Objective: To study the effects of betaxolol hydrochloride (BH) cationic liposomes on intraocular pressure (IOP), blood pressure ( BP) and heart rate ( HR) in rabbits to lay foundation for the development of new BH eye preparations. Methods:N-trimethyl chitosan (TMC60) was used as the coating material, the BH-loaded cationic liposomes (TMC60-BHL) were prepared. Total-ly 24 healthy rabbits were randomly divided into 4 groups using number method. Unilateral carotid artery intubation was carried out in the rabbits and connected a physiological recorder. TMC60-BHL, uncoated BHL, the marketed BH eye drops ( the positive control) and sterilized distilled water ( the negative control) with the volume of 50 μl was respectively used in one eye of the rabbits. IOP was detected by an ophthalmotonometer, and BP and HR were determined by the physiological recorder at the predetermined time intervals. Results:In the ipsilateral eyes, the maximum decrease in IOP for uncoated BHL and TMC60-BHL was 23. 00% and 26. 65%, respec-tively. In the contralateral eyes, the maximum decrease in IOP for uncoated BHL and TMC60-BHL was 18. 54% and 24. 33%, respec-tively. Compared with that of the positive control (19. 01%,15. 19%), the IOP decrease effect of uncoated BHL and TMC60-BHL was significant higher(P<0. 05), and that of TMC60-BHL was the highest(P<0. 05). BP and HR were both reduced in the various BH groups, while there was no notable difference when compared with those in the negative group(P>0. 05). Conclusion:TMC60-BHL shows significant IOP decrease effect without notable effect on BP and HR, which is valuable to be studied further.

Objective To study CT features of cerebral paragonimiasis and the values of CT examination.Methods 14 patients with cerebral paragonimisis underwent CT scanning including plain and contrast-enhanced CT scans.The CT findings were analyzed.Results The lesions of most cases were multiple on CT finding and manifested as nodular,hemorrhage and cystoid change and so on.The calcification may be appeared in cyst.Most of lesions were mixed change.There were no enhancement or spotted or ringshape enhancement .Conclusion CT variable findings of above multiple lesions in childhood brain may suggest as paragonimiasis,CT findings are corresponding to pathological change of cerebral paragonimiasis.

Animals ; Electromagnetic Fields ; adverse effects ; Female ; Gravidity ; radiation effects ; Humans ; Maternal Exposure ; adverse effects ; Pregnancy

Objective To observe the effects of Compound Uncaria Hypotensive Tablets on expressions of MCP-1 and MMP-9 of vascular remodeling in spontaneously hypertensive rats (SHR); To discuss it possible mechanism of action. Methods Totally 24 12-week old male SHR were randomly divided into SHR model group, Compound Uncaria Hypotensive Tablets group, and positive medicine group, with 8 rats in each group. Another 8 WKY rats were set as normal control group. Medication groups were given relevant medicine for gavage for successive 6 weeks. Noninvasive tail cuff method was used to observe blood pressure; morphological changes in thoracic aorta and renal artery were observed by HE staining; immunohistochemistry was used to detect the protein expressions of MCP-1 and MMP-9 in thoracic aortic wall. Results Protein expressions of MCP-1 and MMP-9 in thoracic aortic wall of SHR model group were significantly higher than those of normal control group (P<0.01); Compared with the SHR model group, protein expressions of MCP-1 and MMP-9 in thoracic aortic wall decreased significantly in the medication groups (P<0.05, P<0.01); Compared the Compound Uncaria Hypotensive Tablets group and positive medicine group, there was no obvious difference in protein expressions of MCP-1 and MMP-9 in thoracic aortic wall. Conclusion Compound Uncaria Hypotensive Tablets can reduce the blood pressure of SHR, reduce inflammation reaction, and regulate vascular remodeling, which mechanism may be related to down-regulation of expressions of MCP-1 and MMP-9 in SHR aortic endothelial cells.

