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

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

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

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

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.

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 (0.380.64) to compare the differences in measured indicators above. In addition, patients were divided into two groups according to HOMA-IR, HOMA-IR<2.5 and HOMA-IR≥2.5, and the differences in MHR were compared. Results The patients were divided into four groups according to MHR:group Q1 (n=115), group Q2 (n=110), group Q3 (n=120) and group Q4 (n=109). Fasting insulin (FINS) were respectively 6.17(4.20,9.76), 7.73(4.94,10.66), 8.92(5.32,11.33) and 9.13(5.25,12.27) mU/L, 2-hour postprandial insulin were 22.75(12.87,39.59), 27.55(16.44,39.77), 30.98(17.46,43.11) and 31.28(18.54,45.92) U/L. HOMA-IR were 3.12(1.63,4.25), 3.72(2.26,4.66), 3.87(2.48,5.44) and 3.95(2.42,5.31). Neutrophil (Neu) were 3.10(2.60,3.70), 3.20(2.50,3.93), 3.60(2.80,4.28), 4.20(3.30,5.00)×109/L. Subcutaneous fat area (SFA) were (181.27±53.60), (192.64±62.41), (199.53±61.40) and (203.69±71.51) cm2. They all increased gradually. However, the levels of high-density lipoprotein cholesterol (HDL-c) [1.18(1.06,1.35), 1.02(0.86,1.17), 0.96(0.80,1.03) and 0.80(0.69,0.92) mmol/L] and low-density lipoprotein cholesterol (LDL-c) [(3.00±0.79), (2.76±0.83), (2.67±0.85) and (2.59±0.92) mmol/L] decreased gradually. Pearson's or Spearman's correlation analysis showed that MHR was positively correlated with FINS, 2-hour postprandial insulin (2hINS), HOMA-IR, VFA and SFA (r=0.190, 0.153, 0.184, 0.114, 0.127, P<0.05). The coronary heart disease history, systolic blood pressure,diastolic blood pressure,fasting plasmaglucose (FPG), FINS, alanine aminotransferase (ALT), aspartate aminotransferase (AST), blood uric acid (Ur), body mass index (BMI), VFA, SFA and MHR of patients in group HOMA-IR≥2.5 were higher than group HOMA-IR<2.5 (P<0.05). Conclusion　MHR is positively correlated with IR in male patients with T2DM combined with MAFLD, and as MHR increases, the degree of IR is higher.

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.

Aged ; Biopsy, Needle ; methods ; Coal Mining ; Humans ; Lung ; pathology ; Lung Neoplasms ; complications ; diagnosis ; Middle Aged ; Pneumoconiosis ; complications

OBJECTIVETo investigate the nephrotoxic effects of methyl cantharidimide tablets on urinary protein and enzymes in Beagle dogs.

METHODBeagle dogs were randomly divided into negative control group(blank tablet), methyl cantharidimide tablets group (6.11,12.21, 24.42 mg x kg(-1)), continuously 30 days of oral adminiStration, once a day. The drug and control group were collected and determined fresh urine in 1, 2, 3 and 4 weeks of the administration; Serum urea nitrogen (BUN), creatinine (Crea), total protein (TP) and albumin (ALB) as well as sodium, potassium, chloride electrolyte were determined on 15 and 30 days of the administration; Urine albumin (mAlb), kidney injury molecule-1 (KIM-1), neutrophil gelatinase-associated lipocalin( NGAL), N-acetyl-beta-D-glucosaminidase (NAG), clusterin, beta2-microglobulin (beta2-MG), alpha1-microglobulin (alpha1-MG), alanine aminopeptidase( AAP) and im- munoglobulins IgG were tested on 15 and 30 days of the administration.

RESULTCompared with the control group, urine protein and white blood cells was significantly increased in each dose group. On 15 days of the administration, mAlb were higher in each dose group, KIM-1, NGAL, clusterin, NAG and AAP were significantly higher in high-dose group, while the middle and low dose group had no significant difference, as well as blood SCr and BUN no obvious abnormalities. On 30 days, mAlb, KIM-1, clusterin, NAG, AAP were increased in each dose group, appearing dose-effect relationship, beta2-MG and NGAL levels were significantly increased in high-dose group. Contents above indicators were increased with significant dose and time relationship, and serum BUN, Scr were correlated, suggesting that urine mAlb, KIM-1, clusterin, NAG and AAP indicators that can sensitively respond the changes of proteins and enzymes in urine.

CONCLUSIONMethyl cantharidimide tablets has a renal toxicity, urine mAlb, KIM-1, clusterin, NAG and AAP can be used as the early nephrotoxic biomarkers of methyl cantharidimide tablets.

Animals ; Biomarkers ; urine ; Dogs ; Female ; Kidney ; drug effects ; Kidney Diseases ; chemically induced ; Male ; Proteins ; metabolism ; Tablets ; adverse effects ; Urine ; chemistry

OBJECTIVETo investigate the material base and underlying mechanism of the effect of cluster needling of scalp acupuncture on the neuronal plasticity in rats with focal cerebral infarction.

METHODSThe model rats with acute cerebral infarction were made by blocking the middle cerebral artery with monofilament. One hundred and thirty two Wistar rats were randomly divided into 4 groups: sham-operation group (A), model group (B), point-to-point scalp acupuncture group (C) and cluster-needling of scalp acupunture group (D). Puncturing from "Baihui (GV 20)" to "Qubin (GB 7)" was used in group C. Cluster needling of scalp acupuncture was used in group D, in which needles were inserted forward and slantingly into "Baihui (GV 20)" and its left and right sides at 4 mm. In both groups, the treatment was carried out with rapid twirling reinforcing-reducing for 1 min then retaining needle for 30 min, once a day, 6 days in one course, for treating 4 courses. There was no treatment for group A and B. The change of neurological function was evaluated with Bederson score, while the expression of microtubule-associated protein 2 (MAP-2) in the ischemic penumbra was examined with immunohistochemistry (streptavidin-peroxidase method).

RESULTSIn comparison,with group B, the score of neurological function in group D decreased on 7th day (P<0.05), while the scors in group C and D also decreased on 14th and 28th days (both P<0.05). As compared with group C, the score of neurological function in group D obviously decreased on 28th days (P<0. 05). Comparing with group B, the expression of MAP-2 on the ischemic cortex was significantly increased in group D and C on 7th, 14th and 28th days (all P<0. 05), however, this expression in group D was higher than that in group C on 14th and 28th days (P<0. 05).

CONCLUSIONCluster needling of scalp acupuncture can improve the neurological function of rats with focal cerebral infarction, and increase the expression of MAP-2 in the ischemic penumbra.

Acupuncture Therapy ; methods ; Animals ; Cerebral Infarction ; ethnology ; metabolism ; physiopathology ; therapy ; Disease Models, Animal ; Male ; Microtubule-Associated Proteins ; metabolism ; Random Allocation ; Rats ; Rats, Wistar ; Scalp