A series of isoindoline derivatives were designed, synthesized, and evaluated for their double inhibitory activities. All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS. Preliminary in vitro pharmacological tests showed that all compounds exhibited 5-HT or NE reuptake inhibition activity. Among the tested compounds, compound I-3 exhibited potent inhibitory activity against 5-HT and NE reuptake in vitro, and exhibited potent antidepressant activity in vivo. These compounds designed can be further optimized for finding more potent 5-HT/NE dual reuptake inhibitors and antidepressant candidates as well.
Antidepressive Agents ; chemical synthesis ; chemistry ; Biological Transport ; Drug Design ; Isoindoles ; chemical synthesis ; chemistry ; Serotonin Uptake Inhibitors ; chemical synthesis ; chemistry ; Structure-Activity Relationship

One new dicyclopeptide cyclo-(L-N-methyl Glu-L-N-methyl Glu) (1), together with one new natural dicyclopeptide cyclo-(L-methyl Glu ester-L-methyl Glu ester) (2), and two known dicyclopeptides cyclo-(L-methyl Glu ester-L-Glu) (3), and cyclo-(L-Glu-L-Glu) (4), were isolated from the aerial parts of Dianthus chinensis L. Their structures were determined by spectroscopic analyses and chemical methods.
Dianthus ; chemistry ; Magnetic Resonance Spectroscopy ; Molecular Structure ; Plant Components, Aerial ; chemistry ; Plants, Medicinal ; chemistry

Nine compounds were isolated from the n-butanol fraction of 95% ethanol extract of the fruit of Alpinia oxyphylla Miq. with a combination of various chromatographic approaches, including MDS resin, silica gel, reverse phase C18 and preparative HPLC. On the basis of spectroscopic data analysis, they were elucidated as (1R, 4R, 10R)-1β, 4α-dihydroxy-11, 12, 13-trinor-5, 6-eudesmen-7-one (1), 1β, 4β-dihydroxy-11, 12, 13-trinor-8, 9-eudesmen-7-one (2), oxyphyllenone A (3), oxyphyllenone B (4), rhamnocitrin (5), staphylionoside D (6), benzyl-1-O-β-D-glucopyranoside (7), 2-O-β-D-glucopyranosyl-(1S)-phenylethylene glycol (8), and (S)-1-phenylethyl-β-D-glucopyranoside (9). Among them, compound 1 is a new sesquiterpene, named as oxyphyllenone C; compounds 8 and 9 are new natural products; compounds 2 and 6 were isolated from the genus Alpinia for the first time, and compound 7 was isolated from A. oxyphylla for the first time.
1-Butanol ; Alpinia ; chemistry ; Chromatography, High Pressure Liquid ; Fruit ; chemistry ; Phytochemicals ; chemistry ; isolation & purification ; Sesquiterpenes ; chemistry ; isolation & purification

Tumorous cells are characterized by distinctive metabolic reprogramming and living conditions. Understanding drug metabolizing features in tumor cells will not only favor the estimation of metabolic rate, elimination half life and the assessment of potency, but also facilitate the optimal design of anti-tumor drugs/prodrugs. This article reviewed the expression and activity features of major drug metabolizing enzymes (DMEs) in solid tumorous tissues, such as liver, intestine, breast and lung, and the difference from the correspondingly normal tissues, exemplified by the metabolic properties of some classic antitumor-agents in tumorous tissues. In combination with the data retrieved in vitro tumor cell lines, we discussed the similarities and differences of DMEs expression and function between tumor tissues (in vivo) and tumor cells (in vitro), and proposed the possible factors that cause the differences.
Antineoplastic Agents ; pharmacokinetics ; Cell Line, Tumor ; Humans ; Inactivation, Metabolic ; Liver ; metabolism ; Neoplasms ; enzymology ; Prodrugs ; pharmacokinetics

Fourteen compounds were isolated by column chromatography from the ethyl acetate extract of the seeds of Brassica campestris. Their structures were elucidated by physicochemical properties and spectroscopic data analysis. The isolated compounds were respectively identified as (5Z,7E)-4, 4-dimethyl-5-acetyl-5, 7-nonadienoic acid (1), indole-3-carboxaldehyde (2), blumenol A (3), vinylsyringol (4), sinapinic acid (5), sinapic acid ethyl ester (6), protocatechuic acid (7), crinosterol (8), campesterol (9), 7-oxo-stigmasterol (10), kaempferol (11), 2,5-dihydroxybenzoic acid (12), syringic acid (13) and daucosterol (14). Compound 1 was a new compound and the other compounds were isolated from this plant for the first time except for compounds 4, 5 and 13.
Brassica ; chemistry ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Molecular Structure ; Seeds ; chemistry ; Spectrometry, Mass, Electrospray Ionization

Eyelid Diseases ; diagnosis ; immunology ; pathology ; Facial Dermatoses ; diagnosis ; immunology ; pathology ; HIV Infections ; complications ; immunology ; Humans ; Immunocompromised Host ; Male ; Middle Aged ; Molluscum Contagiosum ; complications ; diagnosis ; immunology ; pathology

The effect of acupuncture cooperated with low-frequency repetitive transcranial magnetic stimulation (rTMS) on chronic insomnia was explored.Seventy-eight patients with chronic insomnia were randomly allocated into two groups:treatment group and control group.In the treatment group,the patients received acupuncture combined with rTMS treatment,and those in the control group were given acupuncture cooperated with sham rTMS treatment,3 days per week for 4 weeks.Before and after treatment,the primary outcomes including the scores on Insomnia Severity Index (ISI) and Pittsburgh Sleep Quality Index (PSQI) and the secondary outcomes including total sleep time (TST),sleep onset latency (SOL),wake after sleep onset (WASO),sleep efficiency (SE％) recorded by sleeping diary and actigraphy were observed in both groups.Seventy-five participants finished the study (38 in treatment group and 37 in control group respectively).After treatment,the scores in the two groups were improved significantly,more significantly in the treatment group than in the control group.It can be inferred that acupuncture cooperated with rTMS can effectively improve sleep quality,enhance the quality of life of patients and has less side effects.

