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1.
Acta Pharmaceutica Sinica ; (12): 2453-2460, 2022.
Article in Chinese | WPRIM | ID: wpr-937058

ABSTRACT

Wuzhi tablet (WZ) is a prescribed herbal medicine extracted from Schisandra sphenanthera, which is widely used to protect the liver injury and drug-induced hepatotoxicity in clinical practices. Previous studies showed that WZ significantly increased the blood concentrations of tacrolimus, cyclosporine A, paclitaxel by inhibiting the cytochrome P450 3A (CYP3A)-mediated metabolism. CYP3A4 and CYP3A5 are the most important isoenzymes among the CYP3A subfamily. However, there are some differences in the catalytic and inhibitory activities between CYP3A4 and CYP3A5, which may lead to different risk of drug-drug and herb-drug interactions, and the risks may be further amplified in vivo. Currently, few reports have compared the herbal medicine inhibitory effects between CYP3A4 and CYP3A5 mediated metabolic reactions. Therefore, detailing the inhibitory effect of WZ on CYP3A4 and CYP3A5 will help understand and predict the potential herb-drug interaction. The results showed that WZ inhibited CYP3A4 and CYP3A5 in a NADPH-, time- and concentration- dependent manner. WZ showed more potent inhibition on CYP3A5 than CYP3A4. Cautions warranted when combining WZ with other therapeutic drugs to avoid the potential herb-drug interaction.

2.
Article in Chinese | WPRIM | ID: wpr-940330

ABSTRACT

By consulting ancient Chinese herbal medicines and medical books, combined with modern documents, the textual research of Polygonati Rhizoma has been conducted to verify the name, origin, bitter-flavored Polygonatum species, Latin name evolution, origin, quality evaluation, harvesting and processing changes, so as to provide reference and basis for the development and utilization of the famous classical formulas. Through textual research, it can be seen that there are many other names for Polygonati Rhizoma, and Huangjing is the correct name since Mingyi Bielu. Based on the original research, it is concluded that P. sibiricum and P. cyrtonema were the mainstream of Polygonati Rhizoma before the Tang dynasty, and P. kingianum was added in the Qing dynasty. According to the shape of medicinal materials, these Polygonatum species were called Jitou Huangjing, Jiangxing Huangjing and Dahuangjing. The harvest time of Polygonati Rhizoma is spring and autumn. After harvest, it is steamed and dried in the sun, and its processing method is mainly "nine steaming and nine storms". Bitter-flavored Polygonatum is mainly P. cirrhifolium, P. zanlanscianense, P. curvistylum and P. verticillatum, which are not suitable for medicine. Based on textual research, it is recommended that when developing famous classical formulas and health products with Polygonati Rhizoma as the main raw material, the origin and producing area should be clear and fixed, and P. sibiricum or P. cyrtonema with clear origin should be used. It is necessary to conduct germplasm survey and sampling in the producing area, establish a planting base and a traceability system for Polygonati Rhizoma, in order to control the quality and stabilize the efficacy of the products. The processing method of Polygonati Rhizoma can be determined according to the product function positioning.

