RESUMEN
Three new furanosesterterpene tetronic acids, sulawesins A-C (1-3), were isolated from a Psammocinia sp. marine sponge, along with the known compounds ircinins-1 (4) and -2 (5). Although ircinins-1 and -2 were previously isolated as (+)- or (-)-enantiomers from marine sponges, we isolated them as enantiomeric mixtures. Sulawesins A and B possess a new carbon skeleton with a 5-(furan-3-yl)-4-hydroxycyclopent-2-enone moiety and were also found to be diastereomeric mixtures of four isomers by an HPLC analysis with a chiral-phase column. Sulawesin C has a dimeric structure of ircinin-1 and is the first dimer in this family. USP7, a deubiquitinating enzyme, is an emergent target of cancer therapy, and the isolated compounds inhibited USP7 with IC50 values in the range of 2.7-4.6 µM.
Asunto(s)
Furanos/aislamiento & purificación , Furanos/farmacología , Poríferos/química , Sesterterpenos/aislamiento & purificación , Sesterterpenos/farmacología , Terpenos/aislamiento & purificación , Terpenos/farmacología , Animales , Relación Dosis-Respuesta a Droga , Ensayos de Selección de Medicamentos Antitumorales , Furanos/química , Humanos , Indonesia , Concentración 50 Inhibidora , Biología Marina , Estructura Molecular , Sesquiterpenos , Sesterterpenos/química , Estereoisomerismo , Relación Estructura-Actividad , Terpenos/química , Ubiquitina Tiolesterasa , Peptidasa Específica de Ubiquitina 7RESUMEN
Misuse of antibiotics led to the world wide spread of antimicrobial resistance threatening human lives. The notable resistance of bacterial cells to antibiotics and immune system is the difficulty associated with biofilm-linked illnesses. Natural products from plant origin with antibiofilm activity could provide more therapeutic activity with fewer adverse effects. Carissa L. is a potential drug candidate that can be considered as an agro-food waste sustainable virulence inhibitor source. This mini-review sheds light on recent studies dealing with the anti-virulence potential of Carissa species and its different mechanisms of action. The traced articles revealed that Carissa species exhibited potent antibiofilm, anti-quorum sensing, hyaluronidase inhibitory and anti-adhesion potentials, in addition to violacein, and swimming motility inhibition activities. Ursolic acid, oleanolic acid, and methyl oleanate are the main phytoconstituents of Carissa with claimed virulence inhibitory potentials. Carissa species are safe, valuable, and effective anti-virulence drugs suppressing pathogenicity when compared to conventional antibiotics.
RESUMEN
BACKGROUND: The underlying etiology of recurrent aphthous stomatitis (RAS) is unclear and treatment aims to provide symptomatic and faster relief. This study compared the efficacy of diode laser, a herbal combination of Acacia nilotica and Licorice (A and L) and Amlexanox in the management of RAS. MATERIAL AND METHODS: Sixty patients with minor aphthae were selected and randomly divided into four groups of 15 each. Group I and II received adhesive preparations of a herbal mixture of A and L and a 2 mg Amlexanox paste respectively, group III received diode laser and the fourth group (control) used a placebo. Ulcer size, pain score were recorded on days 1, 2 and 5. RESULTS: Laser group showed the statistically highest mean percentage (%) of reduction in pain scores and ulcer size than the other groups. The mean % of reduction in pain scores was 43.3+20.0 at day 2 and 67.8+21.5 % at day 5 in the laser group while Amlexanox group demonstrated a 29.8 +11.3 and 61.9+24.5 mean % of reduction in pain scores at day 2 and 5 respectively. A and L group showed a lower mean % of reduction in pain scores than laser and Amlexanox groups with a 22.2+10.5 and 43.4+15.8 mean % reduction in pain scores at day 2 and day 5 respectively. Similarly the highest mean % of reduction in ulcer size was seen in the laser group being 52.7+19.8 at day 2 and 85.1+22.0 at day 5, while it was 48.1+16.5 at day 2 and 77.8+28.7 at day 5 in the Amlexanox group and 42.0+11.5 at day 2 and 63.0+20.5 at day 5 in the A and L group. CONCLUSIONS: All treatment modalities reduced pain and ulcer size than placebo group. Laser therapy demonstrated the highest percentage of reduction of pain score and ulcer size. Key words:Aphthous stomatitis, laser, herbal plants, Acacia nilotica, Licorice.
RESUMEN
A significant increase in body weight with remarkable increase in total food intake and significant increase in protein efficiency ratio were observed following oral administration of R. graveolens ether extract (500 mg/kg body wt) to growing rats for 3 weeks. Serum albumin was significantly decreased after administration of declofenac (15 mg/kg body wt). Albumin/globulin ratio decreased significantly on administration of E. peplus ether extract (500 mg/kg body wt). No significant changes were observed in other biochemical and nutritional parameters on administration of either of the extracts or declofenac. However, only a significant elevation of alkaline phosphatase was noticed during treatment with R. graveolens. The results suggest that both plant extracts have no harmful effect on nutritional status and are safe towards kidney functions, while Euphorbia is more safe than Ruta in relation to liver functions.
Asunto(s)
Antiinflamatorios/farmacología , Euphorbia/química , Estado Nutricional/efectos de los fármacos , Extractos Vegetales/farmacología , Plantas Medicinales , Ruta/química , Administración Oral , Fosfatasa Alcalina/metabolismo , Animales , Antiinflamatorios/administración & dosificación , Peso Corporal/efectos de los fármacos , Ingestión de Energía , Fitoterapia , Extractos Vegetales/administración & dosificación , Ratas , Ratas Endogámicas , Seguridad , Albúmina Sérica/análisisRESUMEN
The purpose of the present study is to formulate Glycyrrhiza glabra root and rhizome aqueous ethanolic extract in microemulsion carrier systems intended for transdermal delivery of incorporated antioxidant actives, flavonoids and polyphenols. The results obtained reveal that the microemulsion system ME3 possesses optimum properties regarding drug content (flavonoids and polyphenols), viscosity, pH, particle size and polydispersity index, zeta potential, stability, permeation of actives and hence possesses high in vitro and ex vivo antioxidant efficacy. These results indicate also that this microemulsion shows approximately 13-fold higher ex vivo antioxidant capacity compared with the liquorice extract solution. In addition, the proposed microemulsion is simple to dispense, cost effective and provides high patient compliance and convenience because of simple topical application and avoidance of non-comfortable oral or parenteral administration.