “plants” and “natural products.” We selected only papers published in the last 10 years (2011–2020), with a further analysis of those which were tested experimentally in malaria infected mice. Most plant species studied were from the African continent, followed by Asia and South America; their antimalarial activities were evaluated against asexual blood parasites, and only one species was evaluated for transmission blocking activity. Only a few compounds isolated from these plants were active and had their mechanisms of action delineated, thereby limiting the contribution of these medicinal plants as sources of novel antimalarial pharmacophores, which are highly necessary for the development of effective drugs. Nevertheless, the search for bioactive compounds remains as a promising strategy for the development of new antimalarials and the validation of traditional treatments against malaria. One species native in South America, Ampelozyzyphus amazonicus, and is largely used against human malaria in Brazil has a prophylactic effect, interfering with the viability of sporozoites in in vitro and in vivo experiments.

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Section: Resultsmentioning

confidence: 99%

Studies on Activities and Chemical Characterization of Medicinal Plants in Search for New Antimalarials: A Ten Year Review on Ethnopharmacology

et al. 2021

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“…Wangchuk et al [47] carried out phytochemical studies of the aerial parts of Meconopsis simplicifolia (D. Don) Walpers (Papaveraceae), resulting in the isolation of one [48]. Besides, Promchai et al [49] isolated five new oxoprotoberberine alkaloids, miliusacunines A-E (63-67), along with nine known compounds from the leaves and twigs of Miliusa cuneata (Annonaceae).…”

Section: Protoberberine Alkaloidsmentioning

confidence: 99%

Alkaloids from Plants with Antimalarial Activity: A Review of Recent Studies

Uzor

2020

Evidence-Based Complementary and Alternative Medicine

106

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Malaria is one of the major health problems in developing countries. The disease kills a large number of people every year and also affects financial status of many countries. Resistance of the plasmodium parasite, the causative agent, to the existing drugs, including chloroquine, mefloquine, and artemisinin based combination therapy (ACT), is a serious global issue in malaria treatment and control. This warrants an urgent quest for novel compounds, particularly from natural sources such as medicinal plants. Alkaloids have over the years been recognized as important phytoconstituents with interesting biological properties. In fact, the first successful antimalarial drug was quinine, an alkaloid, which was extracted from Cinchona tree. In the present review work, the alkaloids isolated and reported recently (2013 till 2019) to possess antimalarial activity are presented. Several classes of alkaloids, including terpenoidal, indole, bisindole, quinolone, and isoquinoline alkaloids, were identified with a promising antimalarial activity. It is hoped that the reports of the review work will spur further research into the structural modification and/or development of the interesting compounds as novel antimalarial drugs.

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“…Berberine is now already a widely used anti‐bacterial applied in the fight against diseases such as bacteria diarrhoea and fungi infection . Similarly, coptisine (50 μmol/L, 0‐120s) was revealed to reduce S.aureus adhesion and inhibit PfDHODH, an anti‐malarial chemotherapy target . Coptisine (50‐200 μmol/L, 30 minutes) also exhibits anti‐H.pylori effect through the inhibition of urease activity, suggesting coptisine was a promising drug for digestive diseases .…”

Section: Anti‐bacterial Propertymentioning

confidence: 99%

Coptisine fromCoptis chinensisexerts diverse beneficial properties: A concise review

Luo

Deng

et al. 2019

J Cellular Molecular Medi

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Coptisine is a natural small‐molecular compound extracted from Coptis chinensis (CC) with a history of using for thousands of years. This work aimed at summarizing coptisine's activity and providing advice for its clinical use. We analysed the online papers in the database of SciFinder, Web of Science, PubMed, Google scholar and CNKI by setting keywords as ‘coptisine’ in combination of ‘each pivotal pathway target’. Based on the existing literatures, we find (a) coptisine exerted potential to be an anti‐cancer, anti‐inflammatory, CAD ameliorating or anti‐bacterial drug through regulating the signalling transduction of pathways such as NF‐κB, MAPK, PI3K/Akt, NLRP3 inflammasome, RANKL/RANK and Beclin 1/Sirt1. However, we also (b) observe that the plasma concentration of coptisine demonstrates obvious non‐liner relationship with dosage, and even the highest dosage used in animal study actually cannot reach the minimum concentration level used in cell experiments owing to the poor absorption and low availability of coptisine. We conclude (a) further investigations can focus on coptisine's effect on caspase‐1‐involved inflammasome assembling and pyroptosis activation, as well as autophagy. (b) Under circumstance of promoting coptisine availability by pursuing nano‐ or microrods strategies or applying salt‐forming process to coptisine, can it be introduced to clinical trial.

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Coptisine, a natural alkaloid from Coptidis Rhizoma, inhibits plasmodium falciparum dihydroorotate dehydrogenase

Cited by 19 publications

References 46 publications

Studies on Activities and Chemical Characterization of Medicinal Plants in Search for New Antimalarials: A Ten Year Review on Ethnopharmacology

Studies on Activities and Chemical Characterization of Medicinal Plants in Search for New Antimalarials: A Ten Year Review on Ethnopharmacology

Alkaloids from Plants with Antimalarial Activity: A Review of Recent Studies

Coptisine fromCoptis chinensisexerts diverse beneficial properties: A concise review

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