Objective To summarize our experience in prevention and treatment of stricture after esopageal burns in the past thirty years.Methods There were 168 cases in this series.Of them,158 cases underwent surgical management in this study.Modified intraluminal stenting was used in 34 cases, colon interposition without resection of strictured esophagus in 77 cases,gastric transposion with resection of the stricture in 27,repair of cervical stricture with platysma myocutaneous flap in 22,and miscellane- ous operation in 12.Eleven cases experienced operation twice or more at our department.Results Twenty-nine cases recovered after treatment with intraluminal stenting,and 5 re-experienced stricture after stent removal.One of the 5 cases with failed stent responded to bougienage,and the remaining 4 cases re- quired esophageal reconstruction later.Of the 77 colon interpositions,5 cases died postoperatively,and complications of cervical anastomotic fistula occurred in 14 cases,anastomotic stenosis in 4,and abdomi- nal incision dehiscence in 2 cases.In the 27 cases with gastric transpositions,postoperative complications of anastomotic stricture occurred in 2 cases and empyema in 1 patient.There was a cervical leak in 3 ca- ses of the 22 cases treated with the repair of cervical esopageal or anastomotic stricture with a platysma myocutaneous flap.In the 12 cases treated with miscellaneous operation,one died of intestinal obstruc- tion.All the survivors had regular diet after discharge.Conclusions Intraluminal stenting can prevent the formation of caustic esophageal stricture.The location of the cicatricial esophagus dictates whether to perform concomitant esophagectomy during esophageal reconstruction.Platysma myocutaneous flap repair is an excellent method for the treatment of severe cervical esophageal or anastomotic stricture.

To construct a secretory-expression vector of antimicrobial peptide Bactenecin 7(Bac7),and identify the secretory-expression product in L.lactis MG1363 and its bioactivity.The splicing primers of regulation elements and Bac7 gene,which designed according to codon usage preferences of L.lactis MG1363,were chemically synthesized,and the overlap-extension PCR method was used to splice the full length of Bac7 gene.Then the Bac7 gene was linked to expression vector pMG36e to construct pMG36e/Bac7 vector,and pMG36e/Bac7 was transformed into L.lactis MG1363 by electrophoration.RT-PCR and Western blot assays were applied to investigate the expression of the Bac7 gene in L.lactis,and bioactivity of Bac7 in culture supernatant of L.lactis was tested with plate-diffusion method.The results showed that the Bac7 gene and its regulation elements was amplified and cloned in the vector pMG36e successfully,The secretory-expressed Bac7 in L.lactis MG1363 harboring pMG36e/Bac7 was identified by Western blot,and it had high bacteriostatic activity against E.coli.These results indicate that the recombinant L.lactis MG1363 could express bioactive Bac7,which lays a foundation for further study of oral administration of a Bac7-secreting L.lactis to treat intestinal bacteria infection.

Objective To study the dry extract rate, determination and transfer rate of maker compounds, and fingerprint of standard decoction of ginger juice Magnoliae Officinalis Cortex (GJMOC) and provide a reference for the preparation and quality assessment of its dispensing granules by establishing 16 batches of standard decoction of GJMOC. Methods A total of 16 batches of GJMOC standard decoctions were prepared following literature requirements. The quantitative analysis method of magnolol and honokiol was according to Chinese Pharmacopoeia (2015 edition). The transfer rate of total magnolol and honokiol and extraction rate were calculated. the pH value was determined and HPLC fingerprint was established under a flow rate of 1 mL/min and eluted with a mobile phase of acetonitrile (A)-0.1% phosphoric acid solution (B) in a gradient mode (0-15 min, 12%-16% A; 15-30 min, 16%-28% A; 30-42 min, 28%-74% A; 42-55 min, 74%-80% A). The column temperature was set at 40℃ and the detection wavelength was 294 nm. Results By measuring the of 16 batches of standard decoction, the transfer rate of the sum of magnolol and honokiol ranged from 6.5% to 12.0%, the extraction rate was at a range of 3.41% to 7.14% and pH value was 4.63 to 5.43. The Similarity Evaluation System for Chromatographic Fingerprint of Traditional Chinese Medicine (2012A) was used to analyze and compare the fingerprints, and seven common peaks were determined and four were identified including magnoloside B (peak 1), magnoloside A (peak 2), honokiol (peak 6), and magnolol (peak 7). The similarity among 16 batches of standard decoction of GJMOC was evaluated, and the similarity was all greater than 0.69. Moreover, this study established an HPLC fingerprint analysis method of GJMOC standard decoction. Conclusion The preparation method established in this study is stable and feasible, and the analysis method shows good precision, stability, and repeatability in fingerprint analysis and it is suitable for evaluating the quality of standard decoction of GJMOC.