Dendroochreatene (1), a new phenanthrene derivative with a spirolactone ring, was isolated from the whole Dendrobium ochreatum plant together with 11 known compounds (2-12). The structure of the new compound was elucidated spectroscopically and phenolic compounds were firstly reported from D. ochreatum. Moscatilin (4), major compound isolated from D. ochreatum, was found to be cytotoxic toward H460 lung-cancer cells, with an IC50 value of 147.3 ± 0.9 µM, while loddigesiinol C (7), C-α-methoxy derivative was inactive.

The gold-catalyzed cyclization of 2,2-bis(3-arylprop-2-yn1-yl)malonic acid has been proposed as an efficient approach to substituted 3,8-dibenzyl-2,7-dioxaspiro[4.4]nonane-1,6-diones. The reaction proceeds smoothly in mild reaction conditions to give the desired products in quantitative yields in the presence of variously substituted starting materials. In addition, the synthesis of γ-arylidene spirobislactone bearing different substituents on the two aromatic rings has been achieved. This kind of compound could be of great interest in pharmaceutical science given the widespread presence of this scaffold in bioactive natural and synthetic products.

Objective:To determine whether taking spirolactone orally after H-UPPP may relieve laryngeal edema and complications for patients with obstructive sleep apnea（OSA）. Method:Fifty patients with OSA to undergo H-UPPP operation were randomly divided equally to the intervention group（taking spirolactone 20 mg orally twice a day for 7 days after H-UPPP） or the control group, all patients received conventional therapy after H-UPPP including anti-infection, hemostatic treatment, fluid replacement and expectorant by fogged absorption. The pharyngeal wound, diet, sleep and speaking pronunciation of all patients in each group were evaluated every other day in 7 days postoperation. The minimum oxygen saturation of blood（SaO2） during sleep at night each day and the period needed for staphyledema resolution of all patients were recorded and compared between each group. Result:Postoperatively, the intervention group had significantly slighter bleeding at wound site, better sleep and more legible speaking pronunciation than the control group after 3 days to 5 days（P<0.05）. The wound dehiscence of the intervention group was significantly slighter than the control group within 7 days after operation（P<0.05）. During 3 days to 7days after operation, the intervention group had a significantly better diet than the control group（P<0.05）. The average minimum SaO2during sleep at night in the intervention group was significantly higher than that in the control group from 3 days to 5 days post operation（P<0.05）. Period needed for staphyledema resolution in the intervention group（4.1±1.5） days was significantly shorter than that in the control group（5.9±1.8） days （P<0.05）. Conclusion:Taking spirolactone orally after H-UPPP may relieve laryngeal edema and complications for OSA patients, and it will also shorten the period needed for staphyledema resolution.
目的：探讨在改良悬雍垂腭咽成形术（H-UPPP）术后口服螺内酯能否减轻OSA患者咽部水肿和并发症的发生。 方法：采用随机数字法，将50例拟行H-UPPP手术的OSA患者随机平均分为螺内酯组和对照组，2组患者术后均予以相同的抗感染、止血、补液及雾化祛痰治疗，螺内酯组患者同时口服螺内酯20 mg，2次/d，使用7 d。隔天评估各组患者术后7 d内的咽部伤口、进食、睡眠及言语发声情况，记录患者每天夜间睡眠的最低血氧饱和度（SaO2）以及术后悬雍垂水肿消退所需的时间。 结果：在术后3~5 d，螺内酯组在伤口出血、睡眠情况及言语发声方面好于对照组（P<0.05）；在伤口裂开方面，螺内酯组在术后7 d内均好于对照组（P<0.05）；在术后3~7 d，螺内酯组在进食情况方面好于对照组（P<0.05）；在术后3~5 d，螺内酯组的夜间睡眠最低SaO2平均值高于对照组（P<0.05）。螺内酯组术后悬雍垂水肿消退所需时间为（4.1±1.5） d，对照组为（5.9±1.8） d，差异有统计学意义（P<0.05）。 结论：H-UPPP术后口服螺内酯能够减轻OSA患者术后的咽部水肿和并发症，并可以缩短悬雍垂水肿消退所需的时间。.

Different models of population pharmacokinetics (PPK) of cyclosporin have been established in various populations. However, the cyclosporin PPK model in patients with pediatric refractory nephrotic syndrome (PRNS) has yet to be constructed. The present study aimed to establish the cyclosporin PPK model in PRNS, and to identify factors that may account for any variability. Chinese patients with PRNS treated with cyclosporin between June 2014 and June 2018 at the Children\'s Hospital of Fudan University (Shanghai, China) were retrospectively analyzed. The impact of demographic features, laboratory parameters and concomitant medications was evaluated. A total of 18 PRNS patients from real-world studies were analyzed by non-linear mixed-effects modeling. A one-compartment model with first-order absorption and elimination was selected as the appropriate model in PRNS. Body weight (WT) and spirolactone intake were included as significant covariates for the apparent oral clearance (CL/F), and the WT was revealed to significantly influence the apparent volume of distribution (V/F). The final covariate models were as follows: CL/F=80.7 × (WT/70)0.75 × (1-0.265×θspirolactone), and V/F=2,030 × (WT/70), where θspirolactone is the coefficient of spirolactone. The inter-individual variability in CL/F and V/F was 44.6 and 53.1%, respectively. In conclusion, in the present study, a cyclosporin PPK model for patients with PRNS was successfully constructed, and the presence of a clinically significant interaction between spirolactone and cyclosporin in PRNS patients was determined based on real-world studies, indicating that concomitant medication with spirolactone was able to reduce cyclosporin clearance in the patients with PRNS.

A general methodology for the synthesis of different steroidal 17-spirolactones is described. This method uses lithium acetylide of ethyl propiolate as the three carbon synthon and the method was successfully applied for the process development of drospirenone.

With this study, we explored the identity and chemistry of fungal endophytes from the roots of yerba mansa [Anemopsis californica (Nutt.) Hook. & Arn. (Saururaceae)], a botanical traditionally used to treat infection. We compared the diversity of fungal endophytes isolated from a wild-harvested A. californica population, and those from plants cultivated for one year in a greenhouse environment. The wild-harvested population yielded thirteen fungal strains (eleven unique genotypes). Of the extracts prepared from these fungi, four inhibited growth of Staphylococcus aureus by >25% at 20 µg/mL, and three inhibited growth of Pseudomonas aeruginosa by ≥20% at 200 µg/mL. By comparison, A. californica roots after one year of cultivation in the greenhouse produced only two unique genotypes, neither of which displayed significant antimicrobial activity. The fungus Chaetomium cupreum isolated from wild-harvested A. californica yielded a new antimicrobial spirolactone, chaetocuprum (1). An additional fourteen known compounds were identified using LC-MS dereplication of the various fungal endophytes. This study provides new insights into the identity and chemistry of A. californica fungal endophytes, and demonstrates the importance of considering growing conditions when pursuing natural product drug discovery from endophytic fungi.