1.Preparation of baicalin-berberine complex nanocrystal enteric microspheres and pharmacodynamic evaluation of ulcerative colitis treatment in rats.
Xiao-Chao HUANG ; Yi-Wen HU ; Peng-Yu SHEN ; Rui-Hong JIAN ; Dong-Li QI ; Zhi-Dong LIU ; Jia-Xin PI
China Journal of Chinese Materia Medica 2025;50(15):4263-4274
To enhance the therapeutic efficacy of the baicalin-berberine complex(BA-BBR) in the treatment of ulcerative colitis(UC), BA-BBR nanocrystal microspheres(BA-BBR NC MS) were prepared using the dropping method. The microspheres were characterized in terms of morphology, particle size, differential scanning calorimetry(DSC), and powder X-ray diffraction(XRD). The release profiles of BA and BBR from the microspheres were measured, and the drug release mechanism was investigated. A rat model of UC was induced by 5% dextran sodium sulfate(DSS) and treated continuously for 7 days to evaluate the therapeutic effects of different formulations. The results showed that the prepared BA-BBR MS and BA-BBR NC MS were uniform gel spheres with particle sizes of(1.77±0.16) mm and(1.67±0.08) mm, respectively. After drying, the gels collapsed inward and exhibited a rough surface. During the preparation process, the BA-BBR nanocrystals(BA-BBR NC) were uniformly encapsulated within the microspheres. The release profiles of the microspheres followed a first-order kinetic model, and the 12-hour cumulative release of BA and BBR from BA-BBR NC MS was higher than that from BA-BBR MS. Compared with BA-BBR, BA-BBR NC, and BA-BBR MS, BA-BBR NC MS further alleviated UC symptoms in rats, most significantly reducing the levels of TNF-α, IL-1β, IL-6, and MPO, while increasing the level of IL-4 in colon tissues. These results indicate that BA-BBR NC MS, based on a "nano-in-micro" design, can deliver BA-BBR to the intestine and exert significant therapeutic effects in a UC rat model, suggesting it as a promising new strategy for the treatment of UC.
Animals
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Colitis, Ulcerative/metabolism*
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Rats
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Nanoparticles/chemistry*
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Microspheres
;
Male
;
Berberine/administration & dosage*
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Flavonoids/administration & dosage*
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Rats, Sprague-Dawley
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Drugs, Chinese Herbal/administration & dosage*
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Humans
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Particle Size
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Tumor Necrosis Factor-alpha/immunology*
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Drug Liberation
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Drug Compounding
2. Effects of berberine on colon dermal cell apoptosis in mice with ulcerative colitis based on JAK/STAT signaling pathway
Chun-Lin LI ; Pi-Xian SHUI ; Shi-Chao LI ; Ying-Tian JIA ; Jian LI ; Kun-Peng ZHAO
Chinese Pharmacological Bulletin 2023;39(5):938-945
Aim To analyze the effects of berberine on the apoptosis of colon epithelial cells and polymorpho-nuclear neutrophils ( PMNs) in mice with ulcerative colitis ( UC ) by regulating JAK/STAT signaling pathway. Methods The UC mouse models were established by dextran sulfate sodium ( DSS) method and were randomly divided into control group, UC group, low-dose, middle-dose and high-dose berberine groups and positive drug group ( mesalazine enteric-coated tablet group) . In addition, the mice were randomly di¬vided into UC group, high-dose berberine group, AG490 group, and high-dose berberine + AG490 group. Levels of serum tumor necrosis factor a (TNF-α) and interleukin 6 (IL-6) and colon epithelial cell apoptosis and PMN apoptosis were compared among the groups. Western blot was used to detect the expres¬sions of colon tissue apoptosis-related and JAK/STAT signaling pathway-related proteins. Results The lev¬els of serum TNF-α and IL-6, apoptosis rate of colon epithelial cell and protein expressions of Fas, FasL, Bax, caspase-3, p-JAK2/JAK2 and p-STAT3/STAT3 in each dose berberine group and positive drug group were significantly lower than those in UC group (P < 0.05), and the above indicators in berberine groups were reduced gradually (P <0.05) . The PMN apoptosis rate and Bcl-2 protein expression were significantly higher in each dose berberine group and positive drug group than those in UC group (P <0. 05) , and the two indicators increased gradually in berberine groups ( P < 0.05). AG490 could reverse the above effects of berberine ( P < 0. 05 ). Conclusions Berberine can inhibit the apoptosis of colon epithelial cell and promote the apoptosis of PMN in UC mice by regulating the JAK/STAT signaling pathway, and then play a role in the treatment of UC.
