Screening of a library of traditional Chinese medicines to identify anti-malarial compounds and extracts

Nonaka, Motohiro; Murata, Yuho; Takano, Ryo; Han, Yongmei; Kabir, Md. Humayun; Kato, Kentaro

doi:10.1186/s12936-018-2392-4

Cited by 35 publications

(31 citation statements)

References 17 publications

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“…Our in vitro nding of Coptis Rhizome and its bioactive compounds strongly supports a previous report [46]. However, their antimalarial activity showed much lower IC 50 using exactly a similar lot of extract and compounds provided from the same KAMPO library of Toyama University.…”

Section: Discussionsupporting

confidence: 90%

“…The IC 50 difference between the 48 hr and parasite growth from 32 to 46 hrs and, the latter one detects the mature trophozoites and schizonts, respectively [47]. In addition, when we saw the cytotoxicity, berberine showed much lower CC 50 (CC 50 8.3 µM) than the previous one [46]. Other study also reported high levels of cytotoxicity of berberine using murine macrophage (CC 50 27.3 µg/mL) [48], or MCF-7 cell (CC 50 36..91 µg/mL) [49], and 8.75 µg/mL [50].…”

Section: Discussionmentioning

confidence: 70%

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Antimalarial activity of traditional Kampo medicine Coptis Rhizome extract and its major active compounds

Teklemichael

Mizukami

Toume

et al. 2020

Preprint

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Background: The herbal medicine has been a rich source of new drugs exemplified by quinine and artemisinin. In this study, examined a variety of Japanese traditional herbal medicine (Kampo) for their potential antimalarial activities. Methods: We designed a comprehensive screening to identify novel antimalarial drugs from a library of Kampo herbal extracts (n = 120) and related compounds (n=96). The antimalarial activity was initially evaluated in vitro against chloroquine/mefloquine-sensitive (3D7) and -resistant (Dd2) strains of Plasmodium falciparum . The cytotoxicity was also evaluated using primary Adult Mouse Brain cells. After being selected through the first in vitro assay, positive extracts and compounds were examined for possible in vivo antimalarial activity. Results: Out of 120 herbal extracts, Coptis Rhizome showed the highest antimalarial activity (IC 50 1.9 µg/mL of 3D7 and 4.85 µg/mL of Dd2) with a high selectivity index (SI) > 263 (3D7) and > 103 (Dd2). Three major chlorinated compounds (coptisine, berberine, and palmatine) related to Coptis Rhizome also showed antimalarial activities with IC 50 1.1, 2.6, and 6.0 µM (against 3D7) and 3.1, 6.3, and 11.8 µM (against Dd2), respectively. Among them, coptisine chloride exhibited the highest antimalarial activity (IC 50 1.1 µM against 3D7 and 3.1 µM against Dd2) with SI of 37.8 and 13.2, respectively. . Finally, the herbal extract of Coptis Rhizome and its major active compound coptisine chloride exhibited significant antimalarial activity in mice infected with P. yoelii 17X strain with respect to its activity on parasite suppression consistently from day 3 to day 7 post-challenge. The effect ranged from 50.38 to 72.13% (P <.05) for Coptis Rhizome and from 81 to 89% (P <.01) for coptisine chloride. Conclusion: Coptis Rhizome and its major active compound coptisine chloride showed promising antimalarial activity against chloroquine-sensitive (3D7) and -resistant (Dd2) strains in vitro as well as in vivo mouse malaria model. Thus Kampo herbal medicine is a potential natural resource for novel antipathogenic agents.

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Section: Discussionsupporting

confidence: 90%

Section: Discussionmentioning

confidence: 70%

Antimalarial activity of traditional Kampo medicine Coptis Rhizome extract and its major active compounds

Teklemichael

Mizukami

Toume

et al. 2020

Preprint

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“…The antimicrobial activity of coumarins, among which Esculetin and Umbelliferone, has been demonstrated in several studies (45)(46)(47)(48)(49)(50). Palmatine chloride has been recently screened against the causative agent of malaria, the protozoan parasite Plasmodium falciparum, showing strong anti-malarial effects (51). Flavonoids, such as 7-Hydroxyflavone, are naturally produced in plants with antifungal properties (52)(53)(54).…”

