2020 Vol. 38, No. 6
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2020, 38(6): 481-484.
doi: 10.12206/j.issn.1006-0111.202003055
Abstract:
COVID-19 patients infected with SARS-CoV-2 showed different degrees of liver injury. A series of studies have shown that cytokine storm, bile duct cell injury caused by SARS-CoV-2 and drug-induced hepatotoxicity can induce secondary liver injury. This article will review the mechanism of liver injury caused by different factors and the treatment of hepatoprotective drugs, in order to provide reference support for further research in this field.
COVID-19 patients infected with SARS-CoV-2 showed different degrees of liver injury. A series of studies have shown that cytokine storm, bile duct cell injury caused by SARS-CoV-2 and drug-induced hepatotoxicity can induce secondary liver injury. This article will review the mechanism of liver injury caused by different factors and the treatment of hepatoprotective drugs, in order to provide reference support for further research in this field.
2020, 38(6): 485-491, 538.
doi: 10.12206/j.issn.1006-0111.202005078
Abstract:
Objective To investigate the active ingredients of Jingfang Baidu San for the prevention and treatment of COVID-19 by using network pharmacology and molecular docking, and to provide references for clinical applications. Methods The chemical constituents and action targets of all medicinal materials in Jingfang Baidu San were retrieved from TCMSP. Uniprot database was used to search the corresponding genes of targets. Cytoscape software was used to construct the network of medicinal materials-compounds-targets for visualization. The target proteins of COVID-19 were searched by disease databases. The intersection of both was considered to be analyzed to establish the protein-protein interaction (PPI) network by STRING database. GO function enrichment analysis and KEGG pathway enrichment analysis were performed through Metascape database to predict its mechanism. The effective strength of core constituents on preventing COVID-19 was calculated by molecular docking method. Results A total of 159 effective ingredients and 277 potential targets were obtained in Jingfang Baidu San within the given screening conditions [oral bioavailability (OB) ≥30%; drug-like (DL) ≥ 0.18], including 55 core targets with the intersection of 273 targets of COVID-19. According to the results of GO and KEGG enrichment analysis performed on the core targets, 1376 GO items and 136 KEGG pathways were obtained, involving infectious diseases, cancer, cell progress, immune system, signaling pathways etc. The results of molecular docking indicated strong binding capacity between the core ingredients and SARS-CoV-2 3CL hydrolase or angiotensin-converting enzyme II (ACE2). The hydrogen binding and hydrophobic effect were the main forms of the interaction. Conclusion The active ingredients in Jingfang Baidu San can inhibit the binding between SARS-CoV-2 protein and ACE2, thus regulating multiple targets and signal pathways, which plays a role in the prevention and the treatment of COVID-19.
2020, 38(6): 492-495.
doi: 10.12206/j.issn.1006-0111.202007063
Abstract:
Humulus lupulus is a kind of special resource plant used both as medicine and food in Xinjiang. In addition to being widely used in beer brewing, Humulus lupulus has long been recognized for its medicinal value, especially for the treatment of postmenopausal osteoporosis. Modern pharmacological research shows that its active components have great potential in the development of anti-osteoporosis drugs. However, in recent years, the wild Humulus lupulus resources in China have been seriously degraded, and the contents of active components are quite different. Ensuring high-quality Humulus lupulus germplasm resources is a prerequisite for the development and utilization of Humulus lupulus. This paper reviews the major chemical components of Humulus lupulus and their effects and application in the prevention and treatment of osteoporosis, and discusses the existing problems, aiming to provide a reference for the development and utilization of Humulus lupulus against osteoporosis.
Humulus lupulus is a kind of special resource plant used both as medicine and food in Xinjiang. In addition to being widely used in beer brewing, Humulus lupulus has long been recognized for its medicinal value, especially for the treatment of postmenopausal osteoporosis. Modern pharmacological research shows that its active components have great potential in the development of anti-osteoporosis drugs. However, in recent years, the wild Humulus lupulus resources in China have been seriously degraded, and the contents of active components are quite different. Ensuring high-quality Humulus lupulus germplasm resources is a prerequisite for the development and utilization of Humulus lupulus. This paper reviews the major chemical components of Humulus lupulus and their effects and application in the prevention and treatment of osteoporosis, and discusses the existing problems, aiming to provide a reference for the development and utilization of Humulus lupulus against osteoporosis.