3.Cesarean section under spinal anesthesia seven years after heart-lung transplantation: a case report
Ting LUO ; Weisi LAI ; Pixiang PI ; Junmei XU ; Hong ZHENG ; Jian HUANG ; Mei PENG
Chinese Journal of Perinatal Medicine 2022;25(9):694-696
This article reported a successful cesarean section performed on a woman with 37 +6 weeks of gestation after heart-lung transplantation (HLTx) at the Second Xiangya Hospital of Central South University. The patient was a 29-year-old woman with singleton pregnancy who underwent HLTx seven years ago. During pregnancy, she was treated with azathioprine and tacrolimus to suppress immune rejection. The patient was in New York Heart Association (NYHA) class Ⅰ and had no fever or shortness of breath. Prenatal examinations indicated that the mother and the fetus were in good condition. A baby girl was delivered successfully at full term by a transverse lower-segment cesarean section under spinal anesthesia. Both the mother and the child were healthy at follow-up of 42 d after discharge.
4.Identification of critical influencing factors in dropping process of Xuesaitong Dropping Pills.
Yi-Zhe HOU ; Pian LI ; Jian ZHANG ; Jing-Li CHEN ; Pei-Pei PI ; Zheng LI ; Wen-Long LI
China Journal of Chinese Materia Medica 2021;46(1):103-109
With the dropping process of Xuesaitong Dropping Pills(XDP) as the study object, critical factors affecting the quality indicators of pill pass rate, average weight of drop pills and roundness were screened out, so as to deepen the understanding of the dropping process. The critical process units, critical quality attributes and potential critical process influencing factors of XDP were determined by risk analysis and prior knowledge, and then the critical influencing factors were screened out by Plackett-Burman design. First, according to the risk assessment, the critical technique of XDP preparation process was dropping, and then the critical quality attributes of dropping process were pill pass rate, average weight of drop pills and roundness. Then, according to fishbone diagram and failure mode and effects analysis(FMEA), potential critical influencing factors were determined as flow rate, matrix ratio, solid-liquid ratio, feed-liquid temperature, top temperature of condensate, bottom temperature of condensate and dropping distance. Finally, among these seven potential factors, the critical influencing factors were determined as material liquid ratio, dropping distance, top temperature of condensate, bottom temperature of condensate. This study revealed the potential of Plackett-Burman design in screening and understanding the influence of selected factors on XDP dropping process, which could provide a reference for studying the dropping process.
Drugs, Chinese Herbal
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Saponins
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Temperature
5.Effect of Shenshuai Xiezhuo Decoction and Its Deficiency Tonifying and Pathogen Eliminating Components on Renal Interstitial Fibrosis in UUO rats
Zi-you YAN ; Jian-qing JIANG ; Fu-li LUO ; Chi-heng PI
Chinese Journal of Experimental Traditional Medical Formulae 2020;26(16):71-78
Objective:To study the effect of Shenshuai Xiezhuo decoction and its deficiency tonifying and pathogen eliminating components on renal interstitial fibrosis in UUO rats. Method:A rat model of unilateral ureteral obstruction (UUO) was established through ligation of a unilateral ureter. The rats were divided into six groups: sham operation group, model group, benazepril group, Shenshuai Xiezhuo decoction group, Buxufang group, and phlegm group, with 24 rats in each group. On the third day after operation, the rats in the Shenshuai Xiezhuo decoction group, Buxufang group, and phlegm group were given Shenshuai Xiezhuo decoction concentrating agent at a dose of 8.0 g·kg-1·d-1, the rats in the benazepril group were given benazepril 1.5 mg·kg-1·d-1, and the rats in the sham operation group and the model group were given the same volume of saline. On the 7th, 14th and 21st days after operation, the expressions of peripheral cells and relevant signal pathway markers in renal tissue were detected by Western blot and Real-time fluorescent quantitative polymerase chain reaction (Real-time PCR) respectively. Result:The stromal damage score and the interstitial collagen accumulation on the 14th and 21st days after UUO were significantly lower in the Shenshuai Xiezhuo decoction group, Buxu prescription group and Qixie prescription group than those in the model group (
6.Mechanism of traditional Chinese medicine balancing Yin-Yang by targeting ERα/ERβ and its application in treatment of menopausal syndrome.
