Objective To examine the effects of formaldehyde on the process of sperm development and reproductive capacity in male mice and the micronucleus rate of liver cells from offspring.Methods The mice were randomly divided into negative control group(NC),formaldehyde exposed group and positive control group (PC).The exposed dose was 21 mg?m-3 (1/24 LC50),42 mg?m-3 (1/12 LC50) and 84 mg?m-3 (1/6 LC50),respectively. 12 male mice were included in each group.Male mice from different formaldehyde exposed groups were inhaled with formaldehyde for 2 h one day,6 d each week,lasted for 13 weeks.The aberration rate of sperm in male mice and the micronucleus rate of liver cells from offspring were observed,and the reproductive capacity of male mice was detected by dominant lethal test.Results The aberration rates of sperm in mice from different formaldehyde exposed groups were significantly higher than that in negative control (P

Objective Neurodegenerative diseases, such as ischemia, traumatic injury, Alzheimer's disease, and Parkinson's disease are characterized by neuronal loss and dysfunction. It is known that glutamate-induced toxicity plays an important role in neurodegenerative diseases. Glutamate toxicity seems to be mediated by excessive influx of Ca2+ into neuronal cells through activation of N-methyl-D-aspartate (NMDA) receptor. To search for potential NMDA receptor inhibitors in traditional Chinese medicine. Methods A series of computer methods including drug-likeness evaluation, ADMET tests as well as molecular docking have been used. Results 1,5-O-dicaffeoyl-quinic acid was identified as NMDA receptor inhibitor by virtual screening. Its neuroprotective activity was further confirmed by in vitro test. 1,5-O-dicaffeoyl-quinic acid showed strong neuroprotection against NMDA-induced cell injury. Conclusion 1,5-O-Dicaffeoylquinic acid may be regarded as a potential NMDA receptor inhibitor for the prevention and treatment of neurodegenerative disorders.

AIMTo investigate the in vitro recovery and influencing factors of ketoprofen in microdialysis probe, and study the pharmacokinetic of unbound ketoprofen in rat after iv administration.

METHODSThe recovery of ketoprofen was detected by a concentration difference method. After microdialysis probe was inserted into the jugular vein of male Wistar rats, the probe was infused with various concentrations perfusate. The in vivo recovery and the pharmacokinetics of unbound ketoprofen in rat were investigated. Dialysate samples were determined by HPLC.

RESULTSThe recovery detected by gain was as the same as that by loss; the recovery was independent of the drug concentration surrounding the probe. The in vitro recovery was 28.75% by concentration difference method and the in vivo recovery was (40.3 +/- 2.7) % by retrodialysis method. After i.v. administration of ketoprofen in rat, T 1/2, AUC and CL of unbound ketoprofen were (181 +/- 16) min, (112 +/- 27) microg x min x mL(-1) and (0.22 +/- 0.05) L x min(-1), respectively.

CONCLUSIONMicrodialysis sampling can be used for the pharmacokinetic study of unbound ketoprofen in rat.

Animals ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; pharmacokinetics ; Area Under Curve ; Chromatography, High Pressure Liquid ; Injections, Intravenous ; Ketoprofen ; administration & dosage ; pharmacokinetics ; Male ; Microdialysis ; methods ; Rats ; Rats, Wistar

OBJECTIVETo determine Ligustilide in volatile oil from Ligustrcum chuanxiong with RP-HPLC.

METHODODS2 column (4.6 mm x 200 mm, 5 microm) was used and nitrendipine was used as internal standard. The mobil phase consisted methanol, acetontrile and water (33:21:46). The ligustilide was at 275 nm.

RESULTThe linear range was 2.92-29.2 mg x L(-1) for ligustilide. The average recovery of ligustilide was 95.1% and RSD was 2.3%.

CONCLUSIONThis method is simple and can be used to determine ligustilide with satisfactory accuracy and reproducibility.

4-Butyrolactone ; analogs & derivatives ; analysis ; Chromatography, High Pressure Liquid ; methods ; Ligusticum ; chemistry ; Oils, Volatile ; chemistry ; isolation & purification ; Plants, Medicinal ; chemistry ; Rhizome ; chemistry

AIMTo prepare clarithromycin emulsion and investigate its pharmacokinetics in rats. And to do irritation test of the emulsion.

METHODSHigh pressure homogenization method was used to prepare clarithromycin emulsion, and the Nicomp380 machine was used to test the mean particle size and zeta-potential of clarithromycin emulsion. Irritation of emulsion was also evaluated compared with the positive control of clarithromycin solution using rat paw lick test and rabbit ear vein irritation test. Microbiological assay method was used for determining the drug concentration in plasma. Pharmacokinetics of two dosage forms in rats was also studied.

RESULTSThe mean particle size and zeta potential of clarithromycin emulsion were 156 nm and -31.8 mV, respectively. The emulsion was stable during the storage time at 4 degrees C for 6 month. The pain caused by emulsion reduced significantly compared with that of clarithromycin solution based on the results of rat paw lick test and rabbit ear vein test. The drug concentration-time curves of clarithromycin emulsion and clarithromycin solution were similar and could be described by two compartment model. AUC(0-1) of clarithromycin emulsion and clarithromycin solution were (66.76 +/- 16.34) and (59.00 +/- 11.20) microg x h x mL(-1), respectively.

CONCLUSIONStable emulsion could be prepared using high pressure homogenization method, and irritation caused by i.v. injection could be reduced significantly by using clarithromycin emulsion.