2020, 38(6): 496-500, 567.
doi: 10.12206/j.issn.1006-0111.202006061
Abstract:
Type 2 diabetes is a high risk factor for atherosclerotic cardiovascular disease. Studies have found that SGLT-2 inhibitor and GLP-1 receptor agonists have cardiovascular protective effects in patients with type 2 diabetes and cardiovascular disease. Therefore, from the aspects of cardiovascular safety test and its Meta-analysis and net-like Meta-analysis, the research progress of cardiovascular safety of SGLT-2 inhibitors and GLP-1 receptor agonists is summarized.
Type 2 diabetes is a high risk factor for atherosclerotic cardiovascular disease. Studies have found that SGLT-2 inhibitor and GLP-1 receptor agonists have cardiovascular protective effects in patients with type 2 diabetes and cardiovascular disease. Therefore, from the aspects of cardiovascular safety test and its Meta-analysis and net-like Meta-analysis, the research progress of cardiovascular safety of SGLT-2 inhibitors and GLP-1 receptor agonists is summarized.
2020, 38(6): 501-505.
doi: 10.12206/j.issn.1006-0111.202007031
Abstract:
Colorectal cancer is a malignant tumor with increasing incidence in China. Chemotherapy or neoadjuvant therapy are needed when the patients have deep tumor invasion of distant metastasis due to the hidden clinical manifestations and limited screening methods for the colorectal cancer. With many side effects of the current chemo-medications and the drug resistance, researchers are actively exploring new chemotherapy drugs for colorectal cancer. Paclitaxel is a first-line chemotherapy drug for the treatment of breast cancer, ovarian cancer, pancreatic cancer and other malignant tumors. Colorectal cancer cells are prone to become resistant to paclitaxel and the treatment efficiency was limited. However, new drug delivery systems and the combination drug therapy can enhance the treatment efficiency. This article reviews the effective treatment strategies of paclitaxel for colorectal cancer with the hope for new ideas and more effective chemotherapy.
Colorectal cancer is a malignant tumor with increasing incidence in China. Chemotherapy or neoadjuvant therapy are needed when the patients have deep tumor invasion of distant metastasis due to the hidden clinical manifestations and limited screening methods for the colorectal cancer. With many side effects of the current chemo-medications and the drug resistance, researchers are actively exploring new chemotherapy drugs for colorectal cancer. Paclitaxel is a first-line chemotherapy drug for the treatment of breast cancer, ovarian cancer, pancreatic cancer and other malignant tumors. Colorectal cancer cells are prone to become resistant to paclitaxel and the treatment efficiency was limited. However, new drug delivery systems and the combination drug therapy can enhance the treatment efficiency. This article reviews the effective treatment strategies of paclitaxel for colorectal cancer with the hope for new ideas and more effective chemotherapy.
2020, 38(6): 506-508, 542.
doi: 10.12206/j.issn.1006-0111.201908127
Abstract:
Objective To design, synthesize and measure antifungal activities of galloyl piperazine derivatives. Methods Trimethoxyl gallic acid was used as starting material, reacted with piperazine in the presence of PyBOP/DIEA to afford the intermediates. The target compounds were obtained through the reaction with corresponding acids after deprotection gave. The antifungal activities of the target compounds were evaluated by FLC-resistant Candida albican isolated according to the CLSI recommended method. Results 11 target compounds were synthesized and six of them showed more potent antifungal activities than gallic acid. Conclusion Galloyl piperazine derivatives could enhance antifungal activities. Galloyl moiety was an important pharmacophore, which could improve antifungal activities with the introduction of cinnamic acid and 2,3-dichlorobenzoic acid.
