Aidia genipiflora (DC.) Dandy (Rubiaceae) is used to treat various microbial and inflammatory conditions by traditional healers in West African countries. However, there is no information on anti-inflammatory potential of A. genipiflora. This work therefore provides information on the anti-inflammatory and the antioxidant activities of the stem bark extracts and some bioactive constituents of Aidia genipiflora. The anti-inflammatory activities of the extracts and compounds from A. genipiflora were investigated using the carrageenan-induced footpad oedema assay and the egg albumin denaturation assay. The antioxidant activities of the extract and compounds were investigated using the DPPH radical scavenging assay and the phosphomolybdenum total antioxidant capacity assay. The whole extract of A. genipiflora was also investigated for its acute oral toxicity using the fixed-dose procedure described by the Organization for Economic Cooperation Development guidelines. The whole extract showed no acute toxicity effect and the LD₅₀ was estimated to be greater than 3000 mg/kg body weight. The whole extract, methanol, and ethyl acetate fractions (30, 100, and 300 mg/kg) showed in vivo anti-inflammatory activity with respective percentage inhibition of oedema of 45.11 ± 3.41, 31.12 ± 3.42 and 29.28 ± 3.58 (p < 0.001) at the highest dose of 300 mg/kg. Diclofenac, used as a reference drug, gave a % inhibition of 48.94 ± 3.58. The compounds isolated from A. genipiflora demonstrated in-vitro anti-inflammatory activity at the IC₅₀ range (16–96 μg/mL) compared to diclofenac (IC₅₀ of 74.48 μg/mL). Oleanonic acid (AG1) and D-mannitol (AG4) further demonstrated in vivo anti-inflammatory activity (ED₅₀ = 20.61 ± 1.29; 23.51 ± 1.26 mg/kg respectively) which was less potent compared to diclofenac (ED₅₀ = 12.50 ± 1.41 mg/kg) in the carrageenan-induced oedema assay. The whole extract, pet. ether, ethyl acetate, and methanol fractions of A. genipiflora exhibited DPPH scavenging activities with respective IC₅₀ of 222.2, 169.7, 121.5, and 40.7 μg/mL. The whole extract of A. genipiflora exhibited considerable total antioxidant capacity with respective values of 248.5 mg/g of ascorbic acid equivalent. All the compounds exhibited low DPPH scavenging activity with IC₅₀ (64–86 μg/mL), compared to ascorbic acid (IC₅₀ of 3.13 ± 1.20 μg/mL). These results highlight the anti-inflammatory and antioxidant activities of Aidia genipiflora stem bark extract and its constituents as evidence to support its traditional uses.

Microbial infections remain a public health problem due to the upsurge of bacterial resistance. In this study, the antibacterial, antibiofilm, and efflux pump inhibitory activities of the stem bark of Acacia macrostachya, an indigenous African medicinal plant, were investigated. In traditional medicine, the plant is used in the treatment of microbial infections and inflammatory conditions. A crude methanol extract obtained by Soxhlet extraction was partitioned by column chromatography to obtain the petroleum ether, ethyl acetate, and methanol fractions. Antibacterial, efflux pump inhibition and antibiofilm formation activities were assessed by the high-throughput spot culture growth inhibition (HT-SPOTi), ethidium bromide accumulation, and the crystal violet retention assay, respectively. The minimum inhibitory concentrations (MICs) of the crude extract and major fractions ranged from 250 to 500μg/mL. At a concentration of 3.9250μg/mL, all extracts demonstrated >80 inhibition of biofilm formation in S. aureus. In P. aeruginosa, the EtOAc fraction showed the highest antibiofilm activity (5969) while the pet-ether fraction was most active against E. coli biofilms (4567). Among the test samples, the crude extract, methanol, and ethyl acetate fractions showed remarkable efflux pump inhibition in S. aureus, E. coli, and P. aeruginosa. At ½ MIC, the methanol fraction demonstrated significant accumulation of EtBr in E. coli having superior efflux inhibition over the standard EPIs: chlorpromazine and verapamil. Tannins, flavonoids, triterpenoids, phytosterols, coumarins, and saponins were identified in preliminary phytochemical studies. Stigmasterol was identified in the EtOAc fraction. This study justifies the use of A. macrostachya in the treatment of infections in traditional medicine and highlights its potential as a source of bioactive compounds that could possibly interact with some resistance mechanisms in bacteria to combat antimicrobial resistance.