3.
Article in Chinese | WPRIM | ID: wpr-940329

ABSTRACT

By consulting ancient herbal medicines and medical books, combined with modern documents and field investigations, the textual research of Pheretima has been conducted to verify the name, origin, producing area, quality, harvesting and processing changes, and sort out the relationship of origin between ancient and modern times, so as to provide reference and basis for the development and utilization of the related famous classical formulas. Through textual research, it is known that there are many aliases for Pheretima, the rectification of name was "Qiuyin" or "Baijing Qiuyin" in materia medica books. In the Song dynasty and later prescription books, the prescription name is mostly Dilong. From the beginning of Yaowu Chuchanbian (《药物出产辨》), Dilong was used as the rectification of name. It is widely distributed in our country, which is produced all over the country and mostly wild. According to ancient Pheretima with "Baijing Dilong", "Jingbai Shenzi" and "Datiao" as the principles of medicine, combined with historical origin, producing area and easy access, it is confirmed that Pheretima used in ancient times to the present is mainly Pheretima aspergillum, and it also has many other Qiuyin as Pheretima for medicinal purposes. Chinese Pharmacopoeia has unified the origin of the Pheretima since the 1995 edition based on historical origins and actual harvesting conditions. The medicinal material processed by P. aspergillum was called Guangdilong, and the medicinal materials processed by P. vulgaris, P. guillelmi and P. pectinifera were called Hudilong. Since then, all the herbal books published in the future are in line with Chinese Pharmacopoeia that was implemented at that time. The authentic production areas of Guangdilong are Guangdong and Guangxi, and the authentic production areas of Hudilong is Jiangsu, Shanghai, Zhejiang and Anhui. The Guangdilong produced in Guangdong and Guangxi has the best quality. After harvesting, remove the soil and offal, wash and dry. Clinically cut into sections for medicine, or prepare medicine according to prescription. The Pheretima in ancient used "Baijing Dilong", "Jingbai Shenzi" and "Datiao" as the mainstream quality evaluation standards. According to historical origins, P. aspergillum should be the main source of Pheretima, and its quality is better than other species. Therefore, it is recommended that Pheretima in Shentong Zhuyutang use P. aspergillum, which is produced in Guangdong, Guangxi and other places. After harvest, the abdomen was opened in time to remove the viscera and sediment, washed and dried.

4.
Acta Pharmaceutica Sinica ; (12): 1465-1470, 2022.
Article in Chinese | WPRIM | ID: wpr-924751

ABSTRACT

Probe electrospray ionization (PESI) is one of the typical types of ambient ionization technology, but its application in quantitative analysis is limited due to its poor sampling stability. Previously, we developed a new micro-pen electrospray ionization tandem mass spectrometry (μPen-ESI-MS/MS) method based on PESI. In this study, a μPen-ESI-MS/MS method to measure testosterone and dextromethorphan in liver microsome samples was developed and validated to further applicate in evaluating drug metabolism stability and CYP450 enzyme activity. A μPen-ESI-MS/MS method for detecting the CYP3A4 substrate testosterone and CYP2D6 substrate dextromethorphan in the liver microsome incubation system were developed, and the linearity, precision and accuracy of the method was validated. The validated method was further used to detect the metabolic stability of testosterone in the liver microsome incubation system. The results showed that the μPen-ESI-MS/MS had high efficiency with 0.3 min spraying time of each sample. The standard curve of the testosterone and dextromethorphan has good linearity (R2 > 0.99), the intra- and inter-batch accuracy of testosterone and dextromethorphan was 95.9%-109.3% and 90.5%-107.3%, respectively; the intra- and inter-batch precision was acceptable with RSD values of 2.4%-13.5% and 3.4%-12.1%. The half-lives of testosterone and dextromethorphan in the liver microsome incubation system were 12 min and 14 min, respectively. This study provided a rapid and sensitive μPen-ESI-MS/MS method for the assay of testosterone and dextromethorphan in liver microsome samples, and provided a new strategy for the evaluation of drug metabolism stability and CYP3A4/CYP2D6 activity.

5.
Article in Chinese | WPRIM | ID: wpr-875952

ABSTRACT

Objective To study the functional antibody and protection effect against pneumonia disease after inoculation with PPV23 in HIV-infected adults. Methods In 2015, 63 HIV-infected adults were randomly selected in Hongkou District of Shanghai, and blood samples were collected before and one month after the inoculation of PPV23.Functional antibodies against 4 serotypes (19F, 19A, 23F, 6B) of Streptococcus pneumoniae were detected by opsonophagocyitosis killing assay (OPA).The incidence of pneumonia after PPV23 inoculation was also determined. Results The GMT of OPA antibodies against 4 serotypes 1 month after inoculation with PPV23 was significantly higher than that before inoculation in HIV-infected subjects.After inoculation, the triple growth rates of OPA antibodies against 4 serotypes in HIV-infected subjects were 50%-91.67%.The protection rate against pneumonia was 100% in 2 years after PPV23 inoculation in HIV-infected subjects when compared with same group before inoculation as well as the control group.The HIV-infected patients who received highly active antiretroviral therapy (HAART) or had CD4 count of≥300/μL showed better response in production of OPA antibodies and obtained protection against community-acquired pneumonia (CAP) after receiving PPV23. Conclusion Routine vaccination of PPV23 is recommended for HIV-infected patients with good basic conditions.