2020, 38(6): 509-515.
doi: 10.12206/j.issn.1006-0111.202008078
Abstract:
Objective To optimize the extraction process of collagen from the jellyfish (Nemopilema nomurai) and explore its characters. Methods The collagen was extracted with acetic acid and pepsin from jellyfish. The crude jellyfish collagen was purified by salting out and ultrafiltration. The purified collagen was characterized and analyzed by XRD (X-ray diffraction), UV (ultraviolet spectroscopy) and FTIR (fourier transform infrared spectroscopy). Results The purity of jellyfish collagen was 97%, the yield was 33% (dry weight). The jellyfish collagen maintained its triple helix structure during the extraction and purification process. Jellyfish collagen conformed to the characteristics of type I collagen according to amino acid composition and gel electrophoresis analysis. The jellyfish collagen exhibited a good solubility under the conditions of pH 3–5 and less than 0.9 mol/L of NaCl. Conclusion The extracted jellyfish collagen exhibited similar characteristics with bovine type I collagen and was a potential new source of collagen.
2020, 38(6): 516-522.
doi: 10.12206/j.issn.1006-0111.202006002
Abstract:
Objective To explore the possible mechanism of activating blood circulation and removing blood stasis herbs in the treatment of endometriosis (EM) with network pharmacology approach. Methods Seven kinds of commonly used activating blood circulation and removing blood stasis herbs, such as: peach kernel, safflower, zeilan, salvia miltiorrhiza, leonuri, radix cyathulae, and wang buliuxing were selected as the research subjects. TCMSP platform, a database of traditional Chinese medicine chemical ingredients, was used to retrieve the effective ingredients of 7 herbs. The targets of the effective ingredients were obtained through the Targets information software. GeneCards database was used to collect EM related target genes. Venn diagram tool was used to obtain the target genes of active ingredients of activating blood circulation and removing blood stasis herbs. Cytoscape 3.6.0 software was used to construct the active ingredient-target-disease network. KEGG database was used to analyze the signal pathways of target gene enrichment. Results A total of 94 active ingredients and 119 targets of 7 herbs were screened. Quercetin, luteolin and kaempferol were the key active components. PTGS2, PTGS1, NCOA2 and NCOA1 were the key targets. The 7 herbs have 20 related KGEE pathways, involving sex hormones, inflammation, apoptosis and angiogenesis. PI3K-Akt signaling pathway, IL-17 signaling pathway, TNF signaling pathway were the main pathways. Conclusion The treatment of EM with activating blood circulation and removing blood stasis herbs has the characteristics of multiple components, multiple targets and multiple pathways, which can relieve the pain, inflammation and menstrual disorders symptoms of EM.
2020, 38(6): 523-527.
doi: 10.12206/j.issn.1006-0111.202005047
Abstract:
Objective To investigate the protective effect of menatetrenone (MK4) on the osteoblasts in oxidative stress, and to clarify the anti-osteoporosis mechanism of MK4. Methods Mouse osteoblasts (MC3T3-E1) induced by hydrogen peroxide (H2O2) was used. Cell viability, ALP activity and the area of bone nodule were observed. The level of ROS was detected by DCFH-DA, mitochondrial membrane potential by JC-1, apoptosis rate by annexin V-FITC/PI, and the expression of FoxO1, FoxO3, SOD, bcl-2 and bax by RT-PCR. Results Menatetrenone at 10 μmol/L significantly increased the proliferation of osteoblasts stimulated by H2O2, ALP activity, bone nodule formation area, cell membrane potential, the antioxidant SOD and transcription factors FoxO1 and FoxO3 mRNA expression. In the meantime, the elevated malondialdehyde and reactive oxygen species level in cells induced by H2O2, the apoptosis rate and the mRNA expression level of bax/Bcl-2 were significantly reduced. Conclusion menatetrenone can protect osteoblasts from oxidative damage by regulating FoxO pathway and reduce osteoblasts apoptosis by up regulating the proportion of Bcl-2/bax.
