Journal of Experimental Pharmacology最新文献

Background: A major cumbersome factor in malaria control measure is the new coming antimalarial drug resistance strains. The increase of resistance to the available marketed antimalarial agents dictates the scientific community to search new alternative antimalarial agent from traditional plants. Therefore, our study assesses the antimalarial activity of the crude root extract and solvent fraction of Sesamum indicum in mice.

Methods: The roots of Sesamum indicum were extracted by 80% methanol and fractionated using three solvents with different polarities. The in vivo antimalarial activity was assessed at 200 mg/kg, 400 mg/kg, and 600 mg/kg of the root crude extract and solvent fraction using the 4-day suppressive test. Similarly, the n- butanol fraction extract, which showed better suppression potential in 4-day suppressive test from other fractions was also evaluated in the curative model to assess its curative potential. The % parasitemia suppression, mean survival time, body weight change, rectal temperature change, and packed cell volume change were also evaluated in both models.

Results: Our finding revealed that the crude extract and solvent fraction treated groups had a statistical significant parasitemia suppression and mean survival time improvement as compared to the negative control (p<0.001) in both models in a dose-dependent fashion. The higher dose n-butanol fraction treated group (600mg/kg) showed the highest suppression effect and mean survival time prolongation in both tests from the other two fractions. However, the lowest suppressive effect was observed in 200 mg/kg aqueous fraction extract-treated groups in the 4-day suppressive test.

Conclusion: The crude root extract and solvent fractions of Sesamum indicum possessed a dose dependent antimalarial activity and a significant change in other parameters in both models that strengthen the traditional claim.

Background: Regardless of the availability of drugs many people still experienced pain and inflammation because current medications often trigger potentially serious adverse effects. A range of medicinal plants with analgesic and anti-inflammatory properties have been widely used by traditional healers. Among them, Gomphocarpus purpurascens is one however there are no experimental studies that support this traditional use.

Objective: This study aimed to evaluate the analgesic and anti-inflammatory activities of 80% methanolic leaf and root extracts of G. purpurascens.

Methods: Air-dried leaves and roots of G. purpurascens were extracted with 80% methanol and an acute oral toxicity study was conducted for the 80% methanolic extract of G. purpurascens according to OECD guideline version eighteen. Preliminary phytochemical screening for the presence of different constituents was carried out. The hot plate method was used to evaluate centrally mediated analgesic activity while peripheral analgesic activity was tested by an acetic acid-induced writhing test. Carrageenan-induced paw edema test and formalin-induced pedal edema test were used to evaluate anti-inflammatory activity.

Results: Dose-dependent inhibition of acetic acid-induced writhing test was observed in mice by 100 mg/kg, 200 mg/kg, and 400 mg/kg of root extract with respective values of 16.6%, 68.9%, and 83%. In the hot plate method, the root extract at doses of 200mg/kg and 400 mg/kg showed a significant (p < 0.05) analgesic effect. Maximum anti-inflammatory effects by all doses of leaf extracts were observed from 2-4hr post-induction in carrageenan-induced paw edema; and all tested doses of the extract inhibited the formalin-induced inflammation significantly (p < 0.001, p < 0.01). The presence of saponins, alkaloids, flavonoids, tannins, terpenoids, anthraquinone, steroids, and phenols might be responsible for these activities.

Conclusion: This study shows that the extract had potential analgesic and anti-inflammatory activity which supports the traditional claim.

Background: Heteromorpha arborescens has been used to treat diabetes traditionally. There was no in vivo study to support the claim. This study aimed to confirm anti-diabetic activity of 80% methanol in water extract and solvent fractions of H. arborescens leaves in mice.

Methods: H. arborescens leaves were macerated and extracted in 80% methanol in water. Hydro-methanol extract of H. arborescens leaves were tested in mice models. Overnight fasted mice were randomly divided into five groups for normoglycemic and glucose-loaded models as a negative control, positive control, and three tested groups, whereas, in streptozotocin-induced diabetic models, the mice were grouped into six groups each comprised six mice: diabetic negative control and normal negative control groups treated with 10 mL/kg distilled water, diabetic positive control group treated with Glibenclamide 5 mg/kg and three diabetic tested groups treated with extract at 100, 200, and 400 mg/kg doses. A one-way ANOVA was performed to analyze the data, and the post hoc Tukey's test was utilized for multiple comparisons. The P-value <0.05 was considered statistically significant.