A new benzene derivative microintegerrin C (1) and a new norsesquiterpenoid microintegerrin D (2), along with six known compounds (3-8), were isolated and identified from stems and leaves of Micromelum integerrimum by various chromatographies such as silica gel, Sephadex LH-20, RP-18 column chromatography and HPLC. Their structures were mainly identified based on the spectral data analysis such as 1D-, 2D-NMR and HR-EI-MS. All known compounds were isolated from this plant for the first time.
Chromatography, High Pressure Liquid ; Plant Leaves ; chemistry ; Plant Stems ; chemistry ; Rutaceae ; chemistry ; Sesquiterpenes ; isolation & purification

SCHWABE Company in German is the first and largest manufacturer of Ginkgo biloba preparation. The company not only has leading technology in this field, but also protects its own market effectively through the high quality of patent drafting and exactly patent layout. Based on multi-angle analysis for patent portfolio of G. biloba preparation at application time, legal status, globally layout, Chinese layout, the article provides technical reference of research and development of G. biloba, also provides valuable experience of traditonal Chinese medicine patent portfolio layout for Chinese enterprises.
Drug Industry ; economics ; legislation & jurisprudence ; trends ; Ginkgo biloba ; chemistry ; Humans ; Patents as Topic ; legislation & jurisprudence ; Phytotherapy ; economics ; trends ; Plant Preparations ; isolation & purification ; Technology, Pharmaceutical ; economics ; trends

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

Objective Light acts as an important zeitgeber and regulates the body's circadian rhythm.Excessive lighting at night leads to light pollution,which interferes with the circadian rhythm and thus adversely affects the body.To observe the adverse effect of continuous light on female reproductive endocrinology and explore effective treatment,the animal experiment was carried out.Methods 185 sexual maturity female SD rats in the age of 2 months with normal estrous cycle were enrolled.60 rats were selected randomly and enrolled into control group.Normal illumination conditions were given.The remaining rats were given 300±20lux light intensity for 24h/d last for 50 days to get reproductive rhythm disorder model.The model rats (100) were randomly divided into models group (n =50) and Traditional Chinese Medicine (TCM) group (n =50).Traditional Chinese Medicine group was treated with sequential TCM.At last we get 50 rats enrolled into model group and herbal group respectively.The TCM group rats were given therapy of nourishing yin and tonifying yang sequential TCM,while the two other groups were gavaged the same volume of physiological saline.The estrous cycle was observed in all groups.20 days later,blood were collected dynamically and E2 (estradiol),P (progesterone),LH (Luteinizing Hormone),FSH (Follicle-Stimulating Hormone)and melatonin were compared to evaluate the therapeutic effect of TCM.Finally,try to explain the mechanism of TCM's effect from the perspective of melatonin.Results At the first day,E2 was lower in TCM group and models group than control group (P＜ 0.05).At the second day,E2 was higher in traditional Chinese Medicine group than control group (9＜0.05).At the third day,E2 was higher in TCM group and models group than that in control group (P＜ 0.05).Progesterone in control group showed low level in pre-estrous and estrous period and elevated in the late stage of estrous.Progesterone showed no obvious change during the estrous cycle in TCM group and models group.At the third and fourth day,Progesterone was significantly lower in models group than TCM group and control group.At the first day,LH in models group [(249.8±50.2)mIU/mL] and TCM group [(83.4±37.3)mIU/mL] were significantly lower than control group [(430.0± 100.4)mIU/mL] (P＜0.05).At the first day,FSH in models group and TCM group were significantly lower than control group (P＜0.05).At the fourth day,FSH in TCM group was significantly lower than control group and models group (P＜0.05).Compared the melatonin among three groups,the circadian rhythm was high at night but low in the day in control group.The highest level was nearly 5 times higher than the lowest level.Neither the models group nor the TCM group had obvious recent rhythm changes.Conclusion Continuous light can induce disordered estrous cycle and loss of rhythm.Traditional Chinese Medicine can somehow induce circulation reconstruction.Continuous light can induce disordered endocrine,E2,FSH,LH surge abnormal,ovulation failure,luteal phase defect.TCM can induce ovulation and luteal support.Continuous light can destroy melatonin circadian rhythm and TCM can increase melatonin,which could be the mechanism of TCM's effect.

