Antiparasitic dibenzalacetone inhibits the GTPase activity of Rab6 protein of Leishmania donovani (LdRab6), a potential target for its antileishmanial effect

Chauhan, Indira Singh; Marwa, Simran; Rao, Gita Subba; Singh, Neeloo

doi:10.1007/s00436-020-06810-4

Cited by 18 publications

(4 citation statements)

References 35 publications

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“…Finally, pharmacokinetic studies in animals and humans are needed as the DBAs (the present study and Chauhan et al., 2020 ) progress to in vivo phase to establish route and dosage for potential treatment of trypanosomiasis and leishmaniasis. Based on the in vitro results, the following comments may be made regarding this: (i) DBA 1 compared favorably under in vitro conditions to antileishmanial drug miltefosine which is orally effective ( Chauhan et al., 2018 ); (ii) based on the current use of DBA 1 as a sunscreen agent, its topical application in treating parasitic diseases has been suggested ( Chauhan et al., 2020 ); and (iii) in addition to oral dosing similar to BZ (for CD) and miltefosine (for visceral leishmaniasis), diveratralacetone should also be amenable to topical administration; such topical ointments containing turmeric and CUR are commonly used in herbal medical practice ( Cheraghipour et al., 2018 ).…”

Section: Discussionmentioning

confidence: 99%

In vitro anti-Trypanosoma cruzi activity enhancement of curcumin by its monoketone tetramethoxy analog diveratralacetone

Souza

Vieira

Cândido

et al. 2021

Current Research in Parasitology & Vector-Borne Diseases

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Section: Discussionmentioning

confidence: 99%

In vitro anti-Trypanosoma cruzi activity enhancement of curcumin by its monoketone tetramethoxy analog diveratralacetone

Souza

Vieira

Cândido

et al. 2021

Current Research in Parasitology & Vector-Borne Diseases

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“…In 2019, the same authors found that the Ldrab6 gene provides L. donovani with resistance via a mechanism of drug-thiol conjugation and sequestration by ABC transporter multidrugresistant protein A (MRPA) [56]. Further mechanistic studies carried out by the same group indicated that compound 1 can inhibit the GTPase activity of L. donovani Rab6 protein (LdRab6), thereby suggesting that this protein can be a potential target of compound 1 [57].…”

Section: Antiparasitic Activitymentioning

confidence: 99%

Monoketone Curcuminoids: An Updated Review of Their Synthesis and Biological Activities

Vieira,

Tanajura,

Heleno

et al. 2024

Future Pharmacology

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Curcumin (or diferuloylmethane), a component of Curcuma longa L. rhizomes, displays various biological and pharmacological activities. However, it is poorly bioavailable and unstable in physiological pH. In this review, we cover papers published between 2019 and 2023 on the synthesis and biological activities of more stable and effective curcumin analogs known as monoketone curcuminoids (MKCs) or “monocarbonyl curcuminoids.” Recent advances in Claisen–Schmidt condensation, the standard procedure to synthesize MKCs, including the use of ionic liquids, are addressed. MKCs’ antimicrobial, anticancer, antioxidant, and antiparasitic actions, as well as other less common MKC biological and pharmacological activities, have been shown to be similar or higher than curcumin. The promising biological and pharmacological activities, combined with the attractive synthetic aspects (e.g., good yields and an easiness of product isolation) to obtain MKCs, make this class of compounds an interesting prospect for further antimicrobial, anticancer, and antiparasitic drug discovery.

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“…In 2019, the same authors found that the Ldrab6 gene provides L. donovani with resistance via a mechanism of drug-thiol conjugation and sequestration by ABC transporter multidrug resistance-protein A (MRPA) [53]. Further mechanistic studies carried out by the same group indicated that compound 1 can inhibit the GTPase activity of L. donovani Rab6 protein (LdRab6), thereby suggesting that this protein can be a potential target of compound 1 [54].…”

Section: Antiparasitic Activitymentioning

confidence: 99%

Monoketone Curcuminoids: An Updated Review of Their Synthesis and Biological Activities

Vieira,

Tanajura,

Heleno

et al. 2023

Preprint

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Curcumin [1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadien-3,5-dione], a component of Curcuma longa L. rhizomes, displays various biological and pharmacological activities. However, it is poorly bioavailable and unstable in physiological pH, which has led more stable and effective curcumin analogs (e.g., monoketone curcuminoids, or MKCs) to be synthesized, and their biological activities to be described. In this review, we cover papers published between 2019 and 2023 on the antimicrobial, anticancer, antioxidant, and antiparasitic actions as well as other less common MKC biological and pharmacological activities. We also address the Claisen-Schmidt condensation as a standard procedure to synthesize MKCs.

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Antiparasitic dibenzalacetone inhibits the GTPase activity of Rab6 protein of Leishmania donovani (LdRab6), a potential target for its antileishmanial effect

Cited by 18 publications

References 35 publications

In vitro anti-Trypanosoma cruzi activity enhancement of curcumin by its monoketone tetramethoxy analog diveratralacetone

In vitro anti-Trypanosoma cruzi activity enhancement of curcumin by its monoketone tetramethoxy analog diveratralacetone

Monoketone Curcuminoids: An Updated Review of Their Synthesis and Biological Activities

Monoketone Curcuminoids: An Updated Review of Their Synthesis and Biological Activities

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