Selective accumulation of a novel antimalarial rhodacyanine derivative, SSJ-127, in an organelle of Plasmodium berghei

Ikegami-Kawai, Mayumi; Arai, Chika; Ogawa, Yuko; Yanoshita, Ryohei; Ihara, Masataka

doi:10.1016/j.bmc.2010.09.054

Cited by 11 publications

(8 citation statements)

References 10 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The current review provides an overview of a great number of bioactive natural products that have recently been described in the literature (from January 2009 to November 2010) as showing antiplasmodial activity ( in vitro ), along with a few compounds that were tested for antimalarial activity in animal models [ 19 ] using Plasmodium knowlesi (in simians), Plasmodium yoelii , Plasmodium berghei, Plasmodium chabaudi (in mice), and Plasmodium gallinaceum (in birds). In most of these bioassays, antiplasmodial activities were assessed using different P. falciparum strains, which include chloroquine-sensitive (NF54, NF54/64, 3D7, D6, F32, D10, HB3, FCC1-HN, Ghana, MRC-02, TM4), chloroquine-resistant (BHz26/86, Dd2, EN36, ENT30, FcB1, FCM29, FCR3, FCR-3/A2, FCR3F86, S20, W2,), chloroquine-resistant and pyrimethamine-resistant (K1, TM91C235), pyrimethamine-resistant (HB3), cycloguanil-resistant (CDC1), and chloroquine- and antifolate-resistant (K1CB1).…”

Section: Introductionmentioning

confidence: 99%

Antiplasmodial Natural Products

2011

View full text Add to dashboard Cite

Malaria is a human infectious disease that is caused by four species of Plasmodium. It is responsible for more than 1 million deaths per year. Natural products contain a great variety of chemical structures and have been screened for antiplasmodial activity as potential sources of new antimalarial drugs. This review highlights studies on natural products with antimalarial and antiplasmodial activity reported in the literature from January 2009 to November 2010. A total of 360 antiplasmodial natural products comprised of terpenes, including iridoids, sesquiterpenes, diterpenes, terpenoid benzoquinones, steroids, quassinoids, limonoids, curcubitacins, and lanostanes; flavonoids; alkaloids; peptides; phenylalkanoids; xanthones; naphthopyrones; polyketides, including halenaquinones, peroxides, polyacetylenes, and resorcylic acids; depsidones; benzophenones; macrolides; and miscellaneous compounds, including halogenated compounds and chromenes are listed in this review.

show abstract

Section: Introductionmentioning

confidence: 99%

Antiplasmodial Natural Products

2011

View full text Add to dashboard Cite

show abstract

“…Both CQ-sensitive (3D7) and CQ-resistant (7G8 and K1) P. falciparum strains were used. Although other fluorescent compounds have been synthesized and assessed for labelling of P. falciparum towards diagnostics applications, the groups behind these reports had either only used CQ-sensitive P. falciparum strains [ 28 ] or Plasmodium species that is not known to infect humans [ 29 ]. Recently, Loh et al had quantitatively reported uptake of a CQ-BODIPY conjugate by 3D7, 7G8 and K1 strains [ 1 ].…”

Section: Resultsmentioning

confidence: 99%

Near Infrared Fluorophore-Tagged Chloroquine in Plasmodium falciparum Diagnostic Imaging

et al. 2018

View full text Add to dashboard Cite

Chloroquine was among the first of several effective drug treatments against malaria until the onset of chloroquine resistance. In light of diminished clinical efficacy of chloroquine as an antimalarial therapeutic, there is potential in efforts to adapt chloroquine for other clinical applications, such as in combination therapies and in diagnostics. In this context, we designed and synthesized a novel asymmetrical squaraine dye coupled with chloroquine (SQR1-CQ). In this study, SQR1-CQ was used to label live Plasmodium falciparum (P. falciparum) parasite cultures of varying sensitivities towards chloroquine. SQR1-CQ positively stained ring, mature trophozoite and schizont stages of both chloroquine–sensitive and chloroquine–resistant P. falciparum strains. In addition, SQR1-CQ exhibited significantly higher fluorescence, when compared to the commercial chloroquine-BODIPY (borondipyrromethene) conjugate CQ-BODIPY. We also achieved successful SQR1-CQ labelling of P. falciparum directly on thin blood smear preparations. Drug efficacy experiments measuring half-maximal inhibitory concentration (IC50) showed lower concentration of effective inhibition against resistant strain K1 by SQR1-CQ compared to conventional chloroquine. Taken together, the versatile and highly fluorescent labelling capability of SQR1-CQ and promising preliminary IC50 findings makes it a great candidate for further development as diagnostic tool with drug efficacy against chloroquine-resistant P. falciparum.

show abstract

“…Of 28 included articles, all studies belong to in vitro studies, in which four studies are both in vitro and in vivo [39][40][41][42], one in vivo study [41], and none clinical study. A summary of the characteristics of all included studies is presented in Table 1.…”

Section: Characteristics Of Included Studiesmentioning

confidence: 99%

Antimalarial activities of benzothiazole analogs: A systematic review

Tran,

Tu,

Dadam

et al. 2023

Fundamemntal Clinical Pharma

View full text Add to dashboard Cite

BackgroundBenzothiazole derivatives have been reported to possess a wide range of biological activities, including antimalarial activity. This systematic review aims to summarize and evaluate the antimalarial activities of benzothiazole analogs.MethodsWe conducted an electronic search using nine databases in October 2017 and subsequently updated in September 2022. We included all original in vitro and in vivo studies that documented the antimalarial activities of compounds containing benzothiazole analogs with no restriction. The risk of bias of each included study was assessed by ToxRTool.ResultsTwenty‐eight articles were included in our study, which are in vitro, in vivo, or both. Of these, 232 substances were identified to have potent antiplasmodial activity against various strains of the malaria parasite. Benzothiazole analogs show different antimalarial mechanisms, including inhibition of Plasmodium falciparum enzymes in in vitro studies and inhibition of blood parasites in in vivo studies.ConclusionsBenzothiazole derivatives are promising substances for treating malaria. The structure–activity relationship studies suggest that the substitution pattern of the benzothiazole scaffold plays a crucial role in determining the antimalarial activity of the analog.

show abstract

Selective accumulation of a novel antimalarial rhodacyanine derivative, SSJ-127, in an organelle of Plasmodium berghei

Cited by 11 publications

References 10 publications

Antiplasmodial Natural Products

Antiplasmodial Natural Products

Near Infrared Fluorophore-Tagged Chloroquine in Plasmodium falciparum Diagnostic Imaging

Antimalarial activities of benzothiazole analogs: A systematic review

Contact Info

Product

Resources

About