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In Vitro Mechanism of Action of Acanthospermum hispidum in Trypanosoma brucei
African trypanosomiasis is a major neglected tropical disease with significant health and economic concerns in sub-Saharan Africa. In the absence of vaccines for African trypanosomiasis, there is a consideration for alternative sources of chemotherapy. Acanthospermum hispidum DC (A. hispidum) is a herbal species of the Asteraceae family that is endowed with rich phytochemicals with unknown mechanisms of antitrypanosomal effects. This study aimed to investigate the cellular mechanisms of antitrypanosomal and antioxidant activities of A. hispidum against Trypanosoma brucei (T. brucei), a causative protozoan species of African trypanosomiasis. Fractions were prepared from the whole plant of A. hispidum through solvent partitioning by employing solvents of varying polarities (hexane, HEX; dichloromethane, DCM; ethyl acetate, EA; aqueous, AQ). The in vitro efficacies and mechanisms of antitrypanosomal activities of A. hispidum were investigated using a panel of cell biological approaches. GC-MS analysis was used to identify the major compounds with a possible contribution to the trypanocidal effects of A. hispidum. A. hispidum fractions displayed significant antitrypanosomal activities in terms of half-maximal effective concentrations (EC50) and selectivity indices (SI) (AH-HEX, EC50 = 2.4 μg/mL, SI = 35.1; AH-DCM, EC50 = 2.2 μg/mL, SI = 38.3; AH-EA, EC50 = 1.0 μg/mL, SI = 92.8; AH-AQ, EC50 = 2.0 μg/mL, SI = 43.8). Fluorescence microscopic analysis showed that at their EC50 values, the fractions of A. hispidum altered the cell morphology as well as the organization of the mitochondria, nucleus, and kinetoplast in T. brucei. At their maximum tested concentrations, the prepared fractions exhibited antioxidant absorbance intensities comparable to the reference antioxidant, Trolox, in contrast to the oxidant intensity of an animal antitrypanosomal drug, diminazene (Trolox, 0.11 A; diminazene, 0.65 A; AH-HEX, 0.20 A, AH-DCM, 0.20 A, AH-EA, 0.13 A, AH-AQ, 0.22 A). GC-MS analysis of the various fractions identified major compounds assignable to the group of alkaloids and esters or amides of aliphatic acids. The results provide useful pharmacological insights into the chemotherapeutic potential of A. hispidum toward drug discovery for African trypanosomiasis.
Phytochemical Screening, Antioxidant, and Antimicrobial Activities of Seven Underinvestigated Medicinal Plants against Microbial Pathogens
Background. Plants are a rich source of therapeutic compounds that have tremendous applications in the pharmaceutical industry. This study aimed to identify the phytochemicals present in the seven selected medicinal plants as well as their antioxidant and antimicrobial activities. Methods. Phytochemical screening, total phenolic, and flavonoid contents were determined using standard methods. The antioxidant activity of plant extracts was determined using 2, 2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl (OH), and nitric oxide (NO) radical scavenging assays. The antimicrobial activity of the plant extracts was determined by the broth microdilution method. Results. The results of phytochemical analysis showed the presence of phenols, flavonoids, and steroids in all plant extracts. The extract of Psychotria peduncularis showed the highest total phenolic and flavonoid contents (5.57 ± 0.22 mg GAE/g and 1.38 ± 0.06 mg QE/g, respectively). All plant extracts showed very strong antioxidant activity against DPPH and NO radical scavenging with IC50 values ranging from 0.55 to 49.43 µg/mL and 0.65 to 13.7 µg/mL, respectively. The extracts of Tristemma mauritianum and P. peduncularis displayed significant antibacterial activity with MIC values ranging from 16 to 1024 µg/mL. T. mauritianum extract showed bactericidal activity against all tested species. The extracts of Alsophila manianna and P. peduncularis showed significant antifungal activity (MIC = 64 µg/mL) against Candida albicans strain. Conclusion. The screened extracts of medicinal plants used in our study can be used as potential antioxidant and antimicrobial agents, and resources for the development of new drugs.
Biological Activity and Chemical Composition of Detarium microcarpum Guill. and Perr—A Systematic Review
Historically, natural products have been the principal source of medications for the treatment of human diseases. Traditional medical practitioners employ Detarium microcarpum as a treatment for diabetes, malaria, wounds, inflammation, and even cancer. This study emphasizes the importance of harmonizing D. microcarpum research so that results from various sources may be directly compared to reach a scientific conclusion. We searched Google Scholar, Science Direct, Google.com, Wiley, PubMed, Hindawi, and Springer for research papers on Detarium microcarpum. This analysis excludes untrustworthy online data, thesis papers, and review publications on D. microcarpum. The leaves and stem bark were shown to have high antioxidant, anti-inflammatory, antibacterial, antidiabetic, and anticancer properties. The study also discovered that too much consumption is harmful. Polyphenols and flavonoids were the most commonly reported compounds. However, human safety and efficacy are yet to be fully evaluated, and further well-designed clinical trials are needed to confirm preclinical findings. The leaves and stem bark extracts and isolated compound mechanism of action should be investigated. It is necessary to set a standard dose and ensure its safety.
