Discovery and Bioinspired Synthesis of Salpratone A.

Salpratone A (1), a novel abietane diterpenoid containing a unique cis-fused A/B ring, was isolated from Salvia prattii. Bioactivity studies showed that 1 has potent activity in inhibiting platelet aggregation induced by multiple agonists as well as antithrombotic efficacy in the FeCl3-induced rat in vivo thrombosis model. Furthermore, a bioinspired synthesis of 1 from the abundant natural product ferruginol was achieved in 6 steps with a 22% overall yield. The key steps include a stereoselective allyl oxidation and a subsequent regioselective Meinwald rearrangement.

11,12-seco-Abietane-type diterpene lactones with potential antiplatelet activity from Salvia prattii.

Eleven new abietane-type diterpene lactones, salpratlactones D-N (1-11), including five 11,12-seco-11-nor-abietane diterpenes (1-5), four 11,12-seco-abietane diterpenes (6-9), two 20(10 â†’ 5)-abeo-4,5;11,12-bis-seco-abietane diterpenes (10-11), and two known analogues (12-13), were characterized from Salvia prattii. Notably, compounds 1-3 were characterized by a unique linear 6/6/6 tricyclic skeleton. The structures were established by spectroscopic data interpretation, calculated NMR-DP4+ and electronic circular dichroism analysis, as well as single-crystal X-ray diffraction. A bioactivity study showed that 1, 2, 5, 11, and 12 can potently inhibit platelet aggregation induced by arachidonic acid (AA), with IC50 values of 5.66-16.10 µg/ml, stronger than aspirin. In addition, the lactate dehydrogenase assay showed that they had no effect on platelet integrity. Structurally, the same 1,2-benzopyrone fragments of 1, 2, and 5 should be the important pharmacophore for antiplatelet activity.

[A clinical study of pelvic floor electrical stimulation in treatment of overactive bladder].

OBJECTIVE: To observe the efficacy of electrical stimulation in treatment of overactive bladder (OAB). METHODS: Patients (n = 60) with overactive bladder were randomly divided into 2 groups. Electrical stimulation group (n = 35) used an instrument for electrical stimulation through a special vagina or rectum probe transfer current (8-70 mA), for 20 min, qd, for 20-30 times. Medical group (n = 25) received oral tolterodine 2 mg, bid, for 2-4 weeks. RESULTS: The total effective rate and cure rate were 74%, 37% in electrical stimulation group and 76%, 40% in medical group, respectively, showing no significant difference between two groups (P > 0.05). While patients' satisfactory rate was significantly higher in electrical stimulation group than in medical group (P < 0.05). Side effects were more commonly seen with tolterodine. CONCLUSIONS: Electrical nerve stimulation is effective and safe for overactive bladder. Further studies are needed to show the long term efficacy and cost-effectiveness.

[Photosystem II characteristics of nine Gramineae species in southern Taklamakan Desert].

Taking the Gramineae species Elytrigia intermedia, Avena sativa, Bromus inermis, Elymus sibiricus, Leymus tianschanicus, Elymus dahuricus, Festuca elata, Agropyron cristatum, and Puccinellia distans at the edge of Cele Oasis in southern Taklimakan Desert as test objects, this paper monitored their fast chlorophyll fluorescence kinetics after 20 minutes adaptation in darkness, compared their photosystem II (PS II) characteristics, and analyzed their adaptability to the local environment. Among the nine Gramineae species, L. tianschanicus and E. dahuricus had markedly higher values of maximum fluorescence yield (F(m)), maximum photochemical efficiency of PS II (F(v)/F(m)), and active reaction centers per cross-section (RC/CS0), but lower values of minimum fluorescence yield (F0), absorption flux per reaction center (ABC/RC), maximal trapping flux per reaction center (TR0/RC), flux of dissipated excitation energy per reaction center (DI0/RC), and initial slope of fluorescence intensity (M0), as compared to F. elata, A. cristatum, and P. distans, whereas E. intermedia, A. sativa, B. inermis, and E. sibiricus had a medium level of the values. These results suggested that all the test pasture species were suffered from the severe environmental conditions of Cele Oasis to some extent, as indicated by the inactivation of PS II reaction center and the depression of electron transport chain. L. tianschanicus and E. dahuricus were least impacted, while F. elata, A. cristatum, and P. distans were most impacted.