Pi-Wen ZHAO ; Yan-Xia WANG ; Jian-Zhao NIU
China Journal of Chinese Materia Medica 2020;45(16):3770-3775
The coordination and unification of Yin and Yang are the basis of normal human life activities. Along with the age growth and aging of the body, women will suffer from menopausal syndrome during menopause. In addition to the significant changes in the genital system, there are also pathological manifestations in estrogen target points including bone, nerve and cardiovascular systems, due to the imbalance of Yin and Yang. Besides the insufficiency of estrogen, the main cause of menopausal syndrome is the changes in the response of target organs to estrogen. In other words, the biological effects mediated by estrogen receptor(ER) alpha and beta subtypes in target cells are often different or even opposite; the changes of expression level and ratio of ERα and ERβ are also important causes for the abnormal estrogenic effects in target organs and the imbalance of Yin and Yang of the body. Therefore, on one hand, the therapeutic mechanism of drugs is ER-mediated estrogenic effect. On the other hand, the drugs have a regulatory effect on ER subtype expression in target cells and Yin-Yang state in target organs and even organisms, so as to cause further changes in the response of target cells to estrogen or estrogenic components, and exert its therapeutic effects. This paper reviews the pharmacological mechanism of gynecological traditional Chinese medicine in harmonizing Yin and Yang in estrogen-positive target cells and the clinical efficacy in the following aspects, including estrogen and its mechanism, the estrogenic effect of ER in traditional Chinese medicine and the mechanism of ER subtype in balancing Yin and Yang and mediating and regulating the main target tissues in menopausal syndrome treatment.
Estrogen Receptor alpha
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Estrogen Receptor beta
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Estrogens
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Female
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Humans
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Medicine, Chinese Traditional
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Yin-Yang
7.18F-FDG PET/CT images quality and its impact factors in diabetic and non-diabetic patients with coronary artery disease
Ziwei ZHU ; Zhi CHANG ; Xiaopeng SHI ; Xiaofen XIE ; Quan LI ; Jingjing MENG ; Yingfei PI ; Xue CAO ; Jian JIAO ; Xia LU ; Yingsheng ZHOU ; Xiaoli ZHANG
Chinese Journal of Nuclear Medicine and Molecular Imaging 2020;40(5):281-287
Objective:To evaluate the image quality (IQ) of 18F-fluorodeoxyglucose (FDG) PET/CT imaging and identify its influenfial factors in diabetes mellitus (DM) and non-DM patients with coronary artery disease (CAD). Methods:A total of 196 consecutive CAD patients (174 males, 22 females, 68 DM; age: (57±10) years) in Beijing Anzhen Hospital between June 2016 and February 2018 were retrospectively analyzed. All patients underwent 18F-FDG myocardial PET/CT imaging. The standardized fasting+ oral glucose loading (OGL) and intravenously injection of insulin protocol was performed. According to the FDG uptake by myocardium, background activity in blood and other visceral organ nearby the heart, the IQ was visually evaluated and scored by 0-4. Zero-two was considered as good IQ, 3-4 was regarded as poor IQ. Patients were divided into three groups: group 1 (non-DM+ good IQ), group 2 (DM+ good IQ), group 3 (DM+ poor IQ). Factors which may affect IQ were analyzed, which including OGL, the injection dose of insulin, fasting blood glucose (FBG), peak blood glucose (PBG), blood glucose (BG) level at 18F-FDG injection (BG injnection), BG increasing rate ((PBG-FBG)/FBG, %), and BG decreasing rate ((PBG-BG injection)/PBG, %). One-way analysis of variance, Spearman correlation analysis and logistic regression analysis were used for data analysis. Results:There were significant differences ( F values: 13.074-38.371, all P<0.05) of FBG, PBG, OGL, BG decreasing rate and the injection dose of insulin among group 1 ( n=132, 67.3%), group 2 ( n=53, 27.1%), group 3 ( n=11, 5.6%). All those parameters, except for OGL, were positively correlated with FDG PET/CT IQ ( r s values: 0.142-0.262, all P<0.05). OGL was negatively correlated with IQ ( r s=-0.324, P<0.05). Logistic regression analysis showed that FBG (odds ratio ( OR)=0.687, 95% CI: 0.633-0.746), PBG( OR=0.786, 95% CI: 0.746~0.829), BG injection( OR=0.631, 95% CI: 0.595-0.716), OGL( OR=0.897, 95% CI: 0.873-0.922), the injection dose of insulin( OR=0.680, 95% CI: 0.618-0.748) were predictive factors (all P<0.01) for good IQ in all patients. For DM patients, OGL was the only predictive factor for good IQ( OR =0.940, 95% CI: 0.904-0.960; P<0.01). Conclusions:FBG, PBG, BG injection, OGL, the injection dose of insulin can predict IQ for all patients with CAD. For DM patients with CAD, OGL is the only predictive factor for good IQ. A good IQ of 18F-FDG PET/CT could be obtained in majority of CAD patients, with the standardized fasting + OGL and intravenously injection of insulin protocol and adjust according to the personal status, and prevent the hypoglycemia from happening.
8.Virulence of Serovar Enteritidis Isolate LN-248-0 and Immune Responses in BALB/c Mice.
