2020 Vol. 38, No. 5
Display Method:
2020, 38(5): 385-397.
doi: 10.12206/j.issn.1006-0111.202005020
Abstract:
Coronavirus infection seriously threatens human health. There is no specific medication or vaccine so far. In recent years, domestic and foreign researchers have developed a variety of small-molecule inhibitors against the ligand S protein, RdRp, PLpro and 3CLpro of three highly pathogenic coronavirus, SARS-CoV, MERS-CoV, SARS-CoV-2. This article reviews the characteristics of these coronaviruses, action targets, small molecule inhibitors, and structure-activity relationships.
Coronavirus infection seriously threatens human health. There is no specific medication or vaccine so far. In recent years, domestic and foreign researchers have developed a variety of small-molecule inhibitors against the ligand S protein, RdRp, PLpro and 3CLpro of three highly pathogenic coronavirus, SARS-CoV, MERS-CoV, SARS-CoV-2. This article reviews the characteristics of these coronaviruses, action targets, small molecule inhibitors, and structure-activity relationships.
2020, 38(5): 398-403, 422.
doi: 10.12206/j.issn.1006-0111.202005042
Abstract:
The corona virus disease 2019 (COVID-19) has recently become pandemic and is still spreading. Many severe or critical COVID-19 cases meet the diagnostic criteria of sepsis and septic shock in the clinical manifestations. It is important to study the pathogenesis and treatment strategy of COVID-19 for the disease prevention and control. This article reviews the clinical features and treatment progress of COVID-19 viral sepsis.
The corona virus disease 2019 (COVID-19) has recently become pandemic and is still spreading. Many severe or critical COVID-19 cases meet the diagnostic criteria of sepsis and septic shock in the clinical manifestations. It is important to study the pathogenesis and treatment strategy of COVID-19 for the disease prevention and control. This article reviews the clinical features and treatment progress of COVID-19 viral sepsis.
2020, 38(5): 404-408, 434.
doi: 10.12206/j.issn.1006-0111.202005040
Abstract:
Objective To investigate the characteristics of the adverse drug reaction (ADR) in the traditional Chinese medicine (TCM) treatment followed the "COVID-19 Diagnosis and Treatment Program (trial version 7)" during the medical observation period, and to provide a guideline for rational clinical drug use. Methods 9 TCM induced ADR were collected from CNKI, Wanfang database and PubMed. Statistical analysis was conducted on gender, age, occurrence time, involved system/organ, treatment, outcome and relevance evaluation. Results 61 literatures were collected according to the inclusion and exclusion criteria with 70 cases and 5 TCM prescriptions. There was no significant bias in gender. The age span was large. Most ADR occurred within 1 day after administration. The involved systems/organs are extensive, mainly on the skin and its accessories. The most common therapeutic drugs were antihistamines and steroids, and other medications are mainly for symptom treatment. The turnaround time was 1 h in most cases (47%). Conclusions During the observation period, the incident population was widely distributed and there was no obvious characteristics. Medication monitoring should be reinforced to reduce the ADR incidence.
2020, 38(5): 409-412.
doi: 10.12206/j.issn.1006-0111.202004035
Abstract:
Cuscuta chinensis is a commonly used traditional Chinese herbal medicine. Cuscuta chinensis has a long history of clinical application in the treatment of varieties of ocular diseases. This review summarized the literatures related to its clinical applications, research progresses in the ophthalmic pharmacology and active ingredients. It was aimed to provide a theoretical basis for the further development and utilization of Cuscuta Chinensis as an effective medication.
Cuscuta chinensis is a commonly used traditional Chinese herbal medicine. Cuscuta chinensis has a long history of clinical application in the treatment of varieties of ocular diseases. This review summarized the literatures related to its clinical applications, research progresses in the ophthalmic pharmacology and active ingredients. It was aimed to provide a theoretical basis for the further development and utilization of Cuscuta Chinensis as an effective medication.
2020, 38(5): 413-417, 430.
doi: 10.12206/j.issn.1006-0111.202004050
Abstract:
Objective To study the action of kaempferol (KAE) against Candida albicans biofilms and explore the potential mechanisms. Methods Biofilm metabolic activity assay was used to investigate the action of KAE against C. albicans biofilm formation as well as mature biofilm. The inhibition of KAE in hyphal formation was examined by microscope. The water-hydrocarbon two-phase separation assay was used to test the effect of KAE on the cell surface hydrophobicity of C. albicans. The mRNA expression of the genes involved in biofilm formation was determined by real time RT-PCR. Results KAE showed inhibition effect on C. albicans biofilm formation in a dose-dependent manner. Moreover, KAE inhibited mature biofilm. The biomass of biofilm was reduced upon KAE treatment. KAE inhibited hyphal formation and reduced the cell surface hydrophobicity of C. albicans. In the presence of KAE, the mRNA expression of the genes involved in biofilm formation was changed, with the up-regulation of BCR1,NRG1,TUP1 and down-regulation of HWP1,EFG1,CPH1,ALS1,ALS3 and CSH1. Conclusion KAE showed antifungal activity against C. albicans biofilm. The mechanisms may relate to the inhibition of hyphal formation and reduction of cell surface hydrophobicity.
