In vivo evaluation of isolated triterpenes and semi-synthetic derivatives as antimalarial agents

Silva, Luiz Francisco Rocha e; Ramalhete, Cátia; Nogueira, Karla Lagos; Mulhovo, Silva; Ferreira, Maria‐José U.; Pohlit, Adrian Martin

doi:10.1016/j.ejmech.2015.08.022

Cited by 23 publications

(3 citation statements)

References 30 publications

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“…Karavoate B (19) exhibited a significant suppression of parasitaemia (58.1%) in mice infected with P. berghei when a dose of 50 mg kg -1 day -1 was administered by sub-cutaneous route (Rocha e Silva et al 2015). When comparing the average survival times of untreated and treated animals with compounds, similar results were observed, which might be explained by the incomplete suppression of parasitaemia or rapid metabolism/excretion of compounds by the animals (Rocha e Silva et al 2015). No signs of toxicity were observed, thus corroborating the in vitro results of these compounds against MCF-7 and Huh-7 cells (Ramalhete et al 2011b(Ramalhete et al , a, 2014Rocha e Silva et al 2015).…”

Section: P-glycoprotein Modulation Activitysupporting

confidence: 69%

Momordica balsamina: phytochemistry and pharmacological potential of a gifted species

et al. 2022

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Momordica balsamina L. (Cucurbitaceae), frequently named balsam apple, southern balsam pear or African pumpkin, is a vegetable with high nutritional value, being mostly used as food in sub-Saharan Africa. It has also been largely used in traditional medicine to treat several diseases, such as malaria fevers and diabetes. As a member of the Cucurbitaceae family, the main constituents are cucurbitane-type triterpenoids, with different oxidation patterns, named cucurbitacins. This review aims at summarizing our contribution to the phytochemical study of M. balsamina and the evaluation of the isolated cucurbitacins and derivatives as multidrug resistance reversers in cancer cells and bacteria. In this way, the selective antiproliferative activity against multidrug resistant cancer cells of cucurbitacins obtained from M. balsamina, their ability as P-glycoprotein inhibitors in cancer cells overexpressing this ABC transporter, as well as efflux pump inhibitors in resistant bacteria strains are reviewed. Moreover, the in vitro antimalarial activity of cucurbitacins and acyl derivatives against the blood and liver-stages of Plasmodium strains, and the in vivo activity of selected compounds is also reviewed. Besides our work, edible and medicinal uses, and other studies mainly reporting the biological activities of M. balsamina extracts, such as antidiabetic, antibacterial, anti-inflammatory, and antioxidant properties are also addressed.

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Section: P-glycoprotein Modulation Activitysupporting

confidence: 69%

Momordica balsamina: phytochemistry and pharmacological potential of a gifted species

et al. 2022

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“…Derivatives exhibited sub-micromolar IC 50 in vitro against P. falciparum strains and exhibited greater in vivo antimalarial activity. Orally and subcutaneously administered karavoate B exhibited the greatest in vivo antimalarial activity (55.2-58.1% maximal suppression of parasitemia at doses of 50 mg/kg/day) [94].…”

Section: Isoprenoids In Plasmodium Sppmentioning

confidence: 96%

Terpenes as Potential Antimalarial Drugs

Gabriel¹,

Sussmann²,

Kimura³

et al. 2018

Terpenes and Terpenoids

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A fact which favors the increase in morbidity and mortality of malaria cases in the world is the resistance to chemotherapeutic agents that the parasite presents. Therefore, it is necessary to identify new potential targets specific to the parasite in order to be able to perform a rational planning. One target for the evaluation of potential antimalarial compounds is isoprenoid synthesis, which occurs via the 2-C-methyl-d-erythritol-4-phosphate pathway in Plasmodium falciparum. Several intermediaries and final products of this pathway were identified in the parasite and lead us to the conclusion that it is different from the vertebrate host. In this chapter, we describe the effect of some monoterpenes and sesquiterpenes on Plasmodium falciparum and Plasmodium berghei as potential antimalarial drugs.

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“…Unfortunately, the precise mechanism of action is currently unexplained. The possible mechanism of triterpenoids as antimalarial action includes their impacts on mitochondrial membrane potential and the reduction of β-haematin synthesis [31][32][33]. Triterpenoid (betulinic acid) antimalarial activity is assumed to be related to its ability to engage the PfATP6 protein, which regulates calcium ion transportation and affects the host-parasite selectivity [34].…”

Section: Evaluation Of Inhibition Rate Percentage and Ic50mentioning

confidence: 99%

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2023

J. Med. Chem. Sci.

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Background: Malaria resistance to artemisinin combination therapy has prompted researchers to explore anti-plasmodium materials. One of the marine biotas thought to have the potential to inhibit the development of malaria parasites (Plasmodium sp) are black trepang and curryfish. These two marine biotas consist of two varieties of sea cucumbers with various therapeutic benefits. However, their antimalarial effects have not been studied. Objective: Two marine biotas, black trepang and curryfish extract, were analyzed using in vitro screening to determine their antimalarial activity. Methods: The experiment was done through in vitro screening technique (culture medium containing P. falciparum). P1 was a negative control; P2 was a positive control/using chloroquine as an antimalarial; P3 was a group that received black trepang extract) and P4 was a group that received curryfish extract. Measurements of parasitemia levels, growth percentage, inhibition rate, and IC50 were performed to determine the antimalarial activity. Results: The antimalarial results suggest that increasing the dose of marine biota extract reduces the parasite development rate and increases the inhibition rate. In line with IC50 analysis, both marine biotas have high antimalarial activity. Curryfish extract has a lower IC50 value than black trepang extract. Conclusion:The study demonstrated that black trepang and curry fish have high antimalarial activity.

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In vivo evaluation of isolated triterpenes and semi-synthetic derivatives as antimalarial agents

Cited by 23 publications

References 30 publications

Momordica balsamina: phytochemistry and pharmacological potential of a gifted species

Momordica balsamina: phytochemistry and pharmacological potential of a gifted species

Terpenes as Potential Antimalarial Drugs

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