Section: Discussionmentioning

confidence: 99%

Comparative Therapeutic Effects of Natural Compounds Against Saprolegnia spp. (Oomycota) and Amyloodinium ocellatum (Dinophyceae)

et al. 2020

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The fish parasites Saprolegnia spp. (Oomycota) and Amyloodinium ocellatum (Dinophyceae) cause important losses in freshwater and marine aquaculture industry, respectively. The possible adverse effects of compounds used to control these parasites in aquaculture resulted in increased interest on the search for natural products with antiparasitic activity. In this work, eighteen plant-derived compounds (2 ′ ,4 ′-Dihydroxychalcone; 7-Hydroxyflavone; Artemisinin; Camphor (1R); Diallyl sulfide; Esculetin; Eucalyptol; Garlicin 80%; Harmalol hydrochloride dihydrate; Palmatine chloride; Piperine; Plumbagin; Resveratrol; Rosmarinic acid; Sclareolide; Tomatine, Umbelliferone, and Usnic Acid) have been tested in vitro. Sixteen of these were used to determine their effects on the gill cell line G1B (ATCC ® CRL-2536 TM) and on the motility of viable dinospores of Amyloodinium ocellatum, and thirteen were screened for inhibitory activity against Saprolegnia spp. The cytotoxicity results on G1B cells determined that only two compounds (2 ′ ,4 ′-Dihydroxychalcone and Tomatine) exhibited dose-dependent toxic effects. The highest surveyed concentrations (0.1 and 0.01 mM) reduced cell viability by 80%. Upon lowering the compound concentration the percentage of dead cells was lower than 20%. The same two compounds revealed to be potential antiparasitics by reducing in a dose-dependent manner the motility of A. ocellatum dinospores up to 100%. With respect to Saprolegnia, a Minimum Inhibitory Concentration was found for Tomatine (0.1 mM), Piperine and Plumbagin (0.25 mM), while 2 ′ ,4 ′-Dihydroxychalcone considerably slowed down mycelial growth for 24 h at a concentration of 0.1 mM. Therefore, this research allowed to identify two compounds, Tomatine and 2 ′ ,4 ′-Dihydroxychalcone, effective against both parasites. These compounds could represent promising candidates for the treatment of amyloodiniosis and saprolegniosis in aquaculture. Nevertheless, further in vitro and in vivo tests are required in order to determine concentrations that are effective against the considered pathogens but at the same time safe for hosts, environment and consumers.

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“…Another antimalarial study in the Plasmodium falciparum 3D7 strain showed that PLT hydrochloride inhibited 99.5% of the growth of the protozoa, with an IC 50 value (SEM) of 26 nM. The antiplasmodial effect was related to the growth inhibition at schizont and trophozoite stages (Nonaka et al, ). In addition, in the studies of Nkwengoua et al (), this compound inhibited the growth of Trypanosoma cruzi and Leishmania infantum (IC 50 = 0.068 and 0.79 μM, respectively).…”

Section: Pharmacology Of Pltmentioning

confidence: 98%

Palmatine: A review of pharmacological properties and pharmacokinetics

Tarabasz¹,

Kukuła-Koch

2019

Phytotherapy Research

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The aim of this review is to collect together the results of the numerous studies over the last two decades on the pharmacological properties of palmatine published in scientific databases like Scopus and PubMed, which are scattered across different publications. Palmatine, an isoquinoline alkaloid from the class of protoberberines, is a yellow compound present in the extracts from different representatives of Berberidaceae, Papaveraceae, Ranunculaceae, and Menispermaceae. It has been extensively used in traditional medicine of Asia in the treatment of jaundice, liver‐related diseases, hypertension, inflammation, and dysentery. New findings describe its possible applications in the treatment of civilization diseases like central nervous system‐related problems. This review intends to let this alkaloid come out from the shade of a more frequently described alkaloid: berberine. The toxicity, pharmacokinetics, and biological activities of this protoberberine alkaloid will be developed in this work.

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Screening of a library of traditional Chinese medicines to identify anti-malarial compounds and extracts

Cited by 35 publications

References 17 publications

Antimalarial activity of traditional Kampo medicine Coptis Rhizome extract and its major active compounds

Antimalarial activity of traditional Kampo medicine Coptis Rhizome extract and its major active compounds

Comparative Therapeutic Effects of Natural Compounds Against Saprolegnia spp. (Oomycota) and Amyloodinium ocellatum (Dinophyceae)

Palmatine: A review of pharmacological properties and pharmacokinetics

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