Luteolin-Rich Extract of Thespesia garckeana F. Hoffm. (Snot Apple) Contains Potential Drug-Like Candidates and Modulates Glycemic and Oxidoinflammatory Aberrations in Experimental Animals

Abstract

The present study evaluated the polyphenolic contents and hypoglycemic, antioxidant, and anti-inflammatory effects of the diethyl ether fraction of Thespesia garckeana using various in vitro and in vivo models. Total phenol and flavonoid contents of the extract were 613.65 ± 2.38 and 152.83 ± 1.56 mg/100 g dry weight, respectively. The extract exhibited in vitro antioxidant activities against DPPH, FRAP, LPO, and ABTS with respective half-maximal inhibitory concentration (IC50) values of 30.91 ± 0.23 , 16.81 ± 0.51 , 41.29 ± 1.82 , and 42.39 ± 2.24 μg/mL. In vitro anti-inflammatory studies using membrane stabilization, protein denaturation, and proteinase activities revealed the effectiveness of the extract with respective IC50 values of 54.45 ± 2.89 , 93.62 ± 3.04 , and 56.60 ± 2.34 μg/mL, while in vitro hypoglycemic analysis of the extract revealed inhibition of α-amylase (IC50 64.59 ± 3.29 μg/mL) and enhancement of glucose uptake by yeast cells. Interestingly, the extract demonstrated in vivo hypoglycemic and anti-inflammatory effects in streptozotocin- (STZ-) induced diabetic and xylene-induced ear swelling models, respectively. In addition, the extract improved insulin secretion, attenuated pancreatic tissue distortion and oxidative stress, and increased the activities of superoxide dismutase (SOD), catalase, and reduced glutathione (GSH), while reducing the concentration of LPO in the diabetic rats. A high-performance liquid chromatography (HPLC) analysis identified the presence of catechin ( 6.81 e − 1 ppm), rutin ( 8.46 e − 1 ppm), myricetin, apigenin ( 4.019 e − 1 ppm), and luteolin (15.09 ppm) with respective retention times (RTs) of 13.64, 24.269, 27.781, 29.58, and 32.23 min, and these were subjected to a pharmacoinformatics analysis, which revealed their drug-likeness and good pharmacokinetic properties. A docking analysis hinted at the potential of luteolin, the most abundant compound in the extract, for targeting glucose-metabolizing enzymes. Thus, the present study provides preclinical insights into the bioactive constituents of T. garckeana, its antioxidant and anti-inflammatory effects, and its potential for the treatment of diabetes.

SIRT1/P53 in retinal pigment epithelial cells in diabetic retinopathy: a gene co-expression analysis and He-Ying-Qing-Re formula treatment

“…The current data on RBG, IPGTT, and AUC showed that luteolin could generate a slightly hypoglycemic effect on DR mice, with weight loss reversed in STZ-induced diabetic mice in later phases ( Figures 7A–D , p > 0.05 vs. model). The finding was in accordance with relevant research reports ( Alozieuwa et al, 2022 ; Ali et al, 2023 ). Nonetheless, as shown in Figures 7A–D , HF with different concentrations failed to reduce RBG ( p all >0.05 vs. model).…”

Effects of Azanza garckeana Fruit Pulp on Metabolic Syndrome in Wistar Rats Fed on High Fructose Diet

“…However, the stabilizing effect of this supplementation may take more than four (4) weeks before the manifestation of the stabilizing effect can be observed. This work agrees with the works of Alozieuwa et al (2022), whose study shows that the experimental evidence offered substantiates the therapeutic effectiveness of the diethyl-ether fraction derived from Thespesia garckeana for treating diabetes. In addition to augmenting the functions of antioxidant enzymes, the extract also impeded inflammatory reactions, thus showcasing antidiabetic effects in experimental models.…”

Phytochemical Composition and Antioxidant Activity of Edible Wild Fruits from Malawi

“…For example, in a study conducted in Zimbabwe on fruits, the methanolic extract of the Uapaca Kirkiana fruits showed DPPH antioxidant activity in the range of 34:96% ± 0:86 to 36:68 ± 0:46% that was higher than the same species found in Malawi evaluated in this study (15.57%) [38]. Similar findings of antioxidant activity parameters for the studied plants showed similar results for the rest of the plants, namely, Ziziphus mauritiana [39], Parinari curatellifolia [40], Cocos nucifera [41], Thespesia garckeana [42], Vitex doniana [43], Adansonia digitate [44],…”