This study investigated the antibacterial, resistance modulation, biofilm inhibition, and efflux pump inhibition potentials of Loeseneriella africana stem extract and its constituents. The antimicrobial activity was investigated by the high-throughput spot culture growth inhibition (HT-SPOTi) and broth microdilution assays. The resistance modulation activity was investigated using the anti-biofilm formation and efflux pump inhibition assays. Purification of the extract was carried out by chromatographic methods, and the isolated compounds were characterized based on nuclear magnetic resonance, Fourier transform infrared and mass spectrometry spectral data and comparison with published literature. The whole extract, methanol, ethyl acetate, and pet-ether fractions of L. africana all showed antibacterial activity against the test bacteria with MICs ranging from 62.5 to 500.0 µg/mL The whole extract demonstrated resistance modulation effect through strong biofilm inhibition and efflux pump inhibition activities against S. aureus ATCC 25923, E. coli ATCC 25922 and P. aeruginosa ATCC 27853. Chromatographic fractionation of the ethyl acetate fraction resulted in the isolation of a triterpenoid (4S,4αS,6αR,6βS,8αS,12αS,12βR,14αS,14βR)-4,4α,6β,8α,11,11,12β,14α-Octamethyloctadecahydropicene-1,3(2H,4H)-dione) and a phytosterol (β-sitosterol). These compounds showed antibacterial activity against susceptible bacteria at a MIC range of 31–125 µg/mL and potentiated the antibacterial activity of amoxicillin (at ¼ MIC of compounds) against E. coli and P. aeruginosa with modulation factors of 32 and 10, respectively. These compounds also demonstrated good anti-biofilm formation effect at a concentration range of 3–100 µg/mL, and bacterial efflux pump inhibition activity at ½ MIC and ¼ MIC against E. coli and P. aeruginosa. Loeseneriella africana stem bark extracts and constituents elicit considerable antibacterial, resistance modulation, and biofilm and efflux pump inhibition activities. The results justify the indigenous uses of L. africana for managing microbial infections.

Background: Antimicrobial resistance is a global health challenge. The involvement of bacterial biofilms and efflux pumps in the development of multidrug resistance (MDR) is well established. Medicinal plants have been proposed as alternatives for combating MDR focusing on their bioactive constituents with resistance modulatory activities. This study was aimed at investigating the stem bark ofAidia genipiflorafor bioactive constituents with anti-biofilm, efflux pump inhibition and resistance modulatory activities.Method: The crude methanol extract was purified by column chromatography and isolated compounds characterized by mass and nuclear magnetic resonance spectrometry. Antibacterial activity was determined by the High-throughput spot culture growth inhibition and the broth micro-dilution assay. The ethidium bromide accumulation assay was used to determine efflux pump inhibition property. Biofilm inhibition was determined in a microplate crystal violet retention assay.Results: Purification of the ethyl acetate fraction led to the isolation of oleanonic acid (1), 4-hydroxy cinnamic acid docosyl ester (2), β-stigmasterol/β-sitosterol (mixture3a/b) and D-mannitol (4). The minimum inhibitory concentrations (MICs) ranged from 250 to > 500 μg/mL for extracts and fractions and from 15 to 250 μg/mL for compounds. In the presence of sub-inhibitory concentrations of the compounds, the MIC of amoxicillin againstE. coli(20 μg/mL) andP. aeruginosa(320 μg/mL) was reduced by 32 and 10 folds respectively. The whole extract demonstrated anti-biofilm formation and efflux pump inhibition inE. coli,S. aureusandP. aeruginosa. The sterol mixture (3a/b) at concentration of 100 μg/mL caused the highest inhibition (73%) of biofilm formation inS. aureus. Oleanonic acid (1) demonstrated remarkable efflux pump inhibition at MIC of 7.8 μg/mL inE. colibetter than the standard drugs verapamil and chlorpromazine.Conclusion: This study confirms the prospects ofA. genipifloraas a source of new antibacterial agents and adjuvants that could interact with some resistance mechanisms in bacteria to enhance the activity of hitherto ineffective antibiotics. “A small portion of the study has been presented in a conference in the form of poster”.

A number of currently used drugs have been obtained from medicinal plants which are a major source of drugs. These drugs are either used in their pure form or modified to a semisynthetic drug. Drug discovery through natural product research has been fruitful over the years. Traditionally, Calotropis procera is used extensively in the management of epilepsy. This study is conducted to explore the anticonvulsant effect of a hydroethanolic leaf extract of Calotropis procera (CPE) in murine models. This effect was evaluated using picrotoxin-induced convulsions, strychnine-induced convulsions, and isoniazid- and pilocarpine-induced status epilepticus in mice of both sexes. The results showed that CPE (100-300 mg/kg) exhibited an anticonvulsant effect against strychnine-induced clonic seizures by significantly reducing the duration ( ) and frequency ( ) of convulsions. The extract (100-300 mg/kg) caused a profound dose-dependent delay in the onset of clonic convulsions induced by picrotoxin ( ) and tonic convulsions ( ) in mice. The duration of convulsions was reduced significantly also for both clonic and tonic ( ) seizures as well. CPE (100-300 mg/kg), showed a profound anticonvulsant effect and reduced mortality in the pilocarpine-induced convulsions. ED₅₀ (~0.1007) determined demonstrated that the extract was less potent than diazepam in reducing the duration and onset of convulsions but had comparable efficacies. Flumazenil—a GABA_A receptor antagonist—did not reverse the onset or duration of convulsions produced by the extract in the picrotoxin-induced seizure model. In isoniazid-induced seizure, CPE (300 mg kg¹, p.o.) significantly ( ) delayed the onset of seizure in mice and prolonged latency to death in animals. Overall, the hydroethanolic leaf extract of Calotropis procera possesses anticonvulsant properties.