2020, 38(6): 528-532.
doi: 10.12206/j.issn.1006-0111.202007015
Abstract:
Objective To investigate the anti-inflammatory and analgesic effects of the active fractions of Tongfeng granules on rats with arthritis induced by complete Freund's adjuvant. Methods 56 SD rats were randomly divided into seven groups, blank group, model group, total flavonoids group, total organic acid group, total alkaloid group, Tongfeng granule group and positive control group. Except for the blank group, the remaining 6 groups established joints pathological model of inflammation. 15 days after the successful modeling, intragastric drug administration was continued for 30 days. The swelling of ankle joint, WBC, N%, IL-6, IL-10, TNF-α and the histopathology of joint were measured. Results Comparing with the model group, each effective fraction group of Tongfeng granules, Gout granules and positive control group decreased the ankle joint swelling rate significantly (P<0.01) and reduced fibrous tissue proliferation. There was no significant difference in WBC and N% of neutrophils. They significantly reduce the level of serum IL-6 and TNF-α, and increase the level of IL-10 (P<0.05, P<0.01). Conclusion This study clarifies the anti-inflammatory and analgesic effects of active fractions of Tongfeng granules and provides a basis for further clinical medication and preparation development.
2020, 38(6): 533-538.
doi: 10.12206/j.issn.1006-0111.202004089
Abstract:
Objective To evaluate the genetic toxicity of Wentilactone A. Methods The classical genotoxicity test combination (Ames test, in vitro CHO cell chromosome aberration test and mouse bone marrow micronucleus test) was used to detect the genotoxicity of Wentilactone A. Results Ames test suggested that Wentilactone A was not mutagenic against Salmonella typhimurium with or without the metabolic activation system (S9) at five doses of 5 000, 500, 50, 5, and 0.5 μg/dish. CHO cell chromosome aberration test suggested that the CHO cells cultured in 4 h and 24 h did not induce chromosomal aberrations in three dose groups at the final concentration of 23.74, 47.48, 94.96 μg/ml, with and without S9. The mouse bone marrow micronucleus test showed no significant difference in the bone marrow micronucleus induction rate of cells at three doses of 100, 200, and 400 mg/kg treated for 24 h and at dose of 400 mg/kg treated for 48 h compared with the solvent control group (P>0.05). Conclusion These results indicated that Wentilactone A did not exhibit genetic toxicity based on the Ames test, CHO chromosomal aberration test and micronucleus assay. It was suggested that Wentilactone A had no genetic toxicity and potential carcinogenicity.
2020, 38(6): 539-542.
doi: 10.12206/j.issn.1006-0111.202004077
Abstract:
Objective In order to solve the obvious adverse reactions of ribavirin, to develop ribavirin liposome inhalation powder and to evaluate its quality characteristics. Methods The ribavirin liposomes were prepared by the thin film dispersion method, and then lyophilized to prepare ribavirin liposome powder. The appearance, fluidity, bulk density, encapsulation efficiency, particle size of the complex solution, PDI, potential and hydrophilicity were examined. Results Ribavirin liposome powder has good morphology, particle size, potential, fluidity and hydrophilicity, which can meet the basic requirements of powder medicine for drug administration. Conclusion The technique of preparing ribavirin liposome powder aerosol preparation by this method is feasible, and it provides the basic technology for future in vivo and in vitro studies.
2020, 38(6): 543-546.
