1.Preventive and Therapeutic Effect of Wenshen Xiaochuan Paste Recipe for Bronchial Asthma and Its Influence on Immune Indexes
Yingjie LI ; Ping HUI ; Tianyun SONG ; Zhaonan CHEN ; Facai FAN
Journal of Guangzhou University of Traditional Chinese Medicine 2015;(5):813-816
Objective To observe the clinical efficacy of Wenshen Xiaochuan Paste Recipe (WXPR) in preventing bronchial asthma, and to explore the mechanism. Methods Eighty patients were randomly divided into treatment group and control group. Each group had 40 patients. The control group was treated by conventional western medicine such as inhalation of steroid, and the treatment group was given oral use of WXPR based on the treatment for the control group. Treatment for both groups covered 60 days, and the follow-up lasted 10 months. The clinical outcomes included the clinical efficacy and immune indexes of peripheral blood T lymphocyte subsets CD3+, CD4+, CD8+and CD4+/CD8+ratio, and the serum IgE level. Results (1) After treatment and 12 months later, the scores of asthma control test (ACT ) in the two groups were increased obviously as compared with those before treatment, and there were statistically significant differences (P<0.05 or P<0.01) . The differences of ACT scores between the two groups were insignificant after treatment ( P>0.05) , but were significant ( P<0.05) 12 months later. (2) Within one year after treatment, the frequency of acute asthma attack was decreased in both groups (P<0.05 compared with that before treatment), and the treatment group had better effect on decreasing the attack frequency than the control group (P<0.05). (3) After treatment, the serum IgE, CD4+level, and CD4+/CD8+ ratio were decreased significantly, while CD8+ level was increased in the treatment group, and there were statistically significant differences ( P<0.05 compared with those before treatment). However, the differences of immune indexes in the control group were insignificant before and after treatment ( P>0.05). The improvement of immune indexes in the treatment group was superior to that in the control group ( P<0.05). Conclusion WXPR has good clinical efficacy in preventing and treating bronchial asthma. The mechanism is related with the inhibition of airway inflammation and improvement of immune function probably through regulating T lymphocyte subsets and lowering serum IgE level in asthma patients.
2.In vitro study on anti-HBV effects and mechanism of hypericin
Tianyun LAN ; Hong FAN ; Yongbin CHEN ; Cuiping YANG ; Xingwang ZHAO ; Yan LI
Chongqing Medicine 2017;46(1):40-43,47
Objective To evaluate the anti-HBV effect of hypericin from the cellular level and to preliminarily explore its po-tential drug target point.Methods Liver cell line HepG2.2.15 cells secreting HBV particles were selected as the experimental ob-jects.Hypericin served as the HY group,lamivudine was taken as 3TC group and deionized water as the blank control group.The cells were grouped and administrated.The HBV-DNA copy level was measured at72 h after medication by Southern blot and fluo-rescent quantitative PCR;the inhibition rate of HBsAg and HBeAg was detected by using ELISA assay;the pgRNA expression level was tested by using Northern blot and fluorescent quantitative PCR;Western blot and fluorescent quantitative PCR were adopted to detect the expression of regulatory factors including HNF3β,HNF4α,PPARαand RXRα.Results Compared to the blank control group,both hypericin and lamivudine had significant inhibiting effect on HBV DNA and expression level of HBsAg and HBeAg in HepG2.2.15 cells (P <0.05).Hypericin could significantly decrease the pgRNA expression compared with the blank control group (P <0.05),while lamivudine had no obvious change (P <0.05).Moreover,hypericin exhibited significant effects on the expression of HNF3βand regulatory factor HNF4αcompared with the blank control group and 3TC group(P <0.05).Conclusion Hypericin represents a strong anti-HBV effect,moreover could increase the negative regulatory factor HNF3βn expression and decreases the positive factor HNF4αexpression,prompting that its drug target point could be pgRNA.