To establish a LC-MS/MS method for quantification of chlorogenic acid, caffeic acid, 3,4-DCQA, ferulic acid and cinnamic acid in rats plasma and study its pharmacokinetics after administration of Mailuoning injection at a single dose to rats. Plasma samples were acidified with hydrochloric acid and extracted with ethyl acetate. The analytes were determined by LC-MS-MS using a ZOBAX SB C18 column with a mobile phase of methanol-water (containing 2 mmol x L(-1) ammonium acetic) (60:40)at a flow rate of 0.5 mL x min(-1) and detected using ESI with negative ionization mode. Ions monitored in the multiple reaction monitoring (MRM) mode were m/z 353.1/191.0 [M-H]- for chlorogenic acid, m/z 178.9/134.9 [M-H]- for caffeic acid, m/z 515.2/353.0 [M-H]-for 3,4-DCQA, m/z 193.0/133.9 [M-H]-for ferulic acid, m/z 146.9/102.9 [M-H]- for cinnamic acid and m/z 246.0/125.8 [M-H]- for tinidazole (IS). After administration of Mailuoning injection at a single dose to eight Sprague-Dawley rats, the concentrations of chlorogenic acid, caffeic acid, 3,4-DCQA, ferulic acid and cinnamic acid in plasma were determined by LC-MS/MS method. The main pharmacokinetics parameters of measured data were caluculated by using DASver 1.0 software. The linear concentration ranges of the calibration curves for chlorogenic acid, caffeic acid, 3,4-DCQA and cinnamic acid were 2.006-1,027 microg x L(-1) (r = 0.999 6), 1.953-1,000 microg x L(-1) (r = 0.999 7), 28.51-1.459 x 10(4) microg x L(-1) (r = 0.998 9), 1.836-940.0, g x L(-1) (r = 0.997 7) and 4.780-2,447 microg x L(-1) (r = 0.998 6) respectively. The inner and inter-days relative standard deviations were both less than 5.0%, indicating legitimate precise and accuracy to the requirement of biological sample analysis. For chlorogenic acid, the pharmacokinetic parameter t1/2, AUC0-t, and CL were (49.78 +/- 12.81) min, (123.55 +/- 14.82) mg x min x L(-1) and (0.004 3 +/- 0.000 5) L x min(-1), respectively. For caffeic acid, the pharmacokinetic parameter t1/2, AUC0-t, and CL were (36.65 +/- 10.59) min, (91.67 +/- 11.77) mg x min L(-1) and (0.005 7 +/- 0.000 7) L x min(-1), respectively. For 3,4-DCQA, the pharmacokinetic parameter t1/2, AUC0-t, and CL were (50.08 +/- 13.78) min, (278.34 +/- 31.82) mg x min x L-1 and (0.001 6 +/- 0.000 2) L x min(-1), respectively. For ferulic acid, the pharmacokinetic parameter t1/2, AUC0-t, and CL were (51.39 +/- 15.52) min, (34.72 +/- 4.67) mg x min x L(-1) and (0.000 4 +/- 0.0001) L x min(-1), respectively. For cinnamic acid, the pharmacokinetic parameter t1/2, AUCo-t, and CL were (74.42 +/- 18.32) min, (34.63 +/- 4.82) mg x min x L(-1) and (0.007 7 +/- 0.001 1) L x min-', respectively. The assay method is proved to be sensitive, accurate and convenient. It can be applied to the pharmacokinetic study of chlorogenic acid, caffeic acid, 3,4-DCQA, ferulic acid and cinnamic acid.
Animals ; Chromatography, Liquid ; methods ; Drugs, Chinese Herbal ; administration & dosage ; pharmacokinetics ; Female ; Hydroxybenzoates ; blood ; pharmacokinetics ; Male ; Rats ; Rats, Sprague-Dawley ; Tandem Mass Spectrometry ; methods

Objective To identify the epidemiological features of COVID-19 epidemic in Chenzhou City, Hunan province so as to provide scientific evidence for effective containment of the COVID-19 epidemic. Methods Descriptive epidemiological method was used to retrospectively characterize the confirmed COVID-19 cases and asymptomatic cases in Chenzhou City from January 23 through March 10, 2020. Results A total of 39 confirmed COVID-19 cases and 6 asymptomatic cases infection were documented in the city, with no death.We identified 8 clusters of COVID-19, which were all familial transmission.There was statistical difference between the sources of different types of epidemic (χ²=15.996, P < 0.001), in which all the local COVID-19 cases were the secondary cases in the clusters.As the epidemic expanded, the trend shifted from imported-case-centered to local-case-centered.The epidemic has covered 81.81% of the city area; in each area, the first COVID-19 cases were all imported. Conclusion The COVID-19 epidemic has been effectively controlled.At present, we focus on the quarantine in the entry and exit to prevent the imported epidemic.