doi: 10.12206/j.issn.1006-0111.202003040
Abstract:
Objective To establish a two-dimensional high-performance liquid chromatography method for the determination of tigecycline in human cerebrospinal fluid, which can be used for the drug monitoring in patients with intracranial infection. Methods The quantification was carried out by an external standard method. The first-dimension column was a Aston SNX5 phenyl chromatographic column (50 mm×4.6 mm, 5 μm) with ammonium phosphate (pH was adjusted with ammonium hydroxide to 7.5)-methanol (45∶55, V/V) as the mobile phase and the flow rate was 1.2 ml/min. The second-dimension chromatographic column was Aston SC5 C18 (275 mm×4.6 mm, 5 μm), with ammonium phosphate (pH was adjusted with ammonium hydroxide to 7.4)-ammonium phosphate (pH was adjusted with ammonium hydroxide to 3.0)- acetonitrile (30∶50∶20, V/V/V) as the mobile phase and the flow rate was 1.0 ml/min. The detection wavelength was 340 nm. The temperature was 40 ℃ and the injection volume was 200 μl. Results The calibration curve of tigecycline showed good linearity from 64.5 to 1 290.0 ng/ml in human cerebrospinal fluid (r=0.999 8). The RSD of intra and inter-day precision were less than 5.0% with the detection accuracy of 98.80%−106.51%. Conclusion This method is simple, quick, accurate, specific and sensitive. It meets the requirements of tigecycline determination in clinical human cerebrospinal fluid, which offers the individualized therapeutic assurance for patients with intracranial infection.
2020, 38(6): 547-551.
doi: 10.12206/j.issn.1006-0111.202003184
Abstract:
Objective To establish an assay method for unbound teicoplanin in plasma by centrifugal ultrafiltration combined with ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). Methods Protein was removed from plasma by a Centrifree® ultrafiltration device. The ultrafiltrate was injected to determine the unbound concentration of teicoplanin. EndeadvorsilTM C18 column (1.8 μm, 50 mm×2.1 mm) was used with gradient elution of acetonitrile and 0.02 mol/L ammonium acetate solution (containing 0.1% formic acid). The detection was performed on a triple-quadrupole tandem mass spectrometer by multiple reaction monitoring (MRM)mode via electro spray ionization (ESI). Results The calibration curve of unbound teicoplanin in plasma was linear over the range of 0.10 to 8.00 μg/ml (r=0.999). The intra-assay precision and the inter-assay precision of samples didn't exceed 7.00%. The average relative recovery ratio was 97.9%, and the matrix effect factor was 0.97. The samples had good stability after being stored at room temperature for 10 h or at −20 ℃ for 15 days, and freeze-thawed 3 times (RSDs were all within 6.50%). Conclusion This method is convenient, fast, sensitive and accurate. It provided a basis for clinical development of teicoplanin unbound concentration monitoring.
2020, 38(6): 552-557.
doi: 10.12206/j.issn.1006-0111.202008069
Abstract:
Objective To investigate the overall incidence and risk of hypertension in the treatment of cancer patients who receive anlotinib and compare the differences between anlotinib and other VEGFR inhibitors. Methods Pubmed, Embase, Cochrane Library, ASCO, CNKI, Wangfang, VIP and CBM databases were searched. Eligible studies were phase II and III prospective clinical trials on cancer patients who received anlotinib and had the hypertension data available. Meta-analysis for the incidence and risk of anlotinib was performed by using R software (version 3.6.0). SPSS software (version 26.0) was used to compare the difference between anlotinib and other VEGFR inhibitors. Results A total of 1387 cancer patients from 13 clinical trials were included in the Meta-analysis. The overall incidences of all grade and high grade hypertension in cancer patients who received anlotinib were about 47.1% (95%CI: 37.7%−56.6%) and 10.6% (95%CI: 7.4%−14.2%). The use of anlotinib was associated with significantly increased risk of all grade (RR=5.58, 95%CI: 2.29−13.60, P<0.01) and high grade hypertension (RR=27.78, 95%CI: 3.56−216.86, P<0.01). In addition, the incidence of high grade hypertension associated with anlotinib was similar to axitinib (RR=0.79, 95%CI: 0.61−1.02, P=0.066) and cabozantinib (RR=0.87, 95%CI: 0.67−1.13, P=0.290). The incidences of rest of other VEGFR inhibitors were lower than that of anlotinib. Conclusions There is a high incidence and significant risk of developing hypertension in cancer patients receiving anlotinib. Adequate monitoring and timely treatment of hypertension is recommended.