Animals ; Anti-Bacterial Agents ; administration & dosage ; adverse effects ; pharmacokinetics ; Area Under Curve ; Clarithromycin ; adverse effects ; blood ; pharmacokinetics ; Drug Compounding ; methods ; Emulsions ; Female ; Injections ; Male ; Pain ; chemically induced ; Pain Measurement ; methods ; Particle Size ; Rabbits ; Rats ; Rats, Wistar ; Solutions

AIMTo prepare solid lipid nanoparticles (SLN) loaded with all trans retinoic acid using an ultrasonic technique with Compritol 888 ATO as matrix material, and investigate properties of nanoparticles in vitro and in vivo.

METHODSUltrasonic technique was adopted to prepare solid lipid nanoparticles in an aqueous system using all-trans retinoic acid (ATRA) as a model drug. Physicochemical proterties of SLN were investigated in detail. Drug release from two sorts of ATRA-SLN was investigated using a dialysis bag method. Compared with ATRA solution, the in vivo pharmacokinetics of two sorts of ATRA-SLN after intravenous injection to rats were studied.

RESULTSSolid lipid nanoparticles loaded with all-trans retinoic acid was readily and quickly prepared by ultrasonic technique. The morphological investigation by Transmission Electron Microscopy (TEM) showed that the particles had round and uniform shapes. The mean diameters of them were (158 +/- 9) nm and (89 +/- 11) nm separately. The SLN dispersion was stable at 4 degrees C for more than one year. Drug loading was 3.3%, drug entrapment efficiency was more than 95%, the in vitro release was well in accordance with Weibull distribution. Compared with ATRA control solution, SLN could stay in the blood circulation for a longer time after intravenous injection.

CONCLUSIONThe ultrasonic technique was appropriate for the preparation of solid lipid nanoparticles.

Animals ; Drug Carriers ; Drug Delivery Systems ; Drug Stability ; Fatty Acids ; Male ; Nanostructures ; chemistry ; Particle Size ; Poloxamer ; chemistry ; Polysorbates ; Rats ; Rats, Wistar ; Tretinoin ; administration & dosage ; pharmacokinetics ; Ultrasonics

Objective To investigate the anti-mutation of Chinese medicinal herb Herba Leonuri and its effect on T lymphocyte proliferation in spleen.Methods The micronucleus test of mouse bone marrow cell(MNT) :thirty mice were divided into six groups(n= 5),negative control(NS),cyclophosphamide group(CP 3.0 mg?kg-1),Herba Leonuri antimutagenesis groups(Herba Leonuri with dosages of 1.0,2.0,4.0,8.0 g?kg-1+CP30 mg?kg-1).The improved method was used to detect the micronuclei frequency.Lymphocyte transformation test:twenty-four mice were divided into four groups(n=6),saline control,CP control(30 mg?kg-1),Herba Leonuri(2.0 g?kg-1),Herba Leonuri +CP(2.0 g?kg-1 Herba Leonuri +CP 30 mg?kg-1).MTT assay was used to calculate the stimulation index(SI).Results The micronuclei frequencies in Herba Leonur 2.0,4.0,8.0 g?kg-1 groups were lower than that in CP group(P

It is a difficult problem of forensic medicine to accurately estimate the post-mortem interval. Entomological approach has been regarded as an effective way to estimate the post-mortem interval. The developmental biology of carrion-breeding flies has an important position at the post-mortem interval estimation. Phorid flies are tiny and occur as the main or even the only insect evidence in relatively enclosed environments. This paper reviews the research progress of carrion-breeding phorid flies for estimating post-mortem interval in forensic medicine which includes their roles, species identification and age determination of immatures.
Animals ; Autopsy ; Diptera ; Entomology ; Environment ; Forensic Medicine ; Humans ; Postmortem Changes

We identified molecular mechanisms by which Isatidis Radix might prevent or mitigate influenza and corona virus disease 2019 (COVID-19) based on chemical composition and network pharmacology. High performance liquid chromatography coupled to tandem quadrupole time-of-flight mass spectrometry (HPLC-Q-TOF-MS) was used to analyze the components of Isatidis Radix. Seventy compounds were identified, of which 33 prototype compounds entered the blood. Network pharmacological analysis of 41 potential active components demonstrated that Isatidis Radix can regulate protein kinase B1 (AKT1), serum albumin (ALB), glyceraldehyde-3-phosphate dehydrogenase (GAPDH), vascular endothelial growth factor A (VEGFA), tyrosine-protein kinase SRC (SRC), epidermal growth factor receptor (EGFR), intercellular adhesion molecule-1 (ICAM1) and other key genes, which have preventive effects on influenza and COVID-19 through hypoxia inducible factor-1 (HIF-1), vascular endothelial growth factor (VEGF), tumor necrosis factor (TNF), influenza A, Toll-like receptor (TLR), phosphatidylinositol-3-kinase-protein kinase B (PI3K-AKT), COVID-19 and other signaling pathways. This study identifies mechanisms by which Isatidis Radix might act against influenza and COVID-19 that are related to the inflammatory response, immunomodulation and viral defense, and provides a basis for subsequent clinical research. All animal experiments were approved by the Ethics Committee of Shenyang Pharmaceutical University (SYPU-IACUC-S2020-12.23-201).

Adult ; Alanine Transaminase ; blood ; Antiviral Agents ; administration & dosage ; therapeutic use ; Child ; Child, Preschool ; DNA, Viral ; blood ; Female ; Follow-Up Studies ; Hepatitis B Surface Antigens ; blood ; Hepatitis B e Antigens ; blood ; Hepatitis B virus ; drug effects ; genetics ; Hepatitis B, Chronic ; blood ; drug therapy ; virology ; Humans ; Interferon-alpha ; administration & dosage ; therapeutic use ; Male ; Polyethylene Glycols ; administration & dosage ; therapeutic use ; Recombinant Proteins ; Time Factors ; Treatment Outcome