Yang LIU ; You Zhi LI ; Tao FENG ; Pi Qian GONG ; Ying Cai JIN ; Hong Wei ZHU ; Lin Lin JIANG ; Jian Long ZHANG ; Guo Zhong CHEN ; Xin YU ; Xing Xiao ZHANG
Biomedical and Environmental Sciences 2020;33(8):628-632
9.Molecular mechanism of apoptosis of breast cancer SKBR-3 cells induced by cryptanshinone via G protein coupled estrogen receptor( GPER) mediated pathway.
Dan-Ning SHI ; Li-Xia CUI ; Pi-Wen ZHAO ; Li-Ping SUN ; Meng CHEN ; Jian-Zhao NIU
China Journal of Chinese Materia Medica 2019;44(22):4905-4911
The study aimed to illuminate the role of G protein coupled estrogen receptor( GPER) and its mediated PI3 K/AKT signaling pathway in cryptotanshinone( CPT) induced apoptosis of breast cancer SKBR-3 cells,which is GPER positive and ER negative.The apoptosis rate of SKBR-3 cells was tested by Annexin V-FITC/PI staining and apoptosis effector caspase-3 was determined by Western blot. The key proteins in PI3 K/AKT signaling pathway mediated by GPER were detected by Western blot and immunofluorescence technique. Meanwhile,the agonist G1 and antagonist G15 of GPER and antagonist LY294002 of PI3 K were employed in the test to further clarify the effect of GPER and PI3 K/AKT pathway. The results indicated that the apoptosis rate was increased from 4. 7% to46. 1% and 69. 0% after treatment with 0,5,10 μmol·L~(-1) CPT for 48 h( P<0. 01). The expression of PI3 K,AKT and p-AKT were inhibited( P<0. 05 or P<0. 01),while caspase-3 level increased obviously after treatment with CPT( P<0. 01). Importantly,inhibitory effect of PI3 K/AKT signaling pathway by CPT was further enhanced by G1 and attenuated by G15. LY294002 also induced a further inhibition of expression of AKT and p-AKT. The mean fluorescence intensity of AKT and p-AKT could be decreased by CPT. Furthermore,CPT could downregulate GPER expression in SKBR-3 cells( P<0. 01),which could be inhibited by G1 and enhanced by G15.In conclusion,CPT could induce the apoptosis of ER negative and GPER positive breast cancer SKBR-3 cells and the molecular mechanism is related to its regulatory effect of GPER and its mediated PI3 K/AKT signaling pathway.
Apoptosis
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Breast Neoplasms
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Drugs, Chinese Herbal
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Humans
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Proto-Oncogene Proteins c-akt
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Receptors, Estrogen
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Receptors, G-Protein-Coupled
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Signal Transduction
10.The relationship between Beclin 1 expression and lymph node metastasis in non-small cell lung cancer
XIONG Jian ; WU Lei ; PI Yuyang ; XU Yongdong
Chinese Journal of Clinical Thoracic and Cardiovascular Surgery 2019;26(10):984-987
Objective To explore the relationship between Beclin 1 level and lymph node metastasis in patients with non-small cell lung cancer. Method A total of 204 surgical specimens of patients with non-small cell lung cancer from September 2011 to September 2016 were collected in our hospital. There were 116 males and 88 females . Beclin 1 levels were detected by Western blotting. There were 116 males and 88 females at average age of 55.3±11.2 years. The patients were divided into three groups including a group N0 (no lymph node metastasis), a group N1(intralobar and interlobar lymph node metastases, and no mediastinal lymph node metastasis), and a group N2 (mediastinal lymph node metastasis). The differences of Beclin 1 levels in tumor tissues and lymph nodes of patients with N0, N1 and N2 were statistically analyzed. Results Among 204 patients of lung cancer, 36 patients were squamous cell carcinoma and 168 patients were adenocarcinoma. The levels of Beclin 1 in tumor tissues of N0, N1 and N2 groups decreased gradually with a statistical difference (P<0.05). In the three groups, the levels of Beclin 1 in the lung hilum and intrapulmonary lymph nodes (N1 Beclin 1) of N1 and N2 groups were less than that of N0 group with a statistical difference (P<0.01). In the three groups, the level of Beclin 1 in the mediastinal lymph nodes (N2 Beclin 1) of N2 group was less than that of the N0 and N1 groups with a statistical difference (P<0.01). In the N1 group, the level of N1 Beclin 1 was less than that of N2 group (P<0.01). In the N2 group, though the level of N1 Beclin 1 was less than N2 Beclin 1, there was no statistical difference (P>0.05). Conclusion Beclin 1 level can be used as a reference index to judge the benign and malignant lung masses, and lymph node Beclin 1 level can be used as an important reference index to help determine whether there is lymph node metastasis in lung cancer.

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