Results: Hydro-methanol extract of H. arborescens leaves at 400 mg/kg in normoglycemic mice significantly lowered blood glucose levels (BGLs) (P< 0.01). Mice with oral glucose-loaded test lowered BGLs at dosages of 200 mg/kg (P < 0.05) and 400 mg/kg (P < 0.01) respectively. Single-dose of ethyl acetate, n-hexane fractions and hydro-methanol extract at 100 mg/kg, 400 mg/kg and 200 mg/kg reduced BGLs (P < 0.05, P < 0.001, and P < 0.01) respectively. BGL drops in diabetic mice given daily repeated doses of 200 mg/kg of hydro-methanol extract and 400 mg/kg of ethyl acetate fraction (P < 0.001). Diabetic mice gained weight at a 400 mg/kg hydro-methanol extract and ethyl acetate fraction (P < 0.05 and P < 0.01) respectively. Hydro-methanol extract and ethyl acetate fraction and at 200 mg/kg decreased total cholesterol, triglycerides, and low-density lipoprotein and increased high-density lipoprotein (P < 0.001).

Conclusion: 80% methanol in water extract and solvent fractions of H. arborescens leaves showed anti-diabetic effects and significantly reduced hyperlipidemia in diabetics, this study supported the traditional usage of H. arborescens for treating diabetes; however, species variation could also limit such a straightforward extrapolation of the findings of this study in humans.

Introduction: There are genuine concerns that long-term use of anti-retroviral drugs may be associated with reproductive complications in females. This study aimed to ascertain the effect of highly active anti-retroviral drugs on the ovarian reserve and reproductive potential of female Wistar rats and by extension to HIV-positive human females.

Methods: A total of 25 female Wistar rats, weighing between 140g and 162g, were randomly allotted into non-intervention and intervention groups, receiving the anti-retroviral drugs, Efavirenz (EFV), Tenofovir Disoproxil Fumarate (TDF), Lamivudine (3TC), and a fixed-dose combination (FDC). The dosage was administered orally at 8 am daily for 4 weeks. Serum concentrations of anti-Mullerian hormone (AMH), follicle-stimulating hormone (FSH), luteinising hormone (LH), and estradiol were measured using standard biochemical techniques (ELISA). Follicular counts were made on fixed ovarian tissue from the sacrificed rats.

Results: The mean AMH level for the control group and the EFV, TDF, 3TC, and FDC groups were 11.20, 6.75, 7.30, 8.27, and 6.60 pmol/L, respectively. The EFV and FDC groups had the lowest AMH, compared to the other groups, but there was no statistically significant difference in AMH across the groups. The mean count of antral follicles was significantly lower in the group that received EFV when compared to the other groups. The corpus luteal count was significantly higher in the control group than in the intervention groups.

Conclusion: The study demonstrated a disruption in the reproductive hormones of female Wistar rats receiving anti-retroviral regimens containing EFV. Clinical studies are required to determine if these changes are seen in women receiving EFV-based treatment, as this may compromise reproductive function and predispose them to early menopause.

Background: The outbreak of COVID-19 has led to the suffering of people around the world, with an inaccessibility of specific and effective medication. Fingerroot extract, which showed in vitro anti-SARS-CoV-2 activity, could alleviate the deficiency of antivirals and reduce the burden of health systems.

Aim of study: In this study, we conducted an experiment in SARS-CoV-2-infected hamsters to determine the efficacy of fingerroot extract in vivo.

Materials and methods: The infected hamsters were orally administered with vehicle control, fingerroot extract 300 or 1000 mg/kg, or favipiravir 1000 mg/kg at 48 h post-infection for 7 consecutive days. The hamsters (n = 12 each group) were sacrificed at day 2, 4 and 8 post-infection to collect the plasma and lung tissues for analyses of viral output, lung histology and lung concentration of panduratin A.

