RESUMEN
ETHNOPHARMACOLOGICAL RELEVANCE: Olea europaea L. and Hyphaene thebaica L. are commonly employed by traditional healers in Africa for treating and preventing hypertension, either individually or in a polyherbal preparation (Ifanosine). AIM OF THE STUDY: The primary aim was to assess the antihypertensive effects of Olea europaea L. leaves aqueous extract (OEL), Hyphaene thebaica L. mesocarp extract (HT), and the Ifanosine on isolated rat aorta rings. The secondary objective was to evaluate the clinical benefits of a new oral formulation of Ifanosine. MATERIALS AND METHODS: In vitro studies using an isometric transducer examined the antihypertensive effects of HT, OEL, and Ifanosine on rat aorta. Ussing chambers technic were employed to measure mucosal to serosal fluxes and total transepithelial electrical conductance (Gt) to assess the intestinal bioavailability of HT, OEL, and Ifanosine. HPLC was utilized to determine the phytochemical composition of OEL and HT extracts. Subchronic toxicity investigations involved two groups of rats, treated with either water (control) or Ifanosine at 5 g/kg for 28 days. Clinical benefits of the new Ifanosine formulation were evaluated in an observational study with 32 hypertensive patients receiving a fixed oral dose of 3.5 mg three times a day for 30 days. RESULTS: Aqueous extracts induced dose-dependent relaxation of rat aorta rings, with HT and OEL having higher IC50 values than Ifanosine (IC50 = 44.76 ± 1.35 ng/mL, 58.67 ± 1.02 ng/mL, and 29.46 ± 0.26 ng/mL, respectively). The pA2 values of OEL and HT were 1 and 0.6, respectively, while Ifanosine was 0.06. Intestinal bioavailability studies revealed better Prazosin bioavailability than plant extracts. Toxicological studies demonstrated the safety of Ifanosine, supported by histological examinations and biochemical parameters in rat blood. Biochemical analyses indicated flavonoids and phenolic acids as dominant active constituents. Clinical benefits in humans included reduced SBP, DBP, LDL-c, VLDL-c, and TAG, and increased HDL-c without overt adverse effects. CONCLUSION: This study validates the traditional use of OEL and HT for hypertension and advocates for alternative and combinatorial polyphytotherapy (ACP) to enhance traditional remedies.
Asunto(s)
Hipertensión , Olea , Humanos , Ratas , Animales , Antihipertensivos/farmacología , Antihipertensivos/uso terapéutico , Antihipertensivos/análisis , Olea/química , Hipertensión/tratamiento farmacológico , Extractos Vegetales/farmacología , Extractos Vegetales/uso terapéutico , Extractos Vegetales/química , Hojas de la Planta/química , Resultado del TratamientoRESUMEN
The ethanol extract of the leaves of Clerodendrum formicarum Gürke, a Lameacious plant of Cameroon, afforded two new long-chained esters named formadienoate-A (1) and B (2) along with two known constituents which have been obtained for the first time from C. formicarum. They include: hexacosyl-(E)-ferulate (3) and 26-hydroxyhexacosyl-(E)-ferulate (4). Structures of all the isolated constituents have been elucidated with the aid of 1D and 2D NMR spectroscopic techniques.
Asunto(s)
Ácidos Cafeicos/química , Clerodendrum/química , CamerúnRESUMEN
A bioassay-guided fractionation of methanol extracts of stem barks, combined with screening based on Epidermal Growth Factor (EGF)-responsive neural stem cells (erNSCs) differentiation assay, has been used. This study resulted in the isolation of 3,3'-di-O-methylellagic acid 1, 3,3'-di-O-methyl ellagic acid-4-O-beta-D-xylopyranoside 2, ellagic acid 3, and arjunolic acid 4. Among them, compounds 1 and 2 exhibit potent induction of neuronal differentiation in neurosphere stem cells with no cytotoxic effect. These results indicate that compounds 1 and 2 may be useful as pharmacological agents for the treatment of neurodegenerative diseases. These compounds may account, for the use of T. superba in folk medicine for nervous system and mental disorders.