2020, 38(5): 418-422.
doi: 10.12206/j.issn.1006-0111.202001071
Abstract:
Objective To discover the medicinal active molecules from the fermentation extract of sponge-symbiotic Streptomyces sp. LHW2432. Methods Compounds were isolated and purified from the fermentation extract of LHW2432 by silica gel, ODS chromatographic columns, and HPLC. The structures of the compounds were elucidated based on the analyses of modern spectrum technologies and the related literatures research. Through plate coating method and broth microdilution method, the antimicrobial activities were tested by the indicator strains of Bacillus mycoides, methicillin-resistant Staphylococcus aureus (MRSA), Mycobacterium smegmatis, Candida Albicans, and Escherichia coli. Results Five compounds were discovered and their structures were identified as descycloavandulyl-lavanduquinocin ( 1 ), N-acetyltyramine ( 2 ), phomapyrone C ( 3 ), germicidin A ( 4 ), and germicidin I ( 5 ). Compound 1 showed inhibitory activities against MRSA (MIC, 100 μg/ml) and M. smegmatis (MIC, 64 μg/ml), respectively. Conclusion Five compounds were discovered from LHW2432, among which compound 1 was a new natural product and could be used as a precursor of the tricyclic carbazole alkaloids with neuroprotective activity. Moreover, compound 1 showed weak inhibitory activities against gram-positive pathogenic bacteria.
2020, 38(5): 423-430.
doi: 10.12206/j.issn.1006-0111.202003073
Abstract:
Objective To analyze and identify the chemical components in the Nocardia rubra cell wall skeleton (Nr-CWS), and to determine the contents of monosaccharides accurately. Methods The extract of Nr-CWS was separated and analyzed by UHPLC-Q-TOF/MS method. The chemical components were quickly identified by matching the data with the information in the Metlin database. The monosaccharide contents in the Nr-CWS extract were determined by UHPLC-MS/MS method after derivatization. Results A total of 64 chemical components were identified in the extract of Nr-CWS, including amino acids, monosaccharides and so on. A assay method for 8 monosaccharides by UHPLC-MS/MS was successfully established. The content of arabinose in Nr-CWS was the highest, followed by galactose, which indicated that the main polysaccharide components in Nr-CWS may be composed of these monosaccharides. Conclusion In this study, we analyzed the main chemical components of Nr-CWS, which are amino acids, fatty acids and so on. The content of monosaccharide after polysaccharide hydrolysis was determined by UHPLC-MS/MS. This will lay a foundation for the screening of the active components of Nr-CWS and the study of its pharmacological mechanism.
Effects of compound Ziyin granule on sex hormones and oxidative stress levels of ovariectomized rats
2020, 38(5): 431-434.
doi: 10.12206/j.issn.1006-0111.201912023
Abstract:
Objective To investigate the effect of compound Ziyin granule (CZG) on sex hormones and oxidative stress levels of ovariectomized rats. Methods The experiment was divided into model group, Liuwei Dihuang pill group, estradiol valerate group, Zishen Yangyin Decoction group, CZG (low, medium, high dose) group, ormal group and sham operation group. After administration for 8 weeks, serum estradiol (E2), follicle stimulation hormone (FSH), luteotropic hormone (LH), total-superoxide dismutase (T-SOD), malonaldehyde (MDA) and glutathione peroxidase (GSH-Px) were measured. Results Compared with the model group, E2 was significantly raised at medium and high doses of CZG, LH was decreased at medium dose, and FSH was reduced at low, medium and high dose; medium and high dose of CZG were capable of remarkably increasing T-SOD, GSH-Px and decreasing MDA, and low dose raised T-SOD and reduced MDA (P<0.05 or P<0.01). Compared with estradiol valerate group, low dose of CZG significantly increased T-SOD (P<0.05). Compared with decoction group, GSH-Px was remarkably raised at medium and high dose (P<0.05). Conclusion The CZG could reverse the abnormal function of sex hormone secretion in the pituitary-ovary axis of the ovariectomy perimenopausal model rat and improve its antioxidant capacity.