Results: All animals in treatment groups reported no death, while one hamster in the control group died on day 3 post-infection. All treatments significantly reduced lung pathophysiology and inflammatory mediators, PGE₂ and IL-6, compared to the control group. High levels of panduratin A were found in both the plasma and lung of infected animals.

Conclusion: Fingerroot extract was shown to be a potential of reducing lung inflammation and cytokines in hamsters. Further studies of the full pharmacokinetics and toxicity are required before entering into clinical development.

Background: The use of phytotherapics is very frequent in men with prostatic diseases, sexual disorders and infertility, and many associations are commercially available. Various vegetable products used as drugs or nutraceuticals are attributed to possess the capacity to exert benefic effects on the reproductive system, and most of these drugs have a rich and varied lipidosterolic fraction, primarily responsible for the effects related to the male genital sphere. Kigelia africana (Lam.) Benth. (Bignoniaceae) is a plant used in African folk medicine as a vegetal remedy for various diseases, including some disorders of the male reproductive system; however, its potential activities have not yet been fully explored. The aim of the present study was to investigate whether the lipidosterolic hexane extract (LHE) from K. africana fruits, analyzed by comprehensive two-dimensional gas chromatography-mass spectrometry/flame ionization detection (GC×GC-MS/FID), can prevent or reverse benign prostatic hyperplasia (BPH) in rats.

Methods: BPH was induced in experimental groups by daily subcutaneous injections of testosterone propionate (TP) for four weeks. β-sitosterol (β-s) was used as positive control. On day 28, the animals were sacrificed by cervical dislocation after anesthesia. Prostates were excised, weighed, and used for macroscopic and histological studies. Testosterone and dihydrotestosterone (DHT) levels in prostate were measured.

Results: The results showed that LHE significantly reduced the prostatic weight, prostatic index, prostatic levels of testosterone and DHT, and the histopathological alterations (including the epithelial thickness, stromal proliferation, and lumen area) induced by testosterone. These effects were superior to those demonstrated by β-s and appear to be due to a partial antiandrogenic activity of LHE.

Conclusion: The results obtained showed that the LHE can prevent, and reverse testosterone induced prostatic hyperplasia, and support the traditional use of Kigelia africana in some disorders of the reproductive system.

Background: Aloe species are among the most significant plants with several applications. Many of the species, however, are underexplored, owing to their scarcity and limited geographical distribution. A. adigratana Reynolds, which is common in Ethiopia, is one of the little-studied and endangered Aloe species.

Objective: This preliminary study focuses on the phytochemical screening, proximate analysis, essential oil content, and antifungal activities of A. adigratana leaf peels. Antifungal activities were also tested on the gels of the plant for comparison.

Methods: Standard procedures were used for phytochemical and proximate composition studies. Essential oil analysis was performed using a gas chromatography-mass spectrometry instrument. Using the well-diffusion method, investigations on antifungal activity were performed on three clinically isolated specimens of dandruff-causing fungus; namely, Malassezia furfur, Malassezia restricta, and Malassezia globosa.

Results: The leaf peels of A. adigratana contained alkaloids, flavonoids, tannins, and terpenes. The mean moisture, ash, and crude fat levels were 85.69, 92.20, and 8.00%, respectively, whereas the mean total protein and mean total carbohydrate values were 2.59 and 3.04%. Gas chromatography-mass spectrometry investigation confirmed the presence of fifteen essential oils. The most prevalent essential oil component was discovered to be phytol (33.78%), followed by decane (11.29%). In a dose-dependent way, the leaf latex and gel extracts prevented the growth of three dandruff-causing Malassezia fungal species (M. furfur, M. restricta, and M. globosa). Both the latex and gel demonstrated the maximum activity on M. globosa, the most prevalent fungus in the research area, with minimum inhibitory concentrations of 0.24 and 0.48 mg/mL and minimum fungicidal concentrations of 0.48 and 0.97 mg/mL, respectively.

Conclusion: In general, the proximate and essential oil compositions of A. adigratana leaves were comparable to those of other Aloe species widely used in the food, cosmetic, and pharmaceutical industries, implying that A. adigratana could be a potential future plant for such industries.