Asunto(s)
Diferenciación Celular/efectos de los fármacos , Ácido Elágico/farmacología , Neuronas/efectos de los fármacos , Células Madre/efectos de los fármacos , Terminalia/química , Animales , Células Cultivadas , Fraccionamiento Químico , Ácido Elágico/análogos & derivados , Ácido Elágico/química , Ácido Elágico/aislamiento & purificación , Ratones , Neuronas/citología , Células Madre/citologíaRESUMEN
Bioassay-guided fractionation of the CHCl (3)-soluble extract of the stem bark of Crassocephalum biafrae (Asteraceae) resulted in the isolation of three new dihydroisocoumarins, named biafraecoumarins A ( 1), B ( 2), and C ( 3); two known triterpenes ( 4 and 5); and a known ceramide ( 6). The structures of the new compounds were established as 7-but-15-enyl-6,8-dihydroxy-3( R)-penta-9,11-dienylisochroman-1-one ( 1), 7-butyl-6,8-dihydroxy-3( R)-penta-9,11-dienylisochroman-1-one ( 2), and 7-butyl-6,8-dihydroxy-3( R)-pent-10-enylisochroman-1-one ( 3) using spectroscopic data. Compounds 1- 3 exhibit low to significant antimicrobial activities against Escherichia coli, Bacillus subtilis, Staphylococcus aureus, Pseudomonas picketti, Trichphyton longifusus, Aspergillus flavus, Microsporum canis, Fusarium solani, Candida albicans, and Candida glabrata.
Asunto(s)
Antiinfecciosos/farmacología , Asteraceae/química , Isocumarinas/farmacología , Antiinfecciosos/química , Antiinfecciosos/aislamiento & purificación , Isocumarinas/química , Isocumarinas/aislamiento & purificación , Pruebas de Sensibilidad MicrobianaRESUMEN
Antibacterial bioassay-guided fractionation of the methanol extract of the stem bark of Terminalia superba led to the isolation of four new triterpene glucosides (1-4) which were characterized as 2 alpha,3 beta-dihydroxyolean-12-en-28-oic acid 28-O-beta-D-glucopyranoside (1), 2 alpha,3 beta, 21 beta-trihydroxyolean-12-en-28-oic acid 28-O-beta-D-glucopyranoside (2), 2 alpha,3 beta, 29-trihydroxyolean-12-en-28-oic acid 28-O-beta-D-glucopyranoside (3) and 2 alpha,3 beta,23,27-tetrahydroxyolean-12-en-28-oic acid 28-O-beta-D-glucopyranoside (4) together with the known triterpene 2 alpha,3 beta,23-trihydroxyolean-12-en-28-oic acid (5). Structures were established by spectroscopic methods including one- and two-dimensional NMR, EI-MS and HR-EI-MS. The antibacterial activity of 1-5 was also investigated against two gram-positive (Bacillus subtilis, Staphylococcus aureus), and four gram-negative (Escherichia coli, Shigella flexenari, Pseudomonas aeruginosa, Salmonella typhi) bacterial strains.
Asunto(s)
Antibacterianos/aislamiento & purificación , Glicósidos/aislamiento & purificación , Extractos Vegetales/aislamiento & purificación , Terminalia/química , Triterpenos/aislamiento & purificación , Antibacterianos/química , Antibacterianos/farmacología , Glicósidos/química , Glicósidos/farmacología , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Espectrometría de Masas , Estructura Molecular , Corteza de la Planta , Extractos Vegetales/química , Extractos Vegetales/farmacología , Tallos de la Planta , Triterpenos/química , Triterpenos/farmacologíaRESUMEN
Six new unusual C-4'-prenylated flavonols, dorsilurins F-K (1-6), together with six known compounds were isolated from the roots of Dorstenia psilurus, and their structures were elucidated on the basis of spectroscopic evidence. The isolated compounds exhibited moderate to low alpha-glucosidase inhibitory activity. Dorsilurin F (1), with three unmodified prenyl groups, was the most active, while dorsilurin K (6), with only one unmodified prenyl group, was the least active compound. Furthermore, NMR data of dorsilurin C (7), isolated some years ago from the same plant, have been revised.