2020, 38(6): 558-562.
doi: 10.12206/j.issn.1006-0111.202007073
Abstract:
Objective To review and analysis the clinical manifestations, occurrence rules, treatment and outcomes of adverse drug reactions caused by anlotinib in order to provide reference for safety and reasonable use of anlotinib in clinical practice. Methods The cases reports of anlotinib were searched in Web of Science, Pubmed, Wiley Online Library, CNKI, Wanfang and VIP. The basic patient information, adverse reaction time, characters, treatment, outcomes and involved systems or organs were collected and analyzed. Results A total of 20 cases were collected, 10 females and 10 males, with a median age of 63.5(36～76 years old). Adverse drug reactions mostly occurred within 2 months after the medication. 52 cases occurred in total, involving 9 systems/organs, of which blood and lymphatic system disorders (all were hypertension) were the most common (21.2%). Conclusion After the administration of anlotinib, the incidence rate of adverse reactions in the cardiovascular system is relatively high. The medication process should be closely monitored, and attention should be paid to monitoring the potential adverse reactions mentioned in the instructions.
2020, 38(6): 563-567.
doi: 10.12206/j.issn.1006-0111.201911056
Abstract:
Objective To improve the quality for authorized distribution of traditional Chinese medicine pieces, reduce patient complaints and increase patient satisfaction. Methods Patient’s complaints against different drug dispensing modes were analyzed. PDCA cycle was used for quality improvements. Results The new quality control mode includes pre monitoring measures, such as pharmacist resident in pharmaceutical factories and unannounced factory inspections, the fast-track handing measures for the problems occurred in patients, pharmacies, pharmaceutical factories and express delivery companies, and retrospective measures, such as evaluation of pharmaceutical factories and quarterly pharmaceutical factory communication meetings. Conclusion Three years after the new quality control mode, patient’s complaints were significantly reduced. The authorized distribution quality for traditional Chinese medicine pieces was greatly improved.
2020, 38(6): 568-573.
doi: 10.12206/j.issn.1006-0111.202003200
Abstract:
Objective To provide data reference for improving the selection criteria of the dosage forms and specifications of the electrolytes and antipyretic analgesics in the Essential Medicines List, and to improve the applicability of these medicines to children and the availability of essential medicines. Methods The market and prices of electrolytes and antipyretic analgesics were retrieved by the system. The data were processed by Excel software, and the different dosage forms were compared and analyzed. Results 8 medication classes were included for adjusting water, electrolytes and acid-base balance, and another 16 classes were analgesic, antipyretic, anti-inflammatory, anti-rheumatic and anti-gout drugs. Those medications were characterized with many registered approval numbers, manufacturers and some considerations for pediatric uses. The proper prices were given for different dosage forms and specifications. There is a room for improvement regarding the specifications of potassium, glucose injections, and acetaminophen preparations. Conclusion The selection of pharmaceutical dosage forms and specifications in the Essential Medicines List should be comprehensively evaluated from the registered approval numbers of base medicines, the manufacturers and related prices in pharmaceutical procurement platforms from various provinces, and the clinical needs for special populations. It is recommended that 10 ml: 1 g potassium chloride injection, 50 ml glucose injection, acetaminophen suppositories and drops were included in the Essential Medicines List.
2020, 38(6): 574-576.
doi: 10.12206/j.issn.1006-0111.202002088
Abstract:
Objective To explore the effect of the intervention of clinical pharmacists on the rational use of piperacillin-tazobactam by using PDCA cycle, in order to provide reference for rational drug use. Methods The problems of piperacillin-tazobactam in our hospital was analyzed. PDCA cycle was used to manage the problems. Then, the data before and after PDCA cycle was compared and analyzed. Results After using PDCA cycle, the irrational use rate of piperacillin-tazobactam gradually decreased, from 9% in February 2018 to 2% in February 2019; the doses decreased from 4380 in February 2018 to 3346 in February 2019; and the frequency of usage decreased from 391 DDDs in February 2018 to 298 DDDs in February 2019. The effectiveness and continuous improvement of PDCA cycle in managing piperacillin-tazobactam were significant. Conclusion PDCA cycle can effectively improve the management effectiveness of piperacillin-tazobactam administration.
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