Anti-malarial activity of traditional Kampo medicine Coptis rhizome extract and its major active compounds

Teklemichael, Awet Alem; Mizukami, Shusaku; Toume, Kazufumi; Mosaddeque, Farhana; Kamel, Mohamed Gomaa; Kaneko, O.; Komatsu, Kenshi; Karbwang, Juntra; Huy, Nguyen Tien; Hirayama, Kenji

doi:10.1186/s12936-020-03273-x

Cited by 17 publications

(31 citation statements)

References 49 publications

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“…To overcome such bottle-neck, it is important to start the process of isolation of compounds using large amount of plant materials. The isolated compounds evaluated for in vivo antimalarial activities were: 1) Coptisine Chloride from Coptis japonica , ( Teklemichael et al, 2020 ); 2) 4-Nerolidylcatechol isolated from Piper peltatum ( Rocha e Silva et al, 2011 ); and 3) Myristic Acid and β-Caryophyllene from Murraya koenigii ( Kamaraj et al, 2014 ) ( Tables 2, 3 ).…”

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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“…In the course of identifying the responsible bioactive compound in the crude drug materials used in the traditional medicine [23][24][25], we focused on the leaves of M. morindoides. Both in vitro and in vivo antimalarial activity of the leaf extract of this plant have been reported [9,26].…”

Section: Introductionmentioning

confidence: 99%

Phenylpropanoid conjugated iridoids with anti-malarial activity from the leaves of Morinda morindoides

et al. 2021

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Two phenylpropanoid conjugated iridoids, deglucosyl gaertneroside (1) and morindoidin (2), were isolated from the leaves of Morinda morindoides (Rubiaceae) by activity-guided fractionation using an anti-malarial activity assay. The known related iridoids molucidin (3) and prismatomerin (4), two lignans, abscisic acid, two megastigmanes, and two avonol glycosides were also identi ed. The structures of isolated compounds were elucidated using spectroscopic analysis. The isolated compounds were evaluated for anti-malarial activity against the chloroquine/me oquine-sensitive strains of Plasmodium falciparum together with cytotoxicity against adult mouse brain cells. Potent anti-malarial activity of and 4 (IC 50 of 0.96 and 0.80 µM, respectively) was shown, while new iridoids 1 and 2 and pinoresinol (5) displayed moderate activity (IC 50 of 40.9, 20.6, and 24.2 µM, respectively). These results indicate that 1-5 may be promising lead compounds for anti-malarial drugs and that extracts of M. morindoides leaves could be effective remedies for malaria infection.

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“…Natural compounds represent a major source for drug development [ 13 , 14 , 15 ]. Rhein (4,5-dihydroxyanthraquinone-2-carboxylic acid) is a natural anthraquinone found in several medicinal plants [ 16 ], particularly in rhubarb [ 17 ].…”

Section: Introductionmentioning

confidence: 99%

Rhein Suppresses Colorectal Cancer Cell Growth by Inhibiting the mTOR Pathway In Vitro and In Vivo

Zhang

Yi²,

Huang

et al. 2021

Cancers

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Colorectal cancer (CRC) is one of the leading causes of mortality and morbidity in the world. Rhein has demonstrated therapeutic effects in various cancer models. However, its effects and underlying mechanisms of action in CRC remain poorly understood. We investigated the potential anticancer activity and underlying mechanisms of rhein in CRC in vitro and in vivo. Cell viability and anchorage-independent colony formation assays were performed to examine the antigrowth effects of rhein on CRC cells. Wound-healing and Transwell assays were conducted to assess cell migration and invasion capacity. Cell cycle and apoptosis were investigated by flow cytometry and verified by immunoblotting. A tissue microarray was used to detect mTOR expression in CRC patient tissues. Gene overexpression and knockdown were done to analyze the function of mTOR in CRC. The anticancer effect of rhein in vivo was assessed in a CRC xenograft mouse model. The results show that rhein significantly inhibited CRC cell growth by inducing S-phase cell cycle arrest and apoptosis. Rhein inhibited CRC cell migration and invasion through the epithelial–mesenchymal transition (EMT) process. mTOR was highly expressed in CRC cancer tissues and cells. Overexpression of mTOR promoted cell growth, migration, and invasion, whereas mTOR knockdown diminished these phenomena in CRC cells in vitro. In addition, rhein directly targeted mTOR and inhibited the mTOR signaling pathway in CRC cells. Rhein promoted mTOR degradation through the ubiquitin-proteasome pathway. Intraperitoneal administration of rhein inhibited HCT116 xenograft tumor growth through the mTOR pathway. In conclusion, rhein exerts anticancer activity in vitro and in vivo by targeting mTOR and inhibiting the mTOR signaling pathway in CRC. Our results indicate that rhein is a potent anticancer agent that may be useful for the prevention and treatment of CRC.

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Anti-malarial activity of traditional Kampo medicine Coptis rhizome extract and its major active compounds

Cited by 17 publications

References 49 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

Phenylpropanoid conjugated iridoids with anti-malarial activity from the leaves of Morinda morindoides

Rhein Suppresses Colorectal Cancer Cell Growth by Inhibiting the mTOR Pathway In Vitro and In Vivo

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