6.
Article in Chinese | WPRIM | ID: wpr-888174

ABSTRACT

The present study aimed to regulate the market circulation of Caryophylli Flos and formulate standards for commodity specifications and grades of Caryophylli Flos. Market survey was carried out in four major medicinal material markets with 48 samples of Caryophylli Flos collected. The property, 100-seed weight, impurity percentage, moisture, and eugenol content in Caryophylli Flos of different specifications from different producing areas were determined and analyzed. The results showed that 27.1% of the samples surveyed on the markets did not meet the requirements of Chinese Pharmacopoeia(2020 edition). The 100-seed weight and the property are important factors for the classification of Caryophylli Flos specifications. There were significant differences in the property, 100-seed weight, impurity percentage, and eugenol content in Caryophylli Flos samples of different specifications from different producing areas, and also differences in the proportions of different specifications in Caryophylli Flos samples from different producing areas. The African-originated Xiaohong(medium grade) and Guangxi-originated Xiaohong(medium grade) accounted for 70% and 66.7% respectively, the Indonesian-originated Dahong(top grade) for 56.2%. In conclusion, there are many problems in the circulation of Caryophylli Flos at present, mainly including the loss of origin information, no standards for specifications, non-implementation of grade standards, excessive impurities, and no evidence for authenticity identification. According to the classification of Caryophylli Flos specifications in this study, the average eugenol content of Xiaohong is significantly higher than the Dahong by 4.74%.


Subject(s)
China , Drugs, Chinese Herbal/analysis , Indonesia
7.
Acta Pharmaceutica Sinica ; (12): 1360-1368, 2021.
Article in Chinese | WPRIM | ID: wpr-887096

ABSTRACT

Pregnane X receptor (PXR), a member of nuclear receptor superfamily, plays an important role in xenobiotic and endogenous metabolism, endocrine balance, and cell proliferation, etc. Previous study has shown that pregnenolone 16α-carbonitrile (PCN), a mouse PXR agonist, could induce liver enlargement. And we found that the change in hepatocytes exhibits regional distribution characteristics: hepatocyte enlargement occurs around the central vein (CV) area, while hepatocyte proliferation occurs around the portal vein (PV) area. In this study, the dynamic changes of hepatocytes during PXR-induced liver enlargement were determined. Serum and liver samples from male C57BL/6 mice were collected for biochemical and pathological analysis after PCN treatment for 1, 2, 3, 5 days, respectively. The animal experiment was approved by the Animal Ethics Committee of Sun Yat-Sen University. The results showed that with the increase in the PCN treatment days, the feature of this regional change of hepatocyte around the CV and PV areas became more and more obvious. At the same time, the factors related to hepatocyte enlargement, such as the expression of PXR downstream genes and the hepatic content of triglyceride (TG), has gradually increased. The upregulation of proliferation-related proteins and downregulation of cyclin-dependent kinases inhibitor proteins were observed in the early stage of PCN treatment, suggesting that hepatocyte proliferation occurs earlier than hepatocyte enlargement during PXR-induced liver enlargement. This study reveals the dynamic change of hepatocytes during PXR-induced liver enlargement and provides a new insight in liver enlargement promoted via PXR activation.

