1.The potential effects of linalool on enantioselective skin permeation of norgestrel.
Yi RONG ; Wen-Ying YU ; Xia GUO ; Shan-Shan ZENG ; Zheng-Rong SHEN ; Su ZENG ; Jin-Cui YE
Acta Pharmaceutica Sinica 2014;49(8):1175-1180
The purpose of this study is to investigate the enantioselectivity of norgestrel (NG) transdermal permeation and the potential influence of linalool and lipids on the enantioselectivity. In vitro skin permeation studies of NG across the excised rat skins were performed with Valia-Chien diffusion cells, and the permeation samples were analyzed by enantioselective HPLC. The possible enantioselective permeation of NG across intact rat back skin and lipids extracted rat back skin and the influence of linalool were evaluated. The skin permeation rate of dl-NG was two times higher than that of l-NG when donor solutions (EtOH/H2O 2 : 8, v/v) containing l-NG or dl-NG. It may be mainly attributed to the solubility discrepancy between enantiomer and racemate. The enantioselective permeation of dl-NG across intact rat skin was observed when the donor solutions containing dl-linalool. The permeation flux of l-NG was 22% higher than that of d-NG. But interestingly, the enantioselective permeation of dl-NG disappeared under the same experimental condition except that the lipid extracted rat skin was used. Attenuated total reflection-fourier transform infrared spectroscopy analysis of stratum corneum showed that the wave number for asymmetric CH2 stretching vibrations of lipids treated with dl-linalool was greater than that of the control. The results indicated that the enantioselective permeation of NG may be contributed by the interaction between dl-linalool and lipids. More than half of lipids were composed of ceramides. The stereospecific interaction maybe existed among chiral enhancer (linalool), lipids (ceramides) and/or chiral drugs (NG).
Administration, Cutaneous
;
Animals
;
Lipids
;
pharmacology
;
Monoterpenes
;
pharmacology
;
Norgestrel
;
pharmacokinetics
;
Rats
;
Skin Absorption
;
drug effects
;
Spectroscopy, Fourier Transform Infrared
;
Stereoisomerism
2.Effect of selected fungi on the reduction of gossypol levels and nutritional value during solid substrate fermentation of cottonseed meal.
Wen-ju ZHANG ; Zi-rong XU ; Jian-yi SUN ; Xia YANG
Journal of Zhejiang University. Science. B 2006;7(9):690-695
The objective of this work was to investigate the effect of six individual strains of fungi on the reduction of gossypol levels and nutritional value during solid substrate fermentation of cottonseed meal (CSM). Six groups of disinfected CSM substrate were incubated for 48 h after inoculation with either of the fungi C. capsuligena ZD-1, C. tropicalis ZD-3, S. cerevisae ZD-5, A. terricola ZD-6, A. oryzae ZD-7, or A. niger ZD-8. One not inoculated group (substrate) was used as a control. Levels of initial and final free gossypol (FG), crude protein (CP), amino acids (AA) and in vitro digestibility were assayed. The experiment was done in triplicate. The experimental results indicated that microbial fermentation could greatly decrease (P<0.05) FG levels in CSM. The detoxification efficiency differed between the species of microorganisms applied. From the perspective of reducing CSM potential toxicity, C. tropicalis ZD-3 was most successful followed by S. cerevisae ZD-5 and A. niger ZD8. They could reduce FG levels of CSM to 29.8, 63.07 and 81.50 mg/kg based on DM (dry matter), respectively, and their detoxification rate were 94.57%, 88.51% and 85.16%, respectively. If crude protein, amino acids content and their in vitro digestibility were also taken into account, A. niger ZD-8 may be the best choice. The CP content of CSM substrate fermented by C. tropicalis ZD-3 and A. niger ZD-8 were improved by 10.76% and 22.24%; the TAA (total amino acids) contents were increased by 7.06% and 11.46%, and the EAA (essential amino acids) were raised by 7.77% and 12.64%, respectively. Especially, the levels of methionine, lysine and threonine were improved greatly (P<0.05). The in vitro CP digestibility of CSM fermented by C. tropicalis ZD-3 and A. niger ZD-8 was improved by 13.42% and 18.22%, the TAA were increased by 17.75% and 22.88%, and the EAA by 16.61% and 21.01%, respectively. In addition, the in vitro digestibility of methionine, lysine and threonine was also improved greatly (P<0.05).
Amino Acids
;
analysis
;
Cottonseed Oil
;
chemistry
;
metabolism
;
Digestion
;
Fermentation
;
Fungi
;
metabolism
;
Gossypol
;
analysis
;
Nutritive Value
;
Plant Proteins
;
analysis
3.Roles of adenosine receptors in Alzheimer's disease.
