Euphejolkinolide A, a new ent-abietane lactone from Euphorbia peplus L. with promising biological activity in activating the autophagy-lysosomal pathway.

A new ent-abietane diterpenoid, named Euphejolkinolide A (1), was isolated from the whole plant of Euphorbia peplus L. Its structure, including absolute configurations, was determined by spectroscopic analyses and was corroborated by single-crystal X-ray diffraction analysis. This new compound was assessed for its activity to induce lysosome biogenesis through Lyso-Tracker Red staining, in which compound 1 could significantly induce lysosome biogenesis. In addition, quantitative real-time PCR (qRT-PCR) analysis demonstrated a direct correlation between the observed lysosome biogenesis and the transcriptional activation of the lysosomal genes after treatment with the compound 1. Moreover, compound 1 promoted autophagic flux by upregulating LC3-II and downregulating SQSTM1 in both human microglia cells and U251 cells, which is required for cellular homeostasis. Further results suggested 1 induced lysosome biogenesis and autophagy which was mediated by TFEB (transcription factor EB). The structure activity relationships (SAR) analysis suggested that the carbony1 at C-7 in 1 might be a key active group. Overall, the current data suggested that 1 could be a potential compound for lysosome disorder therapy by induction of autophagy.

[An integrative metabolomics and network pharmacology method for exploring bioactive components and preliminary pharmacodynamics in medicinal parts of Harrisonia perforata].

In this paper,metabolomics and network pharmacology were used to investigate the bioactive components of Harrisonia perforata and their possible mechanisms of action. Metabolites in the flowers,fruits,branches,leaves and stalks of H. perforata were analyzed by ultra-high performance liquid chromatography-quadrupole-time-of-flight mass spectrometry. Meanwhile,multiple statistical analysis methods including principal component analysis( PCA) and orthogonal partial least squares discriminant analysis( OPLS-DA)were applied to screen and identify differential compounds. With metabolomics method,9 differential compounds were preliminarily identified from leaves and other non-traditional medicinal parts. Subsequently,these compounds were explored by using network pharmacology. With gastrointestinal absorption and drug-likeness as limiting conditions,they were imported into the Swiss ADME,from which 7 compounds with potential medicinal activity were obtained. Then,their targets were predicted by PharmMapper,with Human Protein Targets Only and Normalized Fit Score>0. 9 set as limiting conditions,and 60 standardized potential targets were identified with Uniprot. KEGG( Kyoto encyclopedia of genes and genomes) pathway data was obtained using metascape and the " potential active ingredients-target-pathway" network was constructed with Cytoscape 3. 7. 2. The enrichment analysis of KEGG demonstrated that the 60 targets were enriched in 78 signaling pathways( min overlap: 3,P value cutoff: 0. 01,min enrichment: 1. 5),many of which are related to anti-bacteria,anti-inflammation and anti-virus,such as IL-17 signaling pathway,RIG-I-like receptor signaling pathway and NOD-like receptor signaling pathway. Finally,depending on the clinical activity of H. perforata,the relevant signaling pathways were analyzed through experimental data and literature. Dehydroconiferyl alcohol was reported to have the anti-inflammatory effect and perforamone D to possess the antimycobacterial activity. The KEGG pathway enrichment analysis showed that dehydroconiferyl alcohol could act on the Alzheimer's disease( AD) signaling pathway by targeting CDK5 R1 and BACE1. ACh E inhibitor is the most promising drug to treat AD,while dehydroconiferyl alcohol has been proved to inhibit ACh E according to literature. The experimental results revealed that the extract of leaves of H. perforata can effectively inhibit the growth of Staphylococcus aureus. These are consistent with the enrichment analysis results of KEGG. This study explored the bioactive components and pharmacodynamics of the leaves of the H. perforata,laying a theoretical foundation for its in-depth development and rational application.

New Secodaphnane-Type Alkaloids with Cytotoxic Activities from Daphniphyllum angustifolium Hutch.

One new Daphniphyllum alkaloid, daphnioldhanol A (1), together with three known ones, were isolated from the stem part of Daphniphyllum angustifolium Hutch. Their structures were elucidated by spectroscopic methods and comparing with the literature data. Compound 2 is a new natural product, but known by synthesis as a racemate. Compound 1 exhibited week cytotoxic activity against Hela cell line with IC50 of 31.9 µM.

Jatrophane Diterpenoids from the Seeds of Euphorbia peplus with Potential Bioactivities in Lysosomal-Autophagy Pathway.