8.
Acta Pharmaceutica Sinica ; (12): 1147-1154, 2021.
Article in Chinese | WPRIM | ID: wpr-886998

ABSTRACT

Acetaminophen (APAP, also known as paracetamol)-induced liver injury is the leading cause of drug-induced liver injury in the world. Wuzhi Tablet (WZ, an ethanol extract of Schisandra sphenanthera) is widely used in clinical practice to protect liver function. Our previous studies have shown that pretreatment with WZ for 3 days can significantly protect against APAP-induced liver injury; however, the effect of different intervals between APAP and WZ treatment on APAP-induced liver injury remains unclear. In this study, the change in liver injury indexes, APAP metabolites, and the activity of cytochrome P450 (CYP450) enzymes after treatment with WZ and APAP at different intervals were determined. The animal experiment was reviewed and approved by the Animal Ethics Committee of Sun Yat-sen University. The results show that 0 h, 0.5 h, and 2 h pretreatment with WZ significantly protected against APAP-induced liver injury in mice, as evidenced by a significant decrease in biochemical parameters such as alanine aminotransferase (ALT), aspartate aminotransferase (AST), and malonaldehyde (MDA). WZ inhibited the metabolic activation of APAP mediated by CYP450 enzymes and reduced the formation of APAP metabolites. This study further demonstrates that pretreatment with WZ at different intervals (0 h, 0.5 h, and 2 h before APAP dosing) exerts a significant hepatoprotective effect against APAP-induced liver injury, and a single-dose of WZ inhibits the activity of CYP450 enzymes related to APAP metabolic activation, thereby protecting against APAP-induced hepatotoxicity.

9.
Article in Chinese | WPRIM | ID: wpr-884511

ABSTRACT

Objective:Before the radiotherapy was performed, patients with pelvic tumors were analyzed for the consistency of bladder filling in the three steps of " Immobilization" , " CT Simulation" and " X-ray Simulation" .Methods:In 2014, 105 patients (68 cases of cervical cancer, 32 cases of rectal cancer, 3 cases of vaginal cancer and 2 cases of prostate cancer) with pelvic tumor radiotherapy were randomly assigned to monitor bladder urine volume to a target urine volume of 400 ml. First, patient were exhorted to empty the bladder, and the bladder volume meter BVI 9400 was used to measure the urine volume of the patient after emptying of the bladder. The patient immediately drank about 540 ml of water and suppressed urine, measurements were taken every 0.5 h. At the same time, when the patient complained of " urgency of urine" , bladder urine volume would be measured again and the time would also be recorded. Every other half an hour (emptying, 0.5 h after emptying, 1.0 h after emptying), when complaining of " urgency of urine" , when actually performing urine volume and time were described as: U 0 and t 0, U 0.5 and t 0.5, U 1.0 and t 1.0, U t and t, U T and T. Results:There was a statistically significant difference in gender and age, and women had stronger ability to urinate than men U 1.0( P=0.003), young people had stronger ability to urinate than middle-aged U 1.0( P=0.002). In the three-step comparison, there was no statistically difference between 1 hour after emptying urine volume U 1.0( P=0.177) and the actually performing urine volume U T ( P=0.052). And the final urine volume was concentrated at 298-526 ml. After the patient emptied the urine volume and complained of " urgency of urine" , the time slot was t=(75.2±49.9) min, with the urine volume of U t=(331.2±140.3) ml. And there was no statistically difference between U t and U T ( P=0.198) at X-ray Simulation. Conclusions:The patient emptied the bladder and immediately drank 540 ml of water. After 1 hour of suppressing urine, he complained of " urgency of urine" and achieved the target urine volume (400 ml). At this time, the bladder urine volume U 1.0 was consistency in the immobilization, CT Simulation, and X-ray Simulation.

