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In vitro antiplasmodium and chloroquine resistance reversal effects of mangostin

Aim/Background: Chloroquine (CQ) resistance that appeared among different strains of Plasmodium falciparum is considered as the worst catastrophe in the realm of malaria chemotherapy. CQ is still the most favorable drug among other antimalarials especially in the poor endemic areas due to its high p...

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Principais autores: Ibraheem, Zaid Osamah, Abdul Majid, Roslaini, Alapid, Ashraf, Mohammad Sedik, Hasidah, Md Noor, Sabariah, Faruq, Mohammad, Chin, Voon Kin, Basir, Rusliza
Formato: Atigo
Idioma:English
Publicado em: Medknow Publications 2020
Acesso em linha:http://psasir.upm.edu.my/id/eprint/89329/1/VITRO.pdf
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spelling oai:psasir.upm.edu.my:89329 http://psasir.upm.edu.my/id/eprint/89329/ In vitro antiplasmodium and chloroquine resistance reversal effects of mangostin Ibraheem, Zaid Osamah Abdul Majid, Roslaini Alapid, Ashraf Mohammad Sedik, Hasidah Md Noor, Sabariah Faruq, Mohammad Chin, Voon Kin Basir, Rusliza Aim/Background: Chloroquine (CQ) resistance that appeared among different strains of Plasmodium falciparum is considered as the worst catastrophe in the realm of malaria chemotherapy. CQ is still the most favorable drug among other antimalarials especially in the poor endemic areas due to its high potency and cost-effectiveness. This urged the scientists to explore for other alternatives or sensitizers for CQ. Materials and Methods: In this experiment, the antiplasmodium and the CQ resistance reversing effects of mangostin were tested using the in vitro SYBRE green-1-based drug sensitivity assay and the isobologram technique, respectively. Furthermore, its safety level toward two types of mammalian cells, namely Vero cells and red blood cells (RBCs), was screened using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide-based drug sensitivity and the RBCs hemolysis assays, respectively. On the other hand, its effect against hemozoin formation was screened using β-hematin formation. Meanwhile, its molecular characters were determined the in silico on-line free chemi-informatic Molinspiration software for the molecular characterization as well as the standard testes for the measurement of the antioxidant effect. Results: Mangostin was moderately effective and selective toward the plasmodium so it is unsuitable to be a substituent for CQ. But it improved the sensitivity of the parasite to CQ. The molecular elucidation suggests that its CQ resistance reversal effect can be ascribed to its ability to interfere with hemozoin formation or the intravacuolar accumulation of CQ. Conclusion: Overall, the study suggests mangostin as a possible pharmacophore to develop new CQ resistance reversing agents but further studies are recommended to confirm this notion. Medknow Publications 2020 Article PeerReviewed text en http://psasir.upm.edu.my/id/eprint/89329/1/VITRO.pdf Ibraheem, Zaid Osamah and Abdul Majid, Roslaini and Alapid, Ashraf and Mohammad Sedik, Hasidah and Md Noor, Sabariah and Faruq, Mohammad and Chin, Voon Kin and Basir, Rusliza (2020) In vitro antiplasmodium and chloroquine resistance reversal effects of mangostin. Pharmacognosy Magazine, 16 (70). 276 - 283. ISSN 0973-1296; ESSN: 0976-4062 https://www.phcog.com/article.asp?issn=0973-1296;year=2020;volume=16;issue=70;spage=276;epage=283;aulast=Ibraheem 10.4103/pm.pm_510_19
institution UPM IR
collection UPM IR
language English
description Aim/Background: Chloroquine (CQ) resistance that appeared among different strains of Plasmodium falciparum is considered as the worst catastrophe in the realm of malaria chemotherapy. CQ is still the most favorable drug among other antimalarials especially in the poor endemic areas due to its high potency and cost-effectiveness. This urged the scientists to explore for other alternatives or sensitizers for CQ. Materials and Methods: In this experiment, the antiplasmodium and the CQ resistance reversing effects of mangostin were tested using the in vitro SYBRE green-1-based drug sensitivity assay and the isobologram technique, respectively. Furthermore, its safety level toward two types of mammalian cells, namely Vero cells and red blood cells (RBCs), was screened using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide-based drug sensitivity and the RBCs hemolysis assays, respectively. On the other hand, its effect against hemozoin formation was screened using β-hematin formation. Meanwhile, its molecular characters were determined the in silico on-line free chemi-informatic Molinspiration software for the molecular characterization as well as the standard testes for the measurement of the antioxidant effect. Results: Mangostin was moderately effective and selective toward the plasmodium so it is unsuitable to be a substituent for CQ. But it improved the sensitivity of the parasite to CQ. The molecular elucidation suggests that its CQ resistance reversal effect can be ascribed to its ability to interfere with hemozoin formation or the intravacuolar accumulation of CQ. Conclusion: Overall, the study suggests mangostin as a possible pharmacophore to develop new CQ resistance reversing agents but further studies are recommended to confirm this notion.
format Article
author Ibraheem, Zaid Osamah
Abdul Majid, Roslaini
Alapid, Ashraf
Mohammad Sedik, Hasidah
Md Noor, Sabariah
Faruq, Mohammad
Chin, Voon Kin
Basir, Rusliza
spellingShingle Ibraheem, Zaid Osamah
Abdul Majid, Roslaini
Alapid, Ashraf
Mohammad Sedik, Hasidah
Md Noor, Sabariah
Faruq, Mohammad
Chin, Voon Kin
Basir, Rusliza
In vitro antiplasmodium and chloroquine resistance reversal effects of mangostin
author_facet Ibraheem, Zaid Osamah
Abdul Majid, Roslaini
Alapid, Ashraf
Mohammad Sedik, Hasidah
Md Noor, Sabariah
Faruq, Mohammad
Chin, Voon Kin
Basir, Rusliza
author_sort Ibraheem, Zaid Osamah
title In vitro antiplasmodium and chloroquine resistance reversal effects of mangostin
title_short In vitro antiplasmodium and chloroquine resistance reversal effects of mangostin
title_full In vitro antiplasmodium and chloroquine resistance reversal effects of mangostin
title_fullStr In vitro antiplasmodium and chloroquine resistance reversal effects of mangostin
title_full_unstemmed In vitro antiplasmodium and chloroquine resistance reversal effects of mangostin
title_sort in vitro antiplasmodium and chloroquine resistance reversal effects of mangostin
publisher Medknow Publications
publishDate 2020
url http://psasir.upm.edu.my/id/eprint/89329/1/VITRO.pdf
_version_ 1819300327650754560
score 13.4562235

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