3.The imaging features of osseous metastasis of hepatic alveolar hydatida
Tianyun LI ; Haining FAN ; Haihua BAO
Chinese Journal of Radiology 2018;52(3):209-212
Objective To investigate the CT and MR imaging feature of osseous metastasis of hepatic alveolar hydatida.Methods CT and MR imaging features of osseous metastasis of hepatic alveolar hydatid were retrospectively analyzed in 14 cases confirmed by clinic and radiology. Results Of the 10 vertebral metastasises,three vertebral bodies were involved in 6 cases,two adjacent vertebral bodies were involved in 2 cases, single vertebral body was involved in 1 case, corresponding vertebral accessory was involved in 9 cases,irregular mass was formed in paravertebral muscles with ill-defined margins in 9 cases, adjacent ribs were involved in 6 cases. On CT scans, the lesions of vertebral body showed osteolytic and geographical bone destruction with bone sclerosis. The lesions of vertebral accessory showed swelling and osteolytic bone destruction, small cystic density and calcification of cystic wall and irregular calcification were found in 7 cases.The lesions of scapula,costal cartilage,ribs and pelvis showed swelling and osteolytic bone destruction,and bone sclerosis,and revealed cystic density with calcified speckles.On MR scans,the lesions of vertebral body and paravertebral muscles showed high and low mixed signal,with hypointensity on T1WI and T2WI, vertebral accessory and adjacent ribs were involved in 6 cases. Small cyst with T2 hyperintensity was found in 4 cases. The lesions of ribs and pelvis showed swelling and osteolytic bone destruction and adjacent medullary appeared hypointensity on T1WI and T2WI, cystic signal of T2 hyperintensity was identified. There were 5 cases of pulmonary metastasis and 6 cases of retroperitoneal metastasis. Conclusion Imaging features of osteolytic,geographical bone destruction with bone sclerosis, small cystic density or cystic signal and calcified speckles or arc calcification in mass are helpful for the diagnosis of osseous metastasis of hepatic alveolar hydatid.
4.Effects of Different Landing Postures on Bone Mineral Density and Content During High-Impact Exercises
Yixue LUO ; Chenyu LUO ; Yuhui CAI ; Tianyun JIANG ; Yalin CUI ; Linzhen WANG ; Yubo FAN
Journal of Medical Biomechanics 2018;33(2):E168-E173
Objective To study effects of different types of high-impact exercises on the increment of bone mineral density (BMD) and bone mineral content (BMC) . Methods Thirty-nine male volunteers, including 13 hoopsters, 13 paratroopers, and 13 common college students as the control, were recruited and divided into two subgroups (subgroup 1:20-22 years old; subgroup 2:23-25 years old). Their BMDs and BMCs on calcaneus, first through fifth metatarsus, hip, and lumbar spine (L1-4) were evaluated. Results The BMC of calcaneus, the first and second metatarsals, total lumbar spine, and total hip in the hoopster group was significantly higher than that in the control group and paratrooper group. The hoopster group obtained statistically higher BMD at the lumbar spine, hip, and femoral neck than the other two groups. However, the BMCs and BMDs of the paratrooper group and control group had no significant differences at almost all measured anatomical locations. Conclusions BMC and BMD are not always in positive correlation with vertical ground reaction forces during normal exercises. Compared with parachuting training, playing basketball as a kind of variable load exercise can effectively increase BMC and BMD, and is more beneficial for reducing the risk of osteoporotic fracture.
5.Evaluation of Optimal Gravity Center Position of Backpack in Half-Squat Parachuting Landing
Tianyun JIANG ; Shan TIAN ; Tianhong CHEN ; Chenyu LUO ; Xingyu FAN ; Jie YAO ; Lizhen WANG
Journal of Medical Biomechanics 2021;36(6):E945-E950
Objective To study effects of backpack gravity center position on kinetics and kinematics of lower-extremity joints in parachuting landing and evaluate the injuries. Methods Seven participants performed parachuting landing with backpack gravity center on three positions: low-back (position 1), upper-back (position 2) and abdomen (position 3). Results The peak vertical ground reaction force (GRF) with backpack on position 2 was significantly lower than that on position 1. The joint moment on sagittal plane of the hip with backpack on position 2 was significantly higher than that on position 1 and position 3. The joint energy absorption of the hip with backpack on position 2 was significantly higher than that on position 1. The angular displacement of the hip on sagittal plane with backpack on position 2 was significantly higher than that on position 1 and was significantly lower than that on position 3. The angular velocity of the hip on sagittal plane with backpack on position 2 was significantly lower than that on position 3. Conclusions Different positions of backpack gravity center could significantly influence kinetic and kinematic parameters of the hip. Backpack gravity center on upper-back position could decrease the lower-extremity injuries. The results can provide evidences for evaluating backpack gravity center and decreasing injuries in parachuting landing.