10.
Journal of Integrative Medicine ; (12): 219-225, 2021.
Article in English | WPRIM | ID: wpr-881013

ABSTRACT

OBJECTIVE@#Coronavirus disease 2019 (COVID-19) has become an increasingly severe public health emergency. Although traditional Chinese medicine (TCM) has helped to combat COVID-19, public perception of TCM remains controversial. We used the theory of planned behavior (TPB) to identify factors that affect the intention to use TCM.@*METHODS@#A cross-sectional web-based survey of 10,824 individuals from the general public was conducted between March 16 and April 2, 2020. The participants were recruited using a snowball sampling method. Data were collected using a self-administered questionnaire, based on the TPB. The questionnaire consisted of demographic characteristics and TPB structures. Structural equation modeling was used to identify predictors of intention.@*RESULTS@#The results indicated the model explained 77.5% and 71.9% of intention and attitude variance. Intention to use TCM had the strongest relationship with attitude (P < 0.001), followed by past behavior (P < 0.001), subjective norms (P < 0.001) and perceived behavioral control (P < 0.001). Attitudes toward TCM were significantly affected by perceived behavioral control (P < 0.001), subjective norms (P < 0.001) and cognition of TCM (P < 0.001).@*CONCLUSION@#Attitude is a key factor in determining the intention to use TCM, followed by past behaviors, subjective norms and perceived behavioral control. Our results offer important implications for health policy makers to promote the use of TCM.


Subject(s)
Adult , Attitude , COVID-19/psychology , Cross-Sectional Studies , Female , Humans , Intention , Male , Medicine, Chinese Traditional , Middle Aged , Psychological Theory , SARS-CoV-2
11.
Article in Chinese | WPRIM | ID: wpr-873836

ABSTRACT

Objective To analyze functional antibody and protection effect against pneumonia after inoculation with 23-valent pneumococcal polysaccharide vaccine(PPV23)in healthy elderly. Methods In 2015, 48 healthy elderly people aged ≥60 years were randomly selected in Hongkou District of Shanghai, and their blood samples were collected before, and 1 month and 6 months after the inoculation of PPV23.Functional antibodies against 13 serotypes(1、3、4、5、6A、6B、7F、9V、14、18C、19A、19F、23F)of streptococcus pneumonia were determined by muti-specificity opsonophagocyitosis killing assay(MOPA).The incidence of community-acquired pneumonia(CAP)after PPV23 inoculation was also investigated. Results The GMT of OPA antibodies against 13 serotypes were higher 1 and 6 months after inoculation than that before inoculation.One month after the inoculation, OPA antibodies against 13 serotypes ≥2 times growth rate and ≥4 times growth rate were 64.58%-87.00% and 43.75%-75.00%, respectively.Six months after inoculation with PPV23, OPA antibodies against 13 serotypes ≥2 times growth rate and ≥4 times growth rate were 45.71%-82.86%, 40.00%-80.00%, respectively.There was no significant difference in the growth rate of OPA antibody between 6 months and 1 month after vaccination for most serotypes.Results of self-descriptive survey before and after the inoculation showed that the protection against CAP in healthy elderly people in the first and second years after PPV23 inoculation was 100.00% and 50.00%, respectively. Conclusion PPV23 has better immunogenicity and immune persistence after inoculation in healthy elderly people, and has better protective effect against CAP.

12.
Article in Chinese | WPRIM | ID: wpr-905368

ABSTRACT

Objective:To investigate the effects of a one-way tracheostomy speaking valve based on neuromuscular electrical stimulation on aspiration in patients with dysphagia after tracheotomy for cerebral hemorrhage. Methods:From January to December, 2018, 37 patients with dysphagia after tracheotomy for cerebral hemorrhage were randomly divided into control group (n = 21) and experimental group (n = 16). Both groups accepted neuromuscular electrical stimulation, while the experimental group was trained to use one-way tracheostomy speaking valve additionally, for three weeks. They were assessed with Functional Oral Food Intake Scale (FOIS) and Penetration-Aspiration Scale (PAS) before and after treatment. Results:The scores of FOIS and PAS improved in both groups after treatment (|Z| > 3.544, P < 0.001), and was better in the experimental group than in the control group (|Z| > 2.094, P < 0.05). Conclusion:One-way tracheostomy speaking valve training based on neuromuscular electrical stimulation could improve swallowing and reduce aspiration of patients with dysphagia after tracheotomy.