Rong YAN ; Zeng-Yao HU ; Wen-Xia ZHOU ; Qi WANG ; Yong-Xiang ZHANG
Acta Pharmaceutica Sinica 2014;49(6):751-756
As an important neurotransmitter, adenosine displays its functions by acting on the adenosine receptors. Recent studies have shown that the distribution, expression and balance among subtypes of adenosine receptors are closely related with cognitive activities, and changes of adenosine receptors play key roles in neurodegenerative disorders including Alzheimer's disease. It has been pointed out that prolonged activation of adenosine receptors by high level adenosine may lead to the disturbance of balance among adenosine receptor subtypes. This imbalance mainly performed as increased expression of A2a receptor and decreased expression of A1 receptor, and enhancement of the excitatory signals mediated by A2a receptor and weakened inhibitory signals mediated by A1 receptor. Changes of these two subtypes of adenosine receptors may lead to a lot of disorders of neurological activities which developed into dysfunction of cognition to the end. These findings imply that the potential of maintaining the balance among adenosine receptors on the treatment of AD would facilitate both the revealing of the mechanism and the cure of AD.
Adenosine
;
physiology
;
Alzheimer Disease
;
physiopathology
;
Humans
;
Neurotransmitter Agents
;
physiology
;
Receptors, Purinergic P1
;
classification
;
physiology
4.Primary MALT lymphoma of orbit:a clinicopathological study of 77 cases.
Ying-wen BI ; Rong-jia CHEN ; Ying-yong HOU ; Xia-ping LI
Chinese Journal of Pathology 2007;36(6):414-415
Adult
;
Aged
;
Aged, 80 and over
;
Conjunctival Neoplasms
;
diagnostic imaging
;
pathology
;
radiotherapy
;
surgery
;
Female
;
Follow-Up Studies
;
Humans
;
Lymphoma, B-Cell, Marginal Zone
;
diagnostic imaging
;
pathology
;
radiotherapy
;
surgery
;
Male
;
Middle Aged
;
Orbital Neoplasms
;
diagnostic imaging
;
pathology
;
radiotherapy
;
surgery
;
Prognosis
;
Retrospective Studies
;
Tomography, X-Ray Computed
5.An observation on clinical effectiveness of early rehabilitative training program in patients with acute myocardial infarction
Lei ZHOU ; Guo-Ming WEN ; Xia HUANG ; Wan-Hong HE ; Chun-Rong ZHANG ; Xiao-Lan GONG ;
Chinese Journal of General Practitioners 2005;0(08):-
Objective To investigate the effects of early rehabilitative training program on patients with acute myocardial infarction(AMI).Methods One hundred and twenty-two patients with AMI were randomly divided into early rehabilitation group(n=62)and control group(n=60).In addition to routine treatment,patients in rehabilitation group received early rehabilitative training mainly by walking exercise for two weeks.Results There were no significant differences in ventricular arrhythmia(Lown≥Ⅲ), extension of infarction and heart rate variability(HRV)between the two groups(P>0.05).Forty of 62 patients(64.5%)in rehabilitation group had their left ventricular ejection fraction(LVEF)more than or equal to 50% in the 3~(rd)~4~(th)week after admission,significantly higher than that in control group(45.0%, 27/60 ;P<0.01 ).By the end of the 4~(th)week after admission,25.8% of the patients in rehabilitation group showed positive in treadmill test,significantly lower than that in control group(38.3%,P<0.01). Occurrence of angina pectoris and reinfarction and fatality in rehabilitation group were significantly lower than those in control group(P<0.05)during their hospitalization and follow-up period.Patients in rehabilitation group stayed at hospital for(16?3)days in average,significantly less than that in control group[(27?4) days],with statistically significant difference(P<0.05).Conclusion Early rehabilitative training for patients with uncomplicated AMI is not only safe and feasible,but also useful in improvement for their prognosis and quality of life.