Asunto(s)
Flavonoides/aislamiento & purificación , Flavonoides/farmacología , Inhibidores de Glicósido Hidrolasas , Moraceae/química , Plantas Medicinales/química , Camerún , Flavonoides/química , Estructura Molecular , Resonancia Magnética Nuclear Biomolecular , Raíces de Plantas/químicaRESUMEN
Fractionation of stem barks of Terminalia superba yielded two new ellagic acid derivatives, 3,4'-di-O-methylellagic acid 3'-O-beta-D-xylopyranoside (1) and 4'-O-galloy-3,3'-di-O-methylellagic acid 4-O-beta-D-xylopyranoside (2) together with known 3,3'-di-O-methylellagic acid, ellagic acid and 3,3'-di-O-methylellagic acid 4'-O-beta-D-xylopyranoside. Compounds (1) and (2) showed significant alpha-glucosidase inhibition activity and possessed significant immunoinhibitory activities with no cytotoxic effects.
Asunto(s)
Ácido Elágico/análogos & derivados , Ácido Elágico/farmacología , Inhibidores Enzimáticos/aislamiento & purificación , Inhibidores Enzimáticos/farmacología , Inhibidores de Glicósido Hidrolasas , Inmunosupresores/aislamiento & purificación , Inmunosupresores/farmacología , Terminalia/química , Proliferación Celular/efectos de los fármacos , Ácido Elágico/aislamiento & purificación , Hidrólisis , Luminiscencia , Espectroscopía de Resonancia Magnética , Fagocitos/efectos de los fármacos , Fitohemaglutininas/farmacología , Corteza de la Planta/química , Extractos Vegetales , Estallido Respiratorio/efectos de los fármacos , Espectrometría de Masa por Ionización de Electrospray , Espectrofotometría Infrarroja , Espectroscopía Infrarroja por Transformada de Fourier , Linfocitos T/efectos de los fármacosRESUMEN
Four alkaloids named piperumbellactams A-D (1-4) were isolated from branches of Piper umbellatum together with known N-hydroxyaristolam II (5), N-p-coumaroyl tyramine (6), 4-nerolidylcatechol (7), N-trans-feruloyltyramine, E-3-(3,4-dihydroxyphenyl)-N-2-[4-hydroxyphenylethyl]-2-propenamide, beta-amyrin, friedelin, apigenin 8-C-neohesperidoside, acacetin 6-C-beta-d-glucopyranoside, beta-sitosterol, its 3-O-beta-d-glucopyranoside and its 3-O-beta-d-[6'-dodecanoyl]-glucopyranoside. Glycosidase inhibition, antioxidant and antifungal activities of these compounds were evaluated. Compounds 1-3 showed moderate alpha-glucosidase enzyme inhibition with IC50 values 98.07+/-0.44, 43.80+/-0.56 and 29.64+/-0.46, respectively. In DPPH radical scavenging assay, compounds 2, 3 and 6 showed potent inhibitory activity while compounds 4, 5 and 7 showed potent antifungal activity.
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Alcaloides/química , Antifúngicos/química , Compuestos Heterocíclicos de 4 o más Anillos/química , Lactamas/química , Piper/química , Extractos Vegetales/química , Alcaloides/aislamiento & purificación , Alcaloides/farmacología , Antifúngicos/farmacología , Depuradores de Radicales Libres/química , Depuradores de Radicales Libres/aislamiento & purificación , Compuestos Heterocíclicos de 4 o más Anillos/aislamiento & purificación , Compuestos Heterocíclicos de 4 o más Anillos/farmacología , Lactamas/aislamiento & purificación , Lactamas/farmacología , Estructura Molecular , Componentes Aéreos de las Plantas/química , Extractos Vegetales/farmacologíaRESUMEN
Three new prenylated anthranoids, harunmadagascarins C (1) and D (2) and kenganthranol D (3), together with three known compounds (4-6) were isolated from the leaves of Harungana madagascariensis. Their structures were assigned by spectroscopic methods and by comparison with literature data. In the three new natural products 1-3, one or two prenyl groups are incorporated in furan, pyran, or cyclohexane rings in four different modes of annulation. Compounds 2, 4, and 6 were strongly active against the Gram-positive Bacillus megaterium.