Euphopepluanones F - K (1 - 4), four new jatrophane type diterpenoids were isolated from the seeds of Euphorbia peplus, along with eight known diterpenoids (5 - 12). Their structures were established on the basis of extensive spectroscopic analysis and X-ray crystallographic experiments. The new compounds 1 - 4 were assessed for their activities to induce lysosomal biogenesis through LysoTracker Red staining. Compound 2 significantly induced lysosomal biogenesis. In addition, compound 2 could increase the number of LC3 dots, indicating that it could activate the lysosomal-autophagy pathway.

Three new diterpenoids from Euphorbia peplus.

Three new diterpenoids (1-3) (two abietane type diterpenoids and a paralianone type diterpenoid), together with four known compounds (4-7) were isolated from the whole plants of Euphorbia peplus. Their structures were elucidated through spectroscopic analysis and physicochemical characteristics. The cytotoxic activities of compounds 1-7 against five human tumour cell lines were evaluated, however, they were inactive at the concentration of 40 µM. The compound 3 enhanced lysosomal biogenesis with Lyso Tracker staining intensity of 132.6%.

Clinically randomized controlled trials of moxibustion with salt in bamboo circle for treatment of periarthritis of shoulder / 中国针灸

<p><b>OBJECTIVE</b>To assess the clinical therapeutic effect of moxibustion with salt in bamboo circle on periarthritis of shoulder. METHODS Eighty-six cases were randomly divided into a salt-moxibustion group and an electroacupuncture group, 43 cases in each group. The salt-moxibustion group was treated by moxibustion with salt in bamboo circle on the part of obvious pain and hot compress moxibustion on its periphery. The electroacupuncture group was treated with electroacupuncture at Jianyu (LI 15), Jianliao (TE 14), Jianzhen (SI 9), etc. After treatment, the analgesic effect and improvement degrees of active function of the shoulder joint were observed and 3 months later they were followed-up.</p><p><b>RESULTS</b>The two therapies had analgesic effect and could improve active function of shoulder joint, but the salt-moxibustion group in the transient analgesic effect and the improvement degree of active function of the shoulder joint was better than the electroacupuncture group (P< 0.01, P < 0.05). Follow-up survey showed good clinical therapeutic effects in the two groups. The effective rates of pain and active function of shoulder joint were 97.7% and 93.0% in the salt-moxibustion group and 93.0% and 88.4% in the electroacupuncture group, respectively, with no significant differences between the two groups.</p><p><b>CONCLUSION</b>Moxibustion with salt in bamboo circle has an obvious therapeutic effect on periarthritis of shoulder, and it has transient analgesic effect and improves active function of shoulder joint, with a stable and long-term therapeutic effect.</p>

Hair removal with intense pulsed light (IPL) for hairy skin grafts / 中华整形外科杂志

<p><b>OBJECTIVE</b>To evaluate the hair-removal effect of IPL for hairy skin grafts.</p><p><b>METHODS</b>10 patients with hairy skin grafts were treated with IPL (ELITEplus) for hair removal 3 to 5 times at intervals of 2 months. The patients received IPL(610 - 1 000 nm) with spot size of 10 mm x 50 mm, pulse width of 5 msec with a delay of 2 - 20 msec, fluence of 30 - 38.3 J/cm2 .</p><p><b>RESULTS</b>The treatment was well tolerated with no need of anesthesia in all the patients. The hairs were removed completely after 3 to 5 treatments. The treated site could be washed as usual with no need of dressing. There was no blister, infection, hyperpigmentation and scarring. Only vellus were existed during the follow-up period of 6 - 12 months.</p><p><b>CONCLUSIONS</b>IPL is a safe and reliable method to remove unwanted hair on skin grafts. It can be easily performed with a lower complication.</p>

Hair removal with intense pulsed light / 中华整形外科杂志

<p><b>OBJECTIVE</b>To evaluate the hair-removal effect of intense pulsed light (IPL).</p><p><b>METHODS</b>The unwanted hairs were removed with ELITE plus IPL. The treatment took 3 - 5 procedures, with an interval of over 2 months. 341 patients underwent the treatment.</p><p><b>RESULTS</b>All the patients were well tolerant without anesthesia. The unwanted hairs were wholly removed after 3 - 5 procedures. After operation, routine cleaning and make-up were allowed and bandaging was not necessary. There were blister in 3 cases and infection in 1 case. No pigmentation and scarring happened. Following-up of 3 - 6 months showed steady results with less regeneration of very thin and soft hair.</p><p><b>CONCLUSIONS</b>IPL is an ideal hair-removal method because of the credible effect, simple operation, rapid treatment and no serious complications.</p>