Two flavonol glycosides; U1: naringenin-7-O-glucoside and U2: kaempferol-3-O-glucoside were isolated for the first time, from ethyl acetate fraction of the stem bark of a traditional medicinal plant called Uapaca heudelotti. IR and NMR spectroscopy were used to elucidate the structures of the isolated compound. The two compounds were active against the 7 tested microorganisms; Escherichia coli, Bacillus subtilis, Salmonella typhi, Streptococcus pyogenes, Klebsiella pneumoniae, Staphylococcus aureus and Proteus mirabilis. The zones of inhibition of the compounds ranged from 16 to 23 mm.The MIC value was as low as 6.25 μg/mL against Salmonella typhi, Streptococcus pyogenes, and Bacillus subtilis. The radical scavenging activity of compound U1 and U2 was 80 and 85 % at 240 μg/mL, while that of the standard drug was 98% at 240 μg/mL. The results show an existent possibility of using the plant for the treatment of microbial diseases.

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Phaeophytin a, α-amyrin and lupeol isolated from Brachystelma togoense were screened against S. aureus, E. coli, S. pneumoniae, S. typhi, and C. albicans using Ciprofloxacin and Terbinafine as standards. The results showed that these phytochemicals displayed antimicrobial activity against the tested organisms with the zone of inhibition from 12 -27 mm. The result of minimum inhibitory concentration (MIC) showed that phaeophytin a was most active against C. albicans (0.09 mg/mL). The minimum bactericidal concentration (MBC) showed that phaeophytin a and lupeol were most active against S. aureus, S. pneumoniae and S. typhi (0.37 mg/mL). The result of minimum fungicidal concentration (MFC) showed that phaeophytin a was most active against C. albicans (0.1875 mg/mL).The activities of these phytoconstituents in B. togoense justified ethnomedicinal uses of the plant to treat various ailments.

The medicinal herb Brachystelma togoense schtlr (Apocynaceae) is used traditionally for treatment of ailments.   The secondary metabolites, phaeophytin a, α-amyrin and lupeol were isolated from the CH2Cl2 and MeOH extracts of Brachystelma togoense.  The structures were elucidated using 1H, 13C and 2D NMR. These phytochemicals have previously being reported to have various biological activities such as anti-inflammatory, anti-fungal and anti-cancer. The presence of phaeophytin a, α-amyrin and lupeol in Brachystelma togoense justified the use of the plant for medicinal purpose in Nigeria.

Background Antibiotic resistance has risen as a result of a variety of conditions, prompting researchers to look for new compounds that can combat multidrug-resistant organisms. Over the last two decades, chalcones have been proved to be attractive moieties in drug discovery. Various substituted acetophenones, propiophenones and 4-(Diphenylamino) benzaldehyde were combined, using the Aldol condensation reaction to obtain eight novel triphenylamine chalcones. The compound’s antimicrobial properties were investigated (in vitro). With the non-mutant X-ray Human cytochrome P450 21A2 Hydroxyprogesterone retrieved from Protein Data Bank (PDB: 5VBU), molecular docking experiments were also carried out to analyse the most favourable conformation and find the orientation that maximizes interaction and minimize energy. Results Eight novel triphenylamine chalcones were successfully synthesized and recrystallized using ethanol, the percentage yield of the compounds were between 30 and 92%. The activity against different pathogens revealed that, all synthesized compounds showed marked antimicrobial activity against the tested microorganisms. (E)-3-(4-(diphenylamino)phenyl)-1-(3′-nitrophenyl)prop-2-en-1-one (1b) showed the highest zone of inhibition against Aspergillus niger, measuring 30 mm. The minimum inhibitory concentration (MIC) results revealed that (E)-1-(4′-bromophenyl)-3-(4-(diphenylamino)phenyl)prop-2-en-1-one (1a), (E)-3-(4-(diphenylamino)phenyl)-1-(3′-nitrophenyl)prop-2-en-1-one (1b), (E)-1-(4′-chlorophenyl)-3-(4-diphenylamino)phenyl)prop-2-en-1-one (1c), (E)-3-(4-diphenylamino)phenyl)-1-(4′-fluorophenyl)prop-2-en-1-one (1d) and (E)-4-(3-(diphenylamino)phenyl)-1-(4-fluorophenyl)-2-methylbut-3-en-1-one (2d) had the lowest MIC and inhibit Aspergillus niger growth at 12.5 µg/ml. All the synthesized compounds showed minimum bactericidal concentration and minimum fungicidal concentration (MBC/MFC) effect against Escherichia coli, Pseudomonas aeruginosa, Bacillus subtilis, Candida albicans and Aspergillus niger at 50 µg/ml. The docking studies of the synthesized chalcones with the binding site of the Human cytochrome P450 21A2 Hydroxyprogesterone (PDB: 5VBU) reveal that the binding affinity of the synthesized chalcones was in the range of − 11.2 to − 9.4 kcal/mol and showed highest binding score compared to that of the standard drugs (Fluconazole and Ciproflaxacin), with docking scores of − 7.9 and − 7.3 kcal/mol, respectively. Conclusions The investigation reveals that compound 1b showed the highest ZOI of 30 mm, least MIC and MBC/MFC of 12.5 and 50 µg/ml against Aspergillus niger, respectively. Therefore, displayed better antifungal potential as compared to the rest of the compounds. The outcome of the docking analysis revealed that (E)-4-(3-(diphenylamino)phenyl)-1-(4′-hydroxyphenyl)-2-methylbut-3-en-1-one (2a) showed a better binding affinity of -11.2 kcal/mol, which is higher than the remaining compounds and the control drugs (fluconazole and ciproflaxacin).

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