In Silico, In Vitro, and In Vivo Wound Healing Activity of Astragalus microcephalus Willd.
Background and Objectives. A wound is one of the high-prevalence disorders that affect people’s lives physically, mentally, and financially. This study examined the Astragalus microcephalus Willd. wound healing process in in vivo and in vitro conditions by focusing on the phytoestrogen activity of this extract. Methods. The methanolic root extract was prepared by maceration, and flavonoids were evaluated by LC/MS. In silico examination was performed based on the LC/MS results, and the binding affinity of these compounds to estrogen receptors (ERs) α and β was evaluated. Wound healing evaluation in both in vitro (NHDF cell line, by 500 μg/ml concentration of the extract, 24 h) and in vivo (Wistar rat, topical daily treated with 1.5% of the extract ointment, 21 days) conditions in comparison to control groups was conducted. Rats’ control groups included silver sulfadiazine, Vaseline, and the nontreated groups. Results. Eleven flavonoids were detected using LC/MS. The in silico study showed that formononetin, kaempferol-based structures, quercetin-3-O-neohesperidoside, and calycosin-7-O-beta-D-glucoside had a high affinity (<−6.3) to ERs α and β. Wound closing measurement showed significant improvement in the group treated with the extract in both in vitro and in vivo assays compared to the control groups. Histopathological results confirmed these findings; inflammation factors decreased, and fibroblast proliferation, fibrosis, and epithelization increased, especially in the extract group. Conclusion. This study shows that Astragalus microcephalus has wound healing activity in vitro and in vivo with low toxicity due to the presence of flavonoids, especially isoflavonoids, which show a high affinity to bind to ERs α and β in the skin tissue.
Neuroprotective Effects of the Ethanolic Leaf Extract of Crassocephalum crepidioides (Asteracaeae) on Diazepam-Induced Amnesia in Mice
This study aimed to evaluate the neuroprotective effects of the ethanolic leaf extract of Crassocephalum crepidioides (Cc) on diazepam-induced amnesia in mice. Thirty mice distributed into six groups of five mice each were used. The normal control and negative control groups received 2% ethanol per os, the positive control group received piracetam (150 mg/kg, p.o), and three experimental groups were treated with three doses of ethanolic leaf extract of Cc (100, 200, and 400 mg/kg, p.o). All groups except the normal control group were co-treated with diazepam (3 mg/kg, i.p) daily for 14 days. The memory effects were evaluated using the Radial Arm Maze (RAM) and the Novel Object Recognition (NOR) tests, while the anti-depressive effects were evaluated using the tail suspension test. All animals were sacrificed at the end of the study. Hippocampi, isolated from the right hemisphere, were used to prepare a homogenate for the determination of oxidative stress biomarkers. The ethanolic leaf extract of cc significantly () decreased the number of working and reference memory errors in the RAM test and induced a significant () increase in the time spent exploring the novel object in the NOR test. The extract also induced a significant () increase in the mobility time in tail suspension. Moreover, compared to the negative control group, the extract significantly () increased superoxide dismutase activity and significantly () decreased malondialdehyde levels. The histopathological analysis of hippocampi showed that the cc extract increased cell density when compared with the negative control. These results suggest that the ethanolic left extract of cc could have neuroprotective properties, which could be attributed to its antioxidant properties.
In Vitro and In Vivo Antiproliferative Actions of Solanum gilo Raddi (Solanaceae) Fruit Extract on Breast Tissues
Background. Menopause is a normal event characterized by a drop in estrogen’s production, leading to numerous symptoms. To face these later, women rely on hormone replacement therapy (HRT), which alleviates numerous menopausal symptoms. Unfortunately, long-term exposure to estrogens is associated with an increase in endometrial and breast cancers. This study dealt with the evaluation of in vitro and in vivo antiproliferative effects of Solanum gilo Raddi, a plant used in folk medicine to treat tumors in Cameroon. Materials and Methods. The in vitro antiproliferative effect of S. gilo fruit extract was investigated through the well-characterized MTT assay in one normal and three cancerous breast cells. For the in vivo study, one normal group (NOR) of rats received distilled water (vehicle), and five other groups (n = 6) were treated either with tamoxifen (3.3 mg/kg BW) as standard or with the vehicle (negative control) or S. gilo fruit hydroethanolic extract (125, 250, and 500 mg/kg BW). The treatments were administered concomitantly with the E2V to induce breast hyperplasia for 16 weeks, and the endpoints were the histopathology of the mammary glands and some biochemical parameters. Results. The S. gilo extract significantly inhibited human (MCF-7 and MDA-MB-231) and rodent (4T1) breast carcinoma cell growth. Rats exposed only to E2V presented atypical mammary hyperplasia compared to the normal parenchyma observed in normal rats. While rats treated with S. gilo extract at the dose of 125 mg/kg BW showed a microarchitecture of mammary glands with moderate hyperplasia, the higher doses (250 and 500 mg/kg) inhibited mammary gland hyperplasia compared to the E2V group. Conclusion. S. gilo fruit extract has antiproliferative constituents that could help to fight against estrogen-dependent breast cancer, thanks to their ability to scavenge free radicals, as exhibited in this study.