6.Correlation between monocyte to high-density lipoprotein cholesterol ratio and insulin resistance in male patients with type 2 diabetes mellitus combined with metabolic-related fatty liver disease
QIAN Fang-fang ; LI Hao-xiang ; SHEN Yi-rong ; YU Xia-wen ; XIA Yue ; WANG Dong ; YANG Ling ; JIA Yu
China Tropical Medicine 2023;23(4):333-
Abstract: Objective To explore the correlation between monocyte to high-density lipoprotein cholesterol ratio (MHR) and insulin resistance (IR) in male patients with type 2 diabetes mellitus (T2DM) combined with metabolic-related fatty liver disease (MAFLD). Methods A total of 454 male patients with T2DM combined with MAFLD in National Metabolic Management Center (MMC) of the Affiliated Hospital of Jiangsu University from May 2018 to July 2020 were enrolled. The general clinical data of subjects were collected, blood routine and biochemical indexes were tested, homeostasis model insulin resistance index (HOMA-IR) was calculated, visceral fat area (VFA) and subcutaneous fat area (SFA) were measured. Accordingtothe MHR quartile, patients were divided into group Q1 (MHR≤0.38), group Q2 (0.38
7.Foot hyalohyphomycosis caused by Fusarium subglutinans:a case report
Qiu-Xia CHEN ; Wen-Ming HUANG ; Jian-Qiang SHI ; Wen LI ; Shun-Fan LI ; Rong-Xi LU ; Feng-Yan BAI
Chinese Journal of Dermatology 2003;0(08):-
Objective To report a case of foot hyalohyphomycosis due to Fusarium subglutinans. Methods Medical history was collected and physical examination performed for this patient.Biopsy samples were obtained from the inner side of right ankle of this patient and subjected to pathological examination. Discharge was collected from the lesions for direct microscopic examination and culture.Results A 72-year-old woman presented with an ulcer on the right foot for 3 years.Physical examination disclosed an ulcer,measuring 3 cm x 1.5 cm,with a moist surface and obvious tenderness,at the inner side of the right ankle.Proliferation of dusky-red granulomatous tissue was observed at the base of the ulcer.Pathological examination revealed necrotic granulomatous tissue and slender,septate and hyaline hypha-like structure in the superficial dermis with scattered infiltration of inflammatory cells.PAS staining showed sausage-like hypha and scattered orbicular-ovate spores.Microscopic examination of lesional discharge exhibited septate, branching and hyaline hypha.The isolated fungus was identified as Fusarium subglutinans by culture,and appeared to be highly sensitive to terbinafine,nystatin and amphotericin B.The lesion completely healed after 2 months of treatment with oral terbinafine (0.25 g,twice a day).Conclusions This is a case of foot hyalohyphomycosis due to Fusarium subglutinans,and terbinafine is effective for this condition.
8.Application of percutaneous needle aspiration biopsy by the simulator guided to the diagnosis for pulmonary focus in coal miners' pneumoconiosis.
Si-hai LIU ; Cheng-dong QI ; Wen-shou XU ; Rui-xia ZHU ; Qin YAN ; Wen FENG ; Rong-xia SUN ; Yan-fang ZHANG ; Xiao-fu WU ; Zheng-chuan FU
Chinese Journal of Industrial Hygiene and Occupational Diseases 2004;22(1):72-73
Aged
;
Biopsy, Needle
;
methods
;
Coal Mining
;
Humans
;
Lung
;
pathology
;
Lung Neoplasms
;
complications
;
diagnosis
;
Middle Aged
;
Pneumoconiosis
;
complications
9.Synthesis and structure-activity relationship of cycloberberine as anti-cancer agent.
Chong-Wen BI ; Cai-Xia ZHANG ; Yang-Biao LI ; Wu-Li ZHAO ; Rong-Guang SHAO ; Lin MEI ; Dan-Qing SONG
Acta Pharmaceutica Sinica 2013;48(12):1800-1806
A series of cycloberberine derivatives were designed, synthesized and evaluated for their anti-cancer activities in vitro. Among these analogs, compounds 6c, 6e and 6g showed strong inhibition on human HepG2 cells. They afforded a potent effect against DOX-resistant MCF-7 breast cells as well. The primary mechanism showed that cell cycle was blocked at G2/M phase of HepG2 cells treated with 6g using flow cytometry assay. It significantly inhibited the activity of DNA Top I at the concentration of 0.1 mg mL-1. Our results provided a basis for the development of this kind of compounds as novel anti-cancer agents.
Antineoplastic Agents
;
chemical synthesis
;
chemistry
;
pharmacology
;
Berberine
;
analogs & derivatives
;
chemical synthesis
;
chemistry
;
pharmacology
;
Cell Cycle
;
drug effects
;
Cell Proliferation
;
drug effects
;
DNA Topoisomerases, Type I
;
metabolism
;
Doxorubicin
;
pharmacology
;
Drug Resistance, Neoplasm
;
Hep G2 Cells
;
Humans
;
MCF-7 Cells
;
Molecular Structure
;
Structure-Activity Relationship