Phytoecdysteroids from Dioscorea dumetorum (Kunth) Pax. and their antioxidant and antidiabetic activities.

Diabetes is a significant global health challenge, affecting circa 540 million adults worldwide. Dioscorea dumetorum, a Nigerian folkloric antidiabetic plant is severely understudied in terms of its bioactive phytochemical constituents. Antidiabetic guided isolation of the tubers and peels of D. dumetorum afforded three phytoecdysteroids bearing a cis-fused A/B ring junction including two new ones: 24-hydroxymuristerone A (1) and 24-hydroxykaladasterone (2), alongside the known muristerone A (3). Additionally, 2,2',7,7'-tetramethoxy-[1,1'-biphenanthrene]-4,4',6,6'-tetraol (4), batatasin I (5), and dihydroresveratrol (6) were isolated. Structural elucidation relied on spectroscopic, spectrometric methods, and comparison with existing literature. The ethyl acetate extracts of both the tubers and peels of D. dumetorum exhibited the highest phenolic content, correlating with potent antioxidant activity. Compounds 4 (IC50 = 0.10 mg/mL) and 6 (IC50 = 0.22 mg/mL) demonstrated superior inhibitory effects against α-glucosidase compared to acarbose (IC50 = 0.63 mg/mL). In contrast, compounds 3, 4, and 5 showed reduced α-amylase inhibition, with IC50 values of 2.58, 3.78, and 1.12 mg/mL, respectively, compared to acarbose (IC50 = 0.42 mg/mL). These observed bioactivities validate the traditional use of D. dumetorum and contribute valuable phytochemical data to the scientific literature of the species.

Antioxidant and anti-arthritic activity of Bombax buonopozense P. Beauv. leaves.

BACKGROUND AND AIM: Bombax buonopozense (Bombacaceae) leaves have been used traditionally for arthritis in south-western Nigeria. Therefore, the aim of the study was to investigate the antioxidant and anti-arthritic activity of B. buonopozense in Complete Freund adjuvant-induce arthritic wistar rats. EXPERIMENTAL PROCEDURE: The plant leaves methanol extract and fractions were screened for preliminary phytochemicals and brine shrimp lethality was determined. Total phenolic content (TPC), Total flavonoid content (TFC) as well as anti-oxidant activity of the extract and fractions were evaluated using 2,2-diphenyl-1-picrylhydrazyl (DPPH). Cyclophosphamide, gallic acid, and ascorbic acid were used as standards respectively. Anti-arthritic activity of crude methanol extract (BBME) at 100, 200 and 400mg/kg was evaluated in complete Freund's adjuvant (CFA) induced arthritis model in rats. Data were analysed using Graph pad prism version 5, two-way and one-way ANOVA, and Bonferroni post hoc test. RESULTS AND CONCLUSION: Phytochemical screening revealed the presence of flavonoids, alkaloids, and phenolics. The brine shrimp lethality assay of the crude extract and fractions gave LC50 value≥1000µg/mL, compared to Cyclophosphamide (LC50=224.7±0.35µg/mL). The BBME had TPC value of 19.8±0.56mg GAE/g, while the TFC of ethyl acetate fraction was the highest (173.5±0.05mg QE/g). The ethyl acetate fraction has the highest antioxidant activity (IC50=20.96±0.23µg/mL) as compared to ascorbic acid (2.8±0.01) and rutin (20.6±9.26µg/mL). BBME significantly reduced the paw circumference. BBME (400mg/kg) prevented biochemical changes to a greater extent than Celecoxib (20mg/kg). Bombax buonopozense leaves could be an effective antiarthritic and holds prospect in the treatment of rheumatoid arthritis.

Elemental evaluation, nutritional analysis, GC-MS analysis and ameliorative effects of Artocarpus communis J.R.Forst. & G.Forst. seeds' phytoconstituents on metabolic syndrome via in silico approach.

The nutritional as well as beneficial effects of the Artocarpus communis seed on metabolic syndrome complications have not been studied. In this research, the aim was to investigate the nutritional composition and beneficial effects of Artocarpus communis seeds' phytoconstituents on the p53 core, fat mass and obesity-associated (FTO) protein and cytochrome P450 CYP11A1 domains. The elements and phytochemicals in the seed were determined through atomic absorption spectroscopy assay and gas chromatography-mass spectrometry (GC-MS) analysis, respectively. Also, the compounds detected were docked to the p53 core, FTO protein and cytochrome P450 CYP11A1 domains protein. Artocarpus communis seed contains sodium (7.824 ± 0.0134 ppm), magnesium (10.187 ± 0.0239 ppm) and iron (1.924 ± 0.0017), while zinc and cadmium were undetected. Phenolics and flavonoids were the most abundant phytochemicals in the seed. Phytoconstituents, such as pentadecanoic acid, hexadecanoic acid and methyl ester, possessing different therapeutic effects were identified via GC-MS analysis. In A. communis seed, 3-methyl-4-nitro-5-(1-pyrazolyl) pyrazole and phenanthrene were able to bind more peculiarly and specifically to the p53 core, FTO protein and cytochrome P450 CYP11A1 domains. One of the important processes that were hypothesized for the recovery of metabolic syndrome in affected victims is shown by the molecular dynamics analysis, which shows that the binding of these chemicals to the targeted structure stabilized the proteins. Therefore, Artocarpus communis seeds could be a new strategy for the management of metabolic syndrome.Communicated by Ramaswamy H. Sarma.

Antispasmodic Effect of Alstonia boonei De Wild. and Its Constituents: Ex Vivo and In Silico Approaches.

