RESUMEN
The first investigation of chemical composition in seed kernels of Caesalpinia cucullata Roxb. resulted in the separation of four new cassane diterpenes, including three furanoditerpenes (1, 2 and 4) and one tricyclic type (3). It was the first found cassane diterpenoids from this plant. Their gross structures were elucidated by means of comprehensive spectroscopic analysis (UV, IR, NMR, HRESIMS) as well as electronic circular dichroism (ECD) calculation. The compound 1 possess a rare isomerized dihydrofuran ring in structure framework. In bioassay, compounds 1-4 exhibited moderate anti-inflammatory activity by inhibiting production of NO in LPS-induced RAW 264.7 cells.
Asunto(s)
Caesalpinia , Diterpenos , Antiinflamatorios/análisis , Antiinflamatorios/farmacología , Caesalpinia/química , Diterpenos/química , Lipopolisacáridos/farmacología , Estructura Molecular , Semillas/químicaRESUMEN
BACKGROUND: Jingshu Keli (or Jingshu granules), a traditional Chinese medicine, are widely used for treating cervical spondylotic radiculopathy in China; however, no randomized, double-blind, controlled study has verified their effectiveness. PURPOSE: To evaluate the efficacy and safety of Jingshu Keli for the treatment of cervical spondylotic radiculopathy in a randomized controlled trial. DESIGN: From August 2015 to July 2017, a multicenter, randomized, double-blind, placebo-controlled trial was conducted at 13 large- and medium-sized hospitals in China. PATIENT SAMPLE: A total of 360 and 120 patients were initially enrolled in the Jingshu and control groups, respectively; 386 patients completed the study, with 299 in the Jingshu group and 87 in the control group. OUTCOME MEASURES: The main index for evaluating the curative effect was the pain score on a visual analogue scale (VAS; 0-100 points). METHODS: All patients were administered a bag of Jingshu Keli or placebo 3 times a day for 4 weeks, and were interviewed at the second and fourth weeks. The decrease in pain scores and rate of change in pain scores after treatment were calculated, related laboratory indices were reviewed, and adverse reactions were recorded. RESULTS: In the Per Protocol Set (PPS) analysis, the baseline pain VAS scores in the control and Jingshu groups were 49.31 â± â6.97 and 50.06 â± â7.33, respectively, with no significant difference between the groups (P â> â0.05). While there were no differences at 2 weeks between groups, at four weeks the pain VAS scores in the control and Jingshu groups decreased by 12.86 â± â13.45 and 22.72 â± â15.08, respectively relative to the values at baseline, with significant group differences (P â< â0.0001). While there were similar significant differences between the groups (P â< â0.0001) in the Full Analysis Set (FAS) analyses neither group achieved the minimal clinically important difference at any time point. CONCLUSIONS: Jingshu Keli are effective for the treatment of cervical spondylotic radiculopathy. TRANSLATIONAL POTENTIAL STATEMENT: This is the first prospective, multicenter, randomized, double-blind, placebo-controlled clinical trial that confirmed the clinical efficacy and safety of Jingshu Keli for treating cervical spondylotic radiculopathy, which can provide evidence for clinical treatment.
RESUMEN
Eight unknown pentacyclic triterpenoids (1-4 and 8-11), along with eight known analogues (5-7 and 12-16) have been first isolated from the dried whole plant of Leptopus chinensis. The structures of the new compounds were determined by comprehensive spectroscopic methods, including 1D and 2D NMR, as well as HRESIMS measurements. Meanwhile, the hepatoprotective activities of the isolated compounds were preliminarily evaluated, and the results indicated that compounds 2, 5 and 16 possess potent protective effects on tert-butyl hydroperoxide (t-BHP)-induced oxidative injury in vitro, and further study revealed that 16 significantly alleviates t-BHP-induced hepatotoxicity by effectively improving cell viability and decreasing reactive oxygen species (ROS) generation and the cell apoptosis rate in HepG2 cells.