2020, 38(5): 435-440.
doi: 10.12206/j.issn.1006-0111.202003127
Abstract:
Objective To investigate the potential mechanism of Rhizoma Coptidis extracts (RCE) against sepsis associated with acute kidney injury. Methods C57BL/6 mice were divided into sham group, model group and RCE treatment group. The levels of Scr and BUN were measured by test kits. Gas chromatography-mass spectrometry was used to analyze metabolic changes in kidneys. Results The levels of Scr and BUN were increased in the model group than sham, which were reversed by RCE. 16 metabolites related to the progress of sepsis associated with acute kidney injury were detected, which were involved in amino acid metabolism and carbohydrate metabolism. Among these metabolites, the level of 8 metabolites can be reversed with RCE treatment. Conclusion RCE might exert therapeutic effects in sepsis associated with acute kidney injury by altering multiple metabolic pathways.
2020, 38(5): 441-446, 457.
doi: 10.12206/j.issn.1006-0111.201910022
Abstract:
Objective To evaluate the effects of different solubilizing techniques on the in vitro dissolution and in vivo pharmacokinetics of Sirolimus (SRL). Methods Solid dispersions (SD), inclusion complex (IC), self-micro emulsifying drug delivery system (SMEDDS) and nano-structured lipid carrier (NLC) were selected as the solubilization technology for SRL. SRL-SMEDDS and SRL-NLC have obtained the optimal prescription in the previous studies. Additionally, the formulation process of SRL-SD and SRL-IC was screened by using inclusion rate and dissolution profiles as indicators. 0.4% SDS, water and buffer solutions with pH 1.2, 4.5, 6.8, 7.4 were used as dissolution media. The dissolution profile of the commercially available formulation Rapamune® and the lab-made solubilized preparations were investigated. The in vivo absorption of the above preparations was examined using a pharmacokinetic test in Beagle dogs. Results In 0.4% SDS, the dissolution of each preparation exceeded 80% in 2 h. In the medium of pH 1.2, the dissolution of SRL-SD could not be measured while the dissolution of IC, SMEDDS and NLC increased first and then decreased. In other media, the dissolution of the SRL was reduced. The SRL-IC showed the best dissolution without a significant decrease. The relative bioavailability of APIs, SRL-SD, SRL-IC, SRL-NLC and SRL-SMEDDS were 9.1%, 18.7%, 33.2%, 78.0%, and 97.6% respectively in vivo pharmacokinetic tests. Conclusion SD, SMEDDS, NLC, and IC can improve the in vitro dissolution and in vivo absorption of SRL. Among them, SMEDDS has the most significant improvement in the bioavailability of SRL.
2020, 38(5): 447-450.
doi: 10.12206/j.issn.1006-0111.202003188
Abstract:
Objective To establish the best wine steaming process for morinda officinalis with monotropein as indicator. Methods Response surface methodology was used to optimize the wine steaming process for morinda officinalis with the amount of rice wine, stewing time, moistening time and the monotropein content as evaluation indexes. Results The best condition was identified with rice wine (rice wine/herbs, g/g) 10%, moistening time 1.0 h, fully steamed and dried. Conclusion The Star dot design-response surface method can be used to optimize the wine steaming process for morinda officinalis.
2020, 38(5): 451-457.
doi: 10.12206/j.issn.1006-0111.202004105
Abstract:
Objective To evaluate the developmental toxicity and genotoxicity of leonurine. Methods Leonurine was given orally to SD pregnant rats on the 6th to 15th day of pregnancy at the dose of 500, 1 000 and 2 000 mg/kg body weight. The control group received 0.5% CMC-Na solution orally. Pregnant rats were sacrificed on the 20th day of pregnancy to analyze the reproductive toxicity. Ames test, in vitro chromosomal aberration test of CHO cell and in vivo micronucleus assay were performed to investigate the genotoxicity of leonurine. Results There was no difference statistically in weight gain of pregnant mice between two groups at the dose of 500, 1 000 and 2 000 mg/kg of motherwort alkaloids. In vitro CHO cell chromosomal aberration test indicated that there was no statistical difference between leonurine groups (doses of 250, 500 and 1 000 μg/ml) and the solvent control group with and without metabolic activation system S9. The number of micronuclei in ICR mice did not increase (P>0.05) in the mouse bone marrow micronucleus test at the doses of 100, 500 and 2 000 mg/kg. Conclusion No significant maternal toxicity, embryo toxicity, fetal toxicity and teratogenic effects were observed with leonurine at 500, 1 000 and 2 000 mg/kg doses. Leonurine was not genotoxic in Salmonella typhimurium reverse mutation test, in vitro CHO cells chromosome aberration test or mouse bone marrow micronucleus test. It showed that leonurine had no developmental toxicity and genotoxicity under the conditions of the experiment.
