Evaluation of the in vitro trypanocidal activity of plant extracts from the Brazilian Cerrado

Cunha, WR; Santos, FM Dos; Peixoto, JA; Veneziani, Rcs; Crotti, Aem; Silva, Mla; Filho, AA Da Silva; Turatti, Icc; Bastos, Jairo K.; Albuquerque, S.

doi:10.1055/s-0029-1234485

Cited by 2 publications

(7 citation statements)

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“…The presence of a ketone or the double bond shift also induced a significant activity decrease, as observed for ursonic ( 3 ), 18β‐glycyrrhetinic ( 4 ) and morolic ( 5 ) acids [19] . Similarly, 1 a with a keto function at C3, was reported to lose the antitrypanosomal activity for T. cruzi parasites [20] . For oleanane derivatives, the activity decrease was also associated with a reduction in selectivity.…”

Section: Resultsmentioning

confidence: 82%

“…Cunha et al . reported a loss in activity against T. cruzi of both 1 a and 2 a after acetylation [20] . As for the sleeping sickness parasite, single C3 acetylation decreased the activity on T. cruzi trypomastigotes compared to unesterified acids, with 1 a also being the most active derivative.…”

Section: Resultsmentioning

confidence: 97%

“…The importance of the hydroxylic group at C3 has been reported for the antitrypanosomal action for both 1 a and 2 a and the ursane‐ and oleanane‐type pentacyclic triterpenes [21] . A clear counteracting of anti‐ T. bb activity loss happens when the adjacent carbon, C4, is substituted with a polar group [20] . This indicates that the substituent's nature and orientation effect on the activity might depend on parasite strain as demonstrated for a tri‐esterified oleanane derivative, 3β‐acetoxy‐27‐trans‐caffeoyloxyolean‐12‐en‐28‐oic acid methyl ester.…”

Section: Resultsmentioning

confidence: 99%

“…Cunha et al reported a loss in activity against T. cruzi of both 1 a and 2 a after acetylation. [20] As for the sleeping sickness parasite, single C3 acetylation decreased the activity on T. cruzi trypomastigotes compared to unesterified acids, with 1 a also being the most active derivative. The number and position of polar groups affect antitrypanosomal activities, potentially due to steric hindrance and modified conformation.…”

Section: In Vitro Antiprotozoal Evaluation and Structural Effects On ...mentioning

confidence: 97%

“…[19] Similarly, 1 a with a keto function at C3, was reported to lose the antitrypanosomal activity for T. cruzi parasites. [20] For oleanane derivatives, the activity decrease was also associated with a reduction in selectivity. The importance of the hydroxylic group at C3 has been reported for the antitrypanosomal action for both 1 a and 2 a and the ursane-and oleanane-type pentacyclic triterpenes.…”

Section: In Vitro Antiprotozoal Evaluation and Structural Effects On ...mentioning

confidence: 99%

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Design, Synthesis and Biological Activity of C3 Hemisynthetic Triterpenic Esters as Novel Antitrypanosomal Hits

et al. 2021

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Research for innovative drugs is crucial to contribute to parasitic infections control and eradication. Inspired by natural antiprotozoal triterpenes, a library of 12 hemisynthetic 3‐ O ‐arylalkyl esters was derived from ursolic and oleanolic acids through one‐step synthesis. Compounds were tested on Trypanosoma , Leishmania and the WI38 cell line alongside with a set of triterpenic acids. Results showed that the triterpenic C3 esterification keeps the antitrypanosomal activity (IC 50 ≈1.6–5.5 μ m ) while reducing the cytotoxicity compared to parent acids. Unsaturation of the ester alkyl chain leads to an activity loss interestingly kept when a sterically hindered group replaces the double bond or shields the ester group. An ursane/oleanane C3 hydroxylation was the only important feature for antileishmanial activity. Two candidates, dihydrocinnamoyl and 2‐fluorophenylpropionyl ursolic acids, were tested on an acute mouse model of African trypanosomiasis with significant parasitemia reduction at day 5 post‐infection for the dihydrocinnamoyl derivative. Further evaluation on other alkyl/protective groups should be investigated both in vitro and in vivo .

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Section: Resultsmentioning

confidence: 82%

Section: Resultsmentioning

confidence: 97%

Section: Resultsmentioning

confidence: 99%

Section: In Vitro Antiprotozoal Evaluation and Structural Effects On ...mentioning

confidence: 97%

Section: In Vitro Antiprotozoal Evaluation and Structural Effects On ...mentioning

confidence: 99%

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Design, Synthesis and Biological Activity of C3 Hemisynthetic Triterpenic Esters as Novel Antitrypanosomal Hits

et al. 2021

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In Vitro Screening for Antitrypanosomal Potentials of Punica granatum L. Leaves Crude Extracts

Fathuddin,

Inabo

2024

Preprint

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Punica granatum L. leaves were examined for potential antitrypanosomal properties. These leaves were acquired and identified at Ahmadu Bello University (ABU) Herbarium Unit in Zaria. Following drying, the following solvents—chloroform, ethyl acetate, and ethanol—were used for exhaustive Soxhlet extraction. The crude extracts phytochemical analysis and in vitro antitrypanosomal capability was performed on Trypanosoma brucei brucei, obtained from The National Research Institute for Chemical Technology (NARICT), Basawa, Zaria. In 96-round-bottom-well microtiter plates, the in vitro trypanocide activity was evaluated in duplicate. Wet and thick blood film and rapid matching were used to examine the antitrypanosomal activity under 400x magnification. The antitrypanosomal activity was determined using the chloroform, ethanol and ethyl acetate extracts ranging from 006.25 to 400.00 mg/ml. The red blood cells (RBCs) were lysed at all concentrations between 200.00 and 400.00 mg/ml, while between 006.25 and 100.00 mg/ml, the RBCs were relatively intact. It was observed that as concentrations declined, the parasite's motility decreased. The parasite's motility entirely stopped after 60 minutes, whereas it continued for an additional 80 minutes in the negative control. A standard drug that was made per the manufacturer's instructions and used as the positive control which cleared everything in less than a minute. Accordingly, the chloroform extract despite lysing the RBC, did not affect the parasite and did not kill it. At a minimum concentration of 6.25 mg/ml, the Punica granatum L. ethyl acetate and ethanol extract can potentially operate as antitrypanosomal agents. This research may help in the development of novel antitrypanosomal medications from Punica granatum L.

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Evaluation of the in vitro trypanocidal activity of plant extracts from the Brazilian Cerrado

Cited by 2 publications

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Design, Synthesis and Biological Activity of C3 Hemisynthetic Triterpenic Esters as Novel Antitrypanosomal Hits

Design, Synthesis and Biological Activity of C3 Hemisynthetic Triterpenic Esters as Novel Antitrypanosomal Hits

In Vitro Screening for Antitrypanosomal Potentials of Punica granatum L. Leaves Crude Extracts

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