Favourable physicochemical properties of an organometallic ferrocene and antiplasmodial potency of compounds containing the thiazolidine‐2,4‐dione framework (TZD‐4) prompted us to explore compounds containing both the thiazolidine‐2,4‐dione core and the ferrocenyl unit with the primary aim of identifying compounds with promising antiprotozoal activities. Thus, a new series of rationally designed ferrocene‐based thiazolidine‐2,4‐dione derivatives, containing a selection of secondary cyclic amines, was synthesised and fully characterised using standard spectroscopic techniques. The resulting compounds were screened for their antiplasmodial and antitrypanosomal activities against both the chloroquine‐resistant (Dd2) strain of Plasmodium falciparum and the Nagana Trypanosoma brucei brucei 427. The general trend that emerged indicated that the target compounds were more selective towards T. b. brucei compared to the P. falciparum parasite. Moreover, the analogues bearing methylpiperazine (8a) and piperidine (8b) rings were more active against T. b. brucei compared to hit compound TZD‐4. Except compound 8b, which appeared promising, none of the synthesised compounds showed better activity than TZD‐4 against the P. falciparum parasite. All the synthesised compounds were non‐toxic and often showed >90% viability of the HeLa cell line screened.
With an intention of identifying chalcone derivatives exhibiting anti-protozoal activity, a cohort of relatively unexplored arylpyrrole-based chalcone derivatives were synthesized in moderate to good yields. The resultant compounds were evaluated in vitro for their potential activity against a cultured Trypanosoma brucei brucei 427 strain. Several compounds displayed mostly modest in vitro anti-trypanosomal activity with compounds 10e and 10h emerging as active candidates with IC50 values of 4.09 and 5.11 µM, respectively. More importantly, a concomitant assessment of their activity against a human cervix adenocarcinoma (HeLa) cell line revealed that these compounds are non-toxic.
Objective: Persea americana is a popular plant that is well known for its fruit, which is highly consumed due to its nutritional and medicinal values. The rich secondary metabolites content of P. americana creates an opportunity to utilize it as a functional food or standardized herbal preparations. The quality of a medicinal plant is determined by the active substances produced by the plant. Therefore, the purpose of the present study is to determine the secondary metabolites present in P. americana grown in uncultivated farmland in Ogbomoso, Oyo State Nigeria.
Methods: The dried pulvurised leaves of P. americana from uncultivated farmland in Ogbomoso, Oyo State Nigeria were extracted with methanol by the maceration method and partitioned successively with solvents of increasing polarity. The extracts obtained were subjected to phytochemical screening and the total phenolics were determined spectrometrically using the folin–ciocalteu method.
Results: The phytochemical screening showed that P. americana is rich in various secondary metabolites such as flavonoids, saponins, tannins, and alkaloids. The total phenolic content gave 500µg/g gallic acid equivalent. The total flavonoid content obtained was 250µg/g using quercetin as standard. The anti-oxidant assay of the crude extract showed a high activity of 89.05% at a concentration of 0.05g/ml.
Conclusion: Total phenolic content of the plant is likely to be a key for determining the free radical scavenging and ROS reducing ability of the plant.
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