2020, 38(5): 458-461.
doi: 10.12206/j.issn.1006-0111.202004115
Abstract:
Objective To verify the feasibility and maneuverability of fast bare-handed vertical slicing method for dry Chinese herbal medicine, and to provide reference of this method for different types of medicinal materials. Methods Several representative medicinal herbs were randomly selected in the market to make micro-slices using the top-slicing method to observe its cutting effect. Results Experiments showed that microscopic slices can be obtained for most herbs in a few minutes, which can be used for identification and quality testing. Conclusion This method is fast, effective, simple and practical. It meets the requirements of pharmacopoeia for microscopic identification. This method deserves for promotion.
2020, 38(5): 462-465.
doi: 10.12206/j.issn.1006-0111.202002059
Abstract:
Objective To establish a method for simultaneous determination of chlorogenic acid, luteolin-7-O-β-D-glucoside,3,5-dicaffeoylquinic acid, linarin and pogostone in Fangshu Qingre mixture by RP-HPLC. Methods ZORBAX-SB-C18 column(4.6 mm×250 mm, 5 μm) was used as the chromatographic column.The mobile phase was 0.2% formic acid water solution(A) and acetonitrile solution (B)with a gradient elution mode. The flow rate was 1.0 ml/min.The detective wavelength was 327 nm. The column temperature was 30 ℃. Results There were good linear relationships in the determination of chlorogenic acid, luteolin-7-O-β-D-glucoside, 3,5-dicaffeoylquinic acid, linarin and pogostone (r≥0.999 6), with the average recovery rate of 102.03%(1.63%), 102.38%(1.51%), 102.39%(1.23%), 103.14%(1.87%) and 104.01%(2.33%). Conclusion The method was simple and stable with a good reproducibility, which could be used as a quality control method for active compotents in Fangshu Qingre mixture.
2020, 38(5): 466-468, 480.
doi: 10.12206/j.issn.1006-0111.202003033
Abstract:
Objective To investigate the extraction methods for active components from oral ulcer film and optimize the determination methods of active components dexamethasone sodium phosphate and metronazole. Methods Different extraction solvents(methanol, water and 70% methanol aqueous) were applied to extract the active components dexamethasone sodium phosphate and metronazole from oral ulcer film, which contents were quantified by a HPLC method. Results the extraction solvent water had the best efficacy and more simpler compared to the other two solvents. Clotriazole showed a good linear relationship within 5.014 5-200.5800 μg/ml (r=0.999 8), and the average extraction recovery was (104.23±0.63)%, and for dexamethasone sodium phosphate, a good linear relationship was obtained in the range of 0.482-16.328 μg/ml (r=0.9999), and the average extraction recovery was (103.97±1.02)%. Conclusion The water extraction method established in this study was simple and efficient, which showed features of simplicity, accuracy and repeatable.
2020, 38(5): 469-475.
doi: 10.12206/j.issn.1006-0111.202003080
Abstract:
Objective To introduce the improvements of multi-mode outpatient pharmacy services based on the new medical reform policy. Methods The pharmacist’s roles, responsibilities, working procedures and the achievements were discussed. Results and conclusion On-site pharmacy counseling services and online WeChat pharmacy consulting services were established to include collaborative drug therapy management of pharmacists and physicians (Alzheimer's disease and anticoagulation clinic), the outpatient pharmacy services by pharmacists (chemo medication counseling). The multi-mode pharmacy services in our hospital have optimized patient's medication regime, safeguarded patient's medication therapy, improved patient's compliance and reduced medication cost. The individualized medication therapy reduced adverse reactions significantly. The multi-mode outpatient pharmacy services established by our hospital were successful and could serve as a model for other pharmacies in our country.
2020, 38(5): 476-480.
doi: 10.12206/j.issn.1006-0111.201912161
Abstract:
Objective To improve laboratory research of generic drugs in Chinese pharmaceutical enterprises, avoid the defects in the research process, and explore the feasibility of six sigma management (DMAIC) as improvement model in the process of generic drugs laboratory research. Methods The effectiveness of DMAIC implementation was evaluated through the literature search and case study of a generic API’s process with the DMAIC model. Results The DMAIC model was successfully applied in this case. The model made laboratory research more reasonable, helped R&D personnel to pinpoint key quality attributes and process parameters, etc., ensured the authenticity and completeness of experimental data, and provided valuable data for subsequent industrial production as well as meeting registration requirements. Conclusion DMAIC model can solve the problems, such as poor overall arrangement, poor connection with production, and irregular management. It embodied the idea of Quality by Design (QbD) and can be used as good reference for domestic laboratory research of generic drugs.
Contribution System
Author Login
Review Login
Editor Login
Reader Login
News