In Vitro Antiplasmodial, Heme Polymerization, and Cytotoxicity of Hydroxyxanthone Derivatives

Zakiah, Mistika; Syarif, Rul Afiyah; Mustofa, Mustofa; Jumina, Jumina; Fatmasari, Nela; Sholikhah, Eti Nurwening

doi:10.1155/2021/8866681

Cited by 11 publications

(7 citation statements)

References 36 publications

(55 reference statements)

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“…Our research group has been working on anticancer research employing xanthone derivatives since 2010. Several hydroxyxanthone derivatives including 2-hydroxyxanthone, 3-hydroxyxanthone, 1,3-dihydroxyxanthone, 1,6-dihydroxyxanthone, 3,4-dihydroxyxanthone, 3,6-dihydroxyxanthone, 1,3,6-trihydroxyxanthone, 1,5,6-trihydroxyxanthone, 3,4,6-trihydroxyxanthone, and 1,3,8-trihydroxyxanthone have been synthesized in 2010-2021 [118][119][120][121][122][123][124][125][126]. Among them, 3,4,6-trihydroxyxanthone (13) was one of the most active anticancer agents.…”

Section: In Vitro Anticancer Assay Of Xanthone Derivativesmentioning

confidence: 99%

An Update on the Anticancer Activity of Xanthone Derivatives: A Review

et al. 2021

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The annual number of cancer deaths continues increasing every day; thus, it is urgent to search for and find active, selective, and efficient anticancer drugs as soon as possible. Among the available anticancer drugs, almost all of them contain heterocyclic moiety in their chemical structure. Xanthone is a heterocyclic compound with a dibenzo-γ-pyrone framework and well-known to have “privileged structures” for anticancer activities against several cancer cell lines. The wide anticancer activity of xanthones is produced by caspase activation, RNA binding, DNA cross-linking, as well as P-gp, kinase, aromatase, and topoisomerase inhibition. This anticancer activity depends on the type, number, and position of the attached functional groups in the xanthone skeleton. This review discusses the recent advances in the anticancer activity of xanthone derivatives, both from natural products isolation and synthesis methods, as the anticancer agent through in vitro, in vivo, and clinical assays.

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Section: In Vitro Anticancer Assay Of Xanthone Derivativesmentioning

confidence: 99%

An Update on the Anticancer Activity of Xanthone Derivatives: A Review

et al. 2021

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“…These products 1a–m were tested in vitro against chloroquine-sensitive (3D7) and -resistant (FCR3) strains of Plasmodium falciparum . 43 The antiplasmodium activities were presented as mean of IC 50 values.…”

Section: Resultsmentioning

confidence: 99%

Ultrasound-assisted-one-pot synthesis and antiplasmodium evaluation of 3-substituted-isoindolin-1-ones

Mardjan,

Hariadi,

Mustika

et al. 2023

RSC Adv.

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“…It exerted their antimalarial action by preventing hemozoin formation [ 39 ]. For hydroxyxanthone derivatives, 1,6,8-trihydroxyxantone exhibited the antiplasmodial activity and also inhibited heme polymerization [ 40 ].…”

Section: Discussionmentioning

confidence: 99%

Antimalarial potential of compounds isolated from Mammea siamensis T. Anders. flowers: in vitro and molecular docking studies

Chaniad

Chukaew

Payaka

et al. 2022

BMC Complement Med Ther

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Background: The emergence of antimalarial drug resistance encourages the search for new antimalarial agents. Mammea siamensis belongs to the Calophyllaceae family, which is a medicinal plant that is used in traditional Thai preparations. The hexane and dichloromethane extracts of this plant were found to have potent antimalarial activity. Therefore, this study aimed to isolate active compounds from M. siamensis flowers and evaluate their antimalarial potential and their interactions with Plasmodium falciparum lactate dehydrogenase (PfLDH). Methods: The compounds from M. siamensis flowers were isolated by chromatographic techniques and evaluated for their antimalarial activity against chloroquine (CQ)-resistant P. falciparum (K1) strains using a parasite lactate dehydrogenase (pLDH) assay. Interactions between the isolated compounds and the PfLDH enzyme were investigated using a molecular docking method. Results: The isolation produced the following thirteen compounds: two terpenoids, lupeol (1) and a mixture of β-sitosterol and stigmasterol (5); two mammea coumarins, mammea A/AA cyclo D (6) and mammea A/AA cyclo F (7); and nine xanthones, 4,5-dihydroxy-3-methoxyxanthone (2), 4-hydroxyxanthone (3), 1,7-dihydroxyxanthone (4), 1,6-dihydroxyxanthone (8), 1-hydroxy-5,6,7-trimethoxyxanthone (9), 3,4,5-trihydroxyxanthone (10), 5-hydroxy-1-methoxyxanthone (11), 2-hydroxyxanthone (12), and 1,5-dihydroxy-6-methoxyxanthone (13). Compound 9 exhibited the most potent antimalarial activity with an IC50 value of 9.57 µM, followed by 10, 1, 2 and 13 with IC50 values of 15.48, 18.78, 20.96 and 22.27 µM, respectively. The molecular docking results indicated that 9, which exhibited the most potent activity, also had the best binding affinity to the PfLDH enzyme in terms of its low binding energy (-7.35 kcal/mol) and formed interactions with ARG109, ASN140, and ARG171. Conclusion: These findings revealed that isolated compounds from M. siamensis flowers exhibited antimalarial activity. The result suggests that 1-hydroxy-5,6,7-trimethoxyxanthone is a possible lead structure as a potent inhibitor of the PfLDH enzyme.

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In Vitro Antiplasmodial, Heme Polymerization, and Cytotoxicity of Hydroxyxanthone Derivatives

Cited by 11 publications

References 36 publications

An Update on the Anticancer Activity of Xanthone Derivatives: A Review

An Update on the Anticancer Activity of Xanthone Derivatives: A Review

Ultrasound-assisted-one-pot synthesis and antiplasmodium evaluation of 3-substituted-isoindolin-1-ones

Antimalarial potential of compounds isolated from Mammea siamensis T. Anders. flowers: in vitro and molecular docking studies

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