13.
Article in English | WPRIM | ID: wpr-898146

ABSTRACT

Background@#Data on the effects of excess aldosterone on glucose metabolism are inconsistent. This study compared the changes in glucose metabolism in patients with primary aldosteronism (PA) after adrenalectomy or treatment with a mineralocorticoid receptor antagonist (MRA). @*Methods@#Overall, 241 patients were enrolled; 153 underwent adrenalectomy and 88 received an MRA. Fasting glucose, homeostatic model assessment of insulin resistance (HOMA-IR), and homeostatic model assessment of β-cell function (HOMA-β) were compared between the treatment groups after 1 year. Plasma aldosterone concentration (PAC) and factors determining HOMA-IR and PAC were evaluated. @*Results@#No baseline differences were observed between the groups. Fasting insulin, HOMA-IR, and HOMA-β increased in both groups and there were no significant differences in fasting glucose following treatment. Multiple regression analysis showed associations between PAC and HOMA-IR (β=0.172, P=0.017) after treatment. Treatment with spironolactone was the only risk factor associated with PAC >30 ng/dL (odds ratio, 5.2; 95% confidence interval [CI], 2.7 to 10; P<0.001) and conferred a 2.48-fold risk of insulin resistance after 1 year compared with surgery (95% CI, 1.3 to 4.8; P=0.007). @*Conclusion@#Spironolactone treatment might increase insulin resistance in patients with PA. This strengthened the current recommendation that adrenalectomy is the preferred strategy for patient with positive lateralization test. Achieving a post-treatment PAC of <30 ng/dL for improved insulin sensitivity may be appropriate.

14.
Article in English | WPRIM | ID: wpr-890442

ABSTRACT

Background@#Data on the effects of excess aldosterone on glucose metabolism are inconsistent. This study compared the changes in glucose metabolism in patients with primary aldosteronism (PA) after adrenalectomy or treatment with a mineralocorticoid receptor antagonist (MRA). @*Methods@#Overall, 241 patients were enrolled; 153 underwent adrenalectomy and 88 received an MRA. Fasting glucose, homeostatic model assessment of insulin resistance (HOMA-IR), and homeostatic model assessment of β-cell function (HOMA-β) were compared between the treatment groups after 1 year. Plasma aldosterone concentration (PAC) and factors determining HOMA-IR and PAC were evaluated. @*Results@#No baseline differences were observed between the groups. Fasting insulin, HOMA-IR, and HOMA-β increased in both groups and there were no significant differences in fasting glucose following treatment. Multiple regression analysis showed associations between PAC and HOMA-IR (β=0.172, P=0.017) after treatment. Treatment with spironolactone was the only risk factor associated with PAC >30 ng/dL (odds ratio, 5.2; 95% confidence interval [CI], 2.7 to 10; P<0.001) and conferred a 2.48-fold risk of insulin resistance after 1 year compared with surgery (95% CI, 1.3 to 4.8; P=0.007). @*Conclusion@#Spironolactone treatment might increase insulin resistance in patients with PA. This strengthened the current recommendation that adrenalectomy is the preferred strategy for patient with positive lateralization test. Achieving a post-treatment PAC of <30 ng/dL for improved insulin sensitivity may be appropriate.

