Bioassay-Guided Isolation and Structure Elucidation of Cytotoxic Stilbenes and Flavonols from the Leaves of Macaranga barteri

Bioassay-guided fractionation of the leaves of Macaranga barteri collected from Nigeria led to the isolation of three previously undescribed cytotoxic stilbenes, macabartebenes A-C (1-3), together with six known compounds including prenylated stilbenes: vedelianin (4), schweinfurthin G (5), and mappain (7), prenylated flavonols: 8-prenylkaempferol (6), and broussoflavonol F (8), and the geranylated flavonol, isomacarangin (9). The cytotoxicity of the compounds was evaluated against four human cancer cell lines, with vinblastine as the positive control and DMSO vehicle as the negative control. Vedelianin (IC50 = 0.32 – 0.54 μM) displayed the greatest antiproliferative activity across the panel of cancer cell lines amongst the compounds, while macabartebene A (IC50 = 0.60 – 0.79 μM) was the most potent of the previously unreported compounds. The compounds displayed varying selectivity towards the cancer cell lines compared to the normal human prostate cell line. The findings of this study revealed that M. barteri leaves contain several cytotoxic compounds

Phytochemical Analysis, Antioxidant and Antimicrobial Properties of Hexane, Ethyl acetate, and Methanol Leaf Extracts of Ipomoea hildebrandtii Vatke Shrub Plant

Ipomoea hildebrandtii Vatke have been effectively used to relieve general body pains, treat wounds and cuts in the semi-arid region of Kenya. Hence the objective of this paper was to evaluate the phytochemical analysis, antioxidant and antimicrobial properties of hexane, ethyl acetate and methanol leaf extracts of Ipomoea hildebrandtii Vatke shrub plant. The profiling of the phytochemicals was carried out using the Fourier-transform infrared (FTIR) and Gas Chromatography-Mass spectroscopy (GC-MS) analyses. Antimicrobial and antioxidant activities of the methanol, hexane and ethyl acetate extracts of I. hildebrandtii were determined using disk diffusion and 2,2-diphenyl-l-picrylhydrazyl (DPPH) radical scavenging assays respectively. Preliminary phytochemical screening revealed that the leaf extracts are enriched with alkaloids, tannins, terpenoids, steroids, glycosides, flavonoids, phenols, quinones, and saponins. With GC-MS, the major compound tetratetracontane (73.14%) was identified in hexane and 9-octadecanamide, (Z)- in ethyl acetate and methanol extracts (30.99%) and (43.09%) respectively. The IR spectroscopy revealed various functional groups such as C=O, C=C, –OH and –NH. The methanol extract showed good antimicrobial activity at 1000 mg/mL against all the microorganisms tested except Escherichia coli while the hexane extract was the best antimicrobial activity against E. coli at 1000 mg/mL. The ethyl acetate extract showed the best antioxidant activity against DPPH (IC50 = 48.70 ± 1.54 µg/mL) compared to the standard ascorbic acid (IC50 = 21.24 ± 0.12 µg/mL). The experimental findings showed that all extracts from I. hildebrandtii leaves possess significant antimicrobial and antioxidant activities justifying its use in traditional medicine. These biological activities might be due to the presence of the presence of the identified phytochemicals in them

International Consensus Statement on Rhinology and Allergy: Rhinosinusitis

Background: The 5 years since the publication of the first International Consensus Statement on Allergy and Rhinology: Rhinosinusitis (ICAR‐RS) has witnessed foundational progress in our understanding and treatment of rhinologic disease. These advances are reflected within the more than 40 new topics covered within the ICAR‐RS‐2021 as well as updates to the original 140 topics. This executive summary consolidates the evidence‐based findings of the document. Methods: ICAR‐RS presents over 180 topics in the forms of evidence‐based reviews with recommendations (EBRRs), evidence‐based reviews, and literature reviews. The highest grade structured recommendations of the EBRR sections are summarized in this executive summary. Results: ICAR‐RS‐2021 covers 22 topics regarding the medical management of RS, which are grade A/B and are presented in the executive summary. Additionally, 4 topics regarding the surgical management of RS are grade A/B and are presented in the executive summary. Finally, a comprehensive evidence‐based management algorithm is provided. Conclusion: This ICAR‐RS‐2021 executive summary provides a compilation of the evidence‐based recommendations for medical and surgical treatment of the most common forms of RS