BACKGROUND: Alstonia boonei, belonging to the family Apocynaceae, is one of the best-known medicinal plants in Africa and Asia. Stem back preparations are traditionally used as muscle relaxants. This study investigated the antispasmodic properties of Alstonia boonei Stem back and its constituents. METHOD: The freeze-dried aqueous Stem back extract of A. boonei, as well as dichloromethane (DCM), ethyl acetate, and aqueous fractions, were evaluated for their antispasmodic effect via the ex vivo method. Two compounds were isolated from the DCM fraction using chromatographic techniques, and their antispasmodic activity was evaluated. An in silico study was conducted by evaluating the interaction of isolated compounds with human PPARgamma-LBD and human carbonic anhydrase isozyme. RESULTS: The Stem back crude extract, DCM, ethyl acetate, and aqueous fractions showed antispasmodic activity on high-potassium-induced (K+ 80 mM) contractions on isolated rat ileum with IC50 values of 0.03 ± 0.20, 0.02 ± 0.05, 0.03 ± 0.14, and 0.90 ± 0.06 mg/mL, respectively. The isolated compounds from the DCM fraction were ß-amyrin and boonein, with only boonein exhibiting antispasmodic activity on both high-potassium-induced (IC50 = 0.09 ± 0.01 µg/mL) and spontaneous (0.29 ± 0.05 µg/mL) contractions. However, ß-amyrin had a stronger interaction with the two proteins during the simulation. CONCLUSION: The isolated compounds boonein and ß-amyrin could serve as starting materials for the development of antispasmodic drugs.

Phytochemical and antimicrobial studies of four species of Cola Schott & Endl. (Sterculiaceae).

The in-vitro antimicrobial evaluation of ethanol extracts of four species of Cola Schott & Endl. was done using human isolated strains of Staphylococcus aureus, Staphylococcus albus, Bacillus subtilis, Klebsiella pneumonia, Pseudomonas aeruginosa, Candida albicans, Aspergillus niger as test organisms. The assays were carried out by agar well diffusion, erythromycin and ketoconazole served as the control drugs. The leaf ethanol extracts of the plants were found to be more effective against the tested fungi than the bacteria at high concentrations. None of the extracts was active against Staphylococcus aureus. Plant extract of C. acuminata (P. Beauv.) Schott & Endl. and C. nitida (Vent) Schott & Endl. showed activity on S. albus at concentrations ranging from 10-150 mgml(-) having comparable diameters of zone of inhibition of 7.3+/-0.03-16.0+/-0.0 for C. acuminata and 10.0+/-0.0-19.0+/-0.0 for C. nitida. Also, these two species of Cola demonstrated activities on C. albicans and A. niger at concentrations ranging from 90-150mgml(-1) with relatively close diameters of zone of inhibition. Only C. acuminata inhibited the growth of K. pneumoniae at the MIC of 90mgml(-1) whereas, C. albicans was inhibited by C. acuminata, C. millenii K. Schum and C. gigantea A.Chev. at the MIC of 120mgml(-1). Phytochemical screening of the four species of Cola showed the presence of alkaloids, saponins, tannins and cardenolides in all the plants which apart from showing the probable closeness of the species could also be responsible for the observed activities. The antimicrobial property shown by the plant extracts is an evidence of the ethnomedicinal uses of the plants. The similarity observed in the phytochemical constituents and antimicrobial activities demonstrated by C nitida (Vent.) Schott & Endl., C. millenii and C.gigantea A. Chev. and C. acuminata suggest a probable closeness among these species. The results obtained in this study provide preliminary evidence of the chemotaxonomic significance of secondary metabolites and antimicrobial activities in infra-generic taxonomy of species of Cola.

Phytochemical and antimicrobial studies of four species of Cola Schott & Endl. (Sterculiaceae)

Abstract: The in-vitro antimicrobial evaluation of ethanol extracts of four species of Cola Schott & Endl. was done using human isolated strains of Staphylococcus aureus, Staphylococcus albus, Bacillus subtilis, Klebsiella pneumonia, Pseudomonas aeruginosa, Candida albicans, Aspergillus niger as test organisms. The assays were carried out by agar well diffusion, erythromycin and ketoconazole served as the control drugs. The leaf ethanol extracts of the plants were found to be more effective against the tested fungi than the bacteria at high concentrations. None of the extracts was active against Staphylococcus aureus. Plant extract of C. acuminata (P.Beauv.) Schott & Endl. and C. nitida (Vent) Schott & Endl. showed activity on S. albus at concentrations ranging from 10-150 mgmlˉ¹ having comparable diameters of zone of inhibition of 7.3±0.03-16.0±0.0 for C. acuminata and 10.0±0.0-19.0±0.0 for C. nitida. Also, these two species of Cola demonstrated activities on C. albicans and A. niger at concentrations ranging from 90-150mgmlˉ¹ with relatively close diameters of zone of inhibition. Only C. acuminata inhibited the growth of K. pneumoniae at the MIC of 90mgmlˉ¹ whereas, C. albicans was inhibited by C. acuminata, C. millenii K. Schum and C. gigantea A.Chev. at the MIC of 120mgmlˉ¹. Phytochemical screening of the four species of Cola showed the presence of alkaloids, saponins, tannins and cardenolides in all the plants which apart from showing the probable closeness of the species could also be responsible for the observed activities. The antimicrobial property shown by the plant extracts is an evidence of the ethnomedicinal uses of the plants. The similarity observed in the phytochemical constituents and antimicrobial activities demonstrated by C nitida (Vent.) Schott & Endl., C. millenii and C.gigantea A. Chev. and C. acuminata suggest a probable closeness among these species. The results obtained in this study provide preliminary evidence of the chemotaxonomic significance of secondary metabolites and antimicrobial activities in infra-generic taxonomy of species of Cola