15.
Acta Pharmaceutica Sinica ; (12): 922-929, 2020.
Article in Chinese | WPRIM | ID: wpr-821692

ABSTRACT

Schisandrol B (SolB) is one of the active constituents from a traditional Chinese medicine Schisandra chinensis or Schisandra sphenanthera. Our previous studies found that SolB exerts hepatoprotective effects against drug-induced liver injury and promotes liver regeneration. We further found that SolB significantly induces liver enlargement but the mechanisms remain unclear. The purpose of this study was to investigate the change of lipidome in liver tissues during SolB-induced hepatomegaly. The animal experiment protocol was approved by the Institutional Animal Care and Use Committee at Sun Yat-sen University. Serum and liver samples of male C57BL/6 mice were collected after intraperitoneal injection of SolB (100 mg·kg-1·d-1) for 5 days. Lipidomics analysis was performed using Q Exactive UHPLC-MS/MS system. The results showed that SolB significantly promoted liver enlargement in mice without liver injury and inflammation. Lipid accumulation was observed in the liver tissues after SolB treatment. Thirty-five lipids were identified with significant change and triglycerides (TG) were found to have the most significant increase in SolB-treated group, indicating the increase of energy production during SolB-induced hepatomegaly. This study reveals the impact of SolB on lipid metabolism and provides a potential explanation for liver enlargement induced by SolB.

16.
Article in Chinese | WPRIM | ID: wpr-821031

ABSTRACT

@#The metabolic reprogramming in cancer cells has recently attracted more and more attention from researchers. Lipid metabolism is involved in many cell processes such as cell growth, apoptosis, exercise, membrane homeostasis, chemotherapy response and drug resistance. This article summerizes the advances in research on fatty acids, cholesterol and phospholipid metabolism in non-small cell lung cancer, which may provide new ideas for the prevention, early diagnosis and treatment of non-small cell lung cancer.

17.
Acta Pharmaceutica Sinica ; (12): 1062-1068, 2019.
Article in Chinese | WPRIM | ID: wpr-780186

ABSTRACT

Cyclophosphamide (CPA) is one of the most commonly used alkylating agents in the treatment of malignant cancer. CPA is metabolized by cytochrome P450 enzymes into 4-hydroxycyclophosphamide in vivo which can exhibit anti-tumor activity. Metabolic activation of CPA can cause adverse reactions such as myelosuppression, cystitis, and liver injury. The aim of this study was to evaluate the dynamic changes of hepatic injury induced by CPA in mice. Male BALB/c mice were injected CPA (200 mg·kg-1) intraperitoneally. Both serum and liver samples were collected at 0, 2, 6, 12 and 24 hours after dosing. The animal experiment protocol was approved by the Institutional Animal Care and Use Committee at Sun Yat-sen University. The results showed that hepatotoxicity was observed at 2 hours after CPA dosing, and the most serious liver injury was measured at 12 hours. The level of serum aspartate aminotransferase (AST), alanine aminotransferase (ALT) and malondialdehyde (MDA) was significantly increased, glutathione (GSH) level was significantly decreased, hepatocyte edema and vacuolar degeneration were widely observed in liver tissue, and began to recover 24 hours after dosing. In addition, due to oxidative stress damage caused by CPA, nuclear factor-erythroid 2-related factor 2 (NRF2) signaling pathway was activated and the mRNA and protein expression of its downstream targets such as quinine oxidoreductase 1 (NQO1), heme oxygenase-1 (HO-1), glutamate-cysteine ligase catalytic subunit (GCLC) and glutamate cysteine modifier subunit (GCLM) were up-regulated, which alleviated oxidative stress injury. In a summary, this study demonstrate the dynamic change of CPA-induced liver injury and the NRF2-mediated protective mechanisms, providing new insights into the CPA-induced liver injury.

18.
Acta Pharmaceutica Sinica ; (12): 963-970, 2019.
Article in Chinese | WPRIM | ID: wpr-780180

ABSTRACT

This paper summarizes research progresses of Chinese scholars in the field of drug metabolism and pharmacokinetics (DMPK) in 2018. Chinese scholars focused on drug metabolizing enzymes and transporters, and carried out studies on the mechanisms of drug metabolism and transport of active molecules. Topics of research included regulatory mechanisms of drug metabolizing enzymes or transporters, and their implications in drug development and disease etiology or progression. Here, we summarized studies on drug toxicity based on drug metabolism or transport, rational drug use in the clinic, drug metabolism mediated by intestinal flora, metabolism of traditional Chinese medicines, and new technologies or models in DMPK. In recent years, the research focus of drug metabolism in China has transformed from serving for new drug discovery and rational use, to innovation driven and mechanism oriented research. The domestic research topics and technology utilization are gradually aligning with the international conventions.