Antitrypanosomal activity of some medicinal plants from Nigerian ethnomedicine

Human African trypanosomiasis is a neglected tropical disease with complex clinical presentation, diagnosis, and difficult treatment. The available drugs for the treatment of trypanosomiasis are old, expensive, and less effective, associated with severe adverse reactions and face the problem of drug resistance. This situation underlines the urgent need for the development of new, effective, cheap, and safe drugs for the treatment of trypanosomiasis. The search for new antitrypanosomal agents in this study is based on ethnomedicine. In vitro antitrypanosomal activity of 36 plant extracts from 10 plant species from Nigerian ethnomedicine was evaluated against bloodstream forms of Trypanosoma brucei rhodesiense STIB 900. Cytotoxic activity was determined against mammalian L6 cells. Alamar blue assay was used to measure the endpoint of both antitrypanosomal and toxicity assays. The ethyl acetate extract of leaves of Ocimum gratissimum Linn. (Labiatae) showed the highest antitrypanosomal activity (IC(50) of 2.08 +/- 0.01 mug/ml) and a high selective index of 29. Furthermore, the hexane, ethyl acetate, or methanol extracts of Trema orientalis (L.) Blume (Ulmaceae), Pericopsis laxiflora (Benth. ex Baker) Meeuwen, Jatropha curcas Linn. (Euphorbiaceae), Terminalia catappa Linn. (Combretaceae), and Vitex doniana Sweet (Verbenaceae) displayed remarkable antitrypanosomal activity (IC(50) 2.1-17.2 mug/ml) with high selectivity indices (20-80) for trypanosomes. The antitrypanosomal activity of T. catappa and T. orientalis against T. brucei rhodesiense (STIB 900) is being reported for the first time in Nigerian ethnomedicine, and these plants could be a potential source of antitrypanosomal agent

In Vitro and In Vivo Antimalarial Activity of Ficus thonningii Blume (Moraceae) and Lophira alata Banks (Ochnaceae), Identified from the Ethnomedicine of the Nigerian Middle Belt

Drug resistance in Plasmodium falciparum requires that new drugs must be developed. Plants are a potential source for drug discovery and development. Two plants that used to treat febrile illnesses in Nigeria were tested for in vitro and in vivo antimalarial activity and cytotoxicity in cancer cell lines. Methanol, hexane, and ethyl acetate leaf extracts of Ficus thonningii and Lophira alata were active in in vitro assays against P. falciparum NF54 (sensitive) and K1 (multiresistant) strains. Hexane extracts of F. thonningii and L. alata were the most effective extracts in in vitro assays with IC50 of 2.7±1.6 μg/mL and 2.5±0.3 μg/mL for NF54 and 10.4±1.6 μg/mL and 2.5±2.1 μg/mL for K1 strain. All extracts were nontoxic in cytotoxicity assays against KB human cell line with IC50 of over 20 μg/mL, demonstrating selectivity against P. falciparum. In vivo analysis shows that hexane extracts of both plants reduced parasitaemia. At the maximum dose tested, L. alata had a 74.4% reduction of parasitaemia while F. thonningii had a reduction of 84.5%, both extracts prolonged animal survival in mice infected with P. berghei NK65 when compared with vehicle treated controls. The antiplasmodial activity observed justifies the use of both plants in treating febrile conditions

Comparison of SYBR Green I-, PicoGreen-, and [H-3]-hypoxanthine-based assays for in vitro antimalarial screening of plants from Nigerian ethnomedicine

The standard method for in vitro antimalarial drug screening is based on the isotopic assay which is expensive and utilizes radioactive materials with limited availability, safety, and disposal problems in developing countries. The use of non-radioactive DNA stains SYBR Green I (SG) and PICO greenA (R) (PG) for antimalarial screening had been reported. However, the use of the two DNA stains for antimalarial screening of medicinal plants has not been compared. Thus, this study compared SG, PG with the [H-3]-hypoxanthine (HP) incorporation assays for in vitro antimalarial screening of medicinal plants. The 50% inhibitory concentration (IC50) values obtained using the three methods for antimalarial activity of medicinal plants and standard antimalarial drugs were similar. Data generated from this study suggests that the non-radioactive microflourimetric assay is sufficiently sensitive to reproducibly identify plant extracts with antimalarial activity from those lacking activity. The HP-based assay exhibited the most robust signal-to-noise ratio of 100, compared with signal-to-noise ratios of 7 for SG and 8 for PG. The SG-based assay is less expensive than the PG- and HP-based assays. SG appears to be a cost-effective alternative for antimalarial drug screening and a viable technique that may facilitate antimalarial drug discovery process especially in developing countrie

Anti-Inflammatory and Antimicrobial Activities of Hippocratea Indica Root Bark and Poga Oleosa Fruits

The methanolic extracts of Hippocratea indica root bark and Poga oleosa fruits were investigated for anti-inflammatory and antimicrobial activities. Both extracts inhibited carrageenan-induced paw oedema significantly in rats in a dose-dependent manner in 4 h. H. indica inhibited oedema significantly at the minimal dose (125 mg/ml, p< 0.05) from 2 h onward, and gave 100% inhibition in 4 h. at 250 mg/kg. It was shown to be a more potent anti-inflammatory agent than P. oleosa. Also, H. indica extract exhibited greater antimicrobial activity against tested bacteria, with Staphylococcus aureus being the most susceptible bacterium (MIC, 16 mg/ml). Both plants were inactive against Candida albicans. These results confirm the anti-inflammatory and antibacterial activities of the two plants