19.
Journal of Medical Postgraduates ; (12): 1259-1263, 2019.
Article in Chinese | WPRIM | ID: wpr-818179

ABSTRACT

Objective Lipoxin A4 (LXA4) has been proved to have a good protective effect on spinal cord ischemia-reperfusion injury in rats, but whether autophagy is one of the protective mechanisms remains unclear. This study aims to investigate the effects of lipoxin A4 on rat spinal cord ischemia-reperfusion injury. Methods 48 rats were randomly divided into LXA4 group, ischemia-reperfusion group (SCII group) and sham group with 16 rats in each, and the models of each group were built accordingly. The rats in LXA4 group received intrathecal injection of 10μl LXA4 (300 pmol) 30 minutes after clamping the abdominal aorta. Three groups of rats were sacrificed by cervical dislocation 24 hours after reperfusion and the apoptosis-positive cells were then obtained. The spinal cord tissues of three groups of rats were stained and counted by LC3B fluorescence staining, and the expressions of LC3-II/LC3-I and GABARAP protein were detected by Western blot. Results There were few LC3B positive cells in the sham group. Compared to those in the sham group (73.40±19.42), the number of LC3B positive cells in SCII group (399.80±18.46) and LXA4 group (240.80±12.76) significantly increased (P<0.05), and the number in LXA4 group was significantly lower than that in SCII group (P<0.05). The ratio of LC3-II/LC3-I and the expression of GABARAP in SCII group and LXA4 group was significantly higher than those in sham group (P<0.05). The ratio of LC3-II/LC3-I in spinal cord tissue significantly declined compared with that of SCII group (P<0.05). Conclusion The autophagy is activated when SCII occurs, indicating that the autophagy is involved in SCII. After LXA4 is administered, autophagy is inhibited and SCII is alleviated.

20.
Article in Chinese | WPRIM | ID: wpr-802039

ABSTRACT

Objective:To observe the clinical efficacy of Shugan granule on perimenopausal depressive disorder (stagnation of liver Qi and Qi stagnation) and its effect on sex hormone and inflammatory factors. Method:One hundred and twenty patients were randomly divided into control group (60 cases) and observation group (60 cases) by random number table. Both groups got Tibolone tablets, 2.5 mg/time, 1 time/day. Patients in control group got flupentixol and melitracen tablets once every morning and noon, 1 tablet/time. In addition to the therapy of control group, patients in observation group got Shugan granule, 1 pack/time, 2 times/days. And a course of treatment was 8 weeks. Main indexes were graded by Hamilton depression scale (HAMD-17), self-rating depression scale (SDS) and Eysenck Personality Questionnaire (EPQ). And secondary indexes were scored by self-rating anxiety scale (SAS), stagnation of liver Qi and Qi stagnation, improved kupperman (KI), levels of follicle stimulating hormone (FSH), luteinizing hormone (LH), estradiol (E2), 5-serotonin (5-HT), brain derived neurotrophic factor (BDNF), interleukin-1β (IL-1β), IL-6 and tumor necrosis factor-α (TNF-α) before and after treatment. Result:By rank sum test, the clinical efficacy on depressed and perimenopausal syndrome in observation groups was better than that in control group (Z=2.038, PZ=2.316, PPPβ, IL-6 and TNF-α were lower than those in control groups (P2, BDNF and 5-HT were higher than those in control groups (PConclusion:Shugan granule can relieve depression, inquietude and symptoms caused by perimenopausal syndrome, regulate sex hormone, 5-HT, BDNF and inflammatory reaction, with a better clinical effect than pure western medicine treatment.

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