6.Fracture Classification and Injury Segment Analysis of Tibiofibula and Ankle in Half-Squat Parachuting Landing
Chenyu LUO ; Shan TIAN ; Tianyun JIANG ; Songyang LIU ; Hao ZHANG ; Jiakang ZHANG ; Lizhen WANG ; Yubo FAN
Journal of Medical Biomechanics 2022;37(2):E268-E273
Objective To make classification and segment measurement for the cases with tibiofibular and ankle fractures in parachuting landing, and investigate main classification types of parachuting fractures and fracture segments of high risk.Methods A total of 56 fracture cases in parachuting landing were collected, and the tibiofibula and ankle fractures were classified according to AO-OTA or Lauge-Hansen classification standards respectively based on their digital X-ray images. The medium plane between talus and tibia joint planes in ankle joint was defined as the reference plane. The highest and lowest injury points of tibia and fibula were marked respectively, and the fracture segment was defined between the highest and lowest point for statistical analysis.Results For tibiofibular and ankle fracture cases in parachuting landing, fracture at both tibia and fibula accounted for 80.4%. The major classification of tibiofibula fracture was 42-D/5.2 (45.8%) and 42-D/5.1 (16.7%). The major classification for ankle fracture was pronation-external rotation (PER, 59.4%) and supination-external rotation (SER, 37.5%). When tibiofibular and ankle fracture cases in parachuting landing occurred, the fracture segment of the tibia was mainly from 57 to 143 mm above the reference plane and from 6 mm below the reference plane to 24 mm above the reference plane, while the fracture segment of the fibula was 4-45 mm and 74-83 mm above the reference plane. Injury risks of all above segments were higher than 50%.Conclusions For protection of lower limbs in parachuting landing, the fracture at both tibia and fibula should be highly noticed. The ankle motion of PER and SER should be especially restricted in parachuting ankle protection.
7.Discovery and identification of EIF2AK2 as a direct key target of berberine for anti-inflammatory effects.
Wei WEI ; Qingxuan ZENG ; Yan WANG ; Xixi GUO ; Tianyun FAN ; Yinghong LI ; Hongbin DENG ; Liping ZHAO ; Xintong ZHANG ; Yonghua LIU ; Yulong SHI ; Jingyang ZHU ; Xican MA ; Yanxiang WANG ; Jiandong JIANG ; Danqing SONG
Acta Pharmaceutica Sinica B 2023;13(5):2138-2151
Using chemoproteomic techniques, we first identified EIF2AK2, eEF1A1, PRDX3 and VPS4B as direct targets of berberine (BBR) for its synergistically anti-inflammatory effects. Of them, BBR has the strongest affinity with EIF2AK2 via two ionic bonds, and regulates several key inflammatory pathways through EIF2AK2, indicating the dominant role of EIF2AK2. Also, BBR could subtly inhibit the dimerization of EIF2AK2, rather than its enzyme activity, to selectively modulate its downstream pathways including JNK, NF-κB, AKT and NLRP3, with an advantage of good safety profile. In EIF2AK2 gene knockdown mice, the inhibitory IL-1β, IL-6, IL-18 and TNF-α secretion of BBR was obviously attenuated, confirming an EIF2AK2-dependent anti-inflammatory efficacy. The results highlight the BBR's network mechanism on anti-inflammatory effects in which EIF2AK2 is a key target, and inhibition of EIF2AK2 dimerization has a potential to be a therapeutic strategy against inflammation-related disorders.
8.Evolution and development of potent monobactam sulfonate candidate IMBZ18g as a dual inhibitor against MDR Gram-negative bacteria producing ESBLs.
Zhiwen LI ; Zhihao GUO ; Xi LU ; Xican MA ; Xiukun WANG ; Rui ZHANG ; Xinxin HU ; Yanxiang WANG ; Jing PANG ; Tianyun FAN ; Yonghua LIU ; Sheng TANG ; Haigen FU ; Jingpu ZHANG ; Yinghong LI ; Xuefu YOU ; Danqing SONG
Acta Pharmaceutica Sinica B 2023;13(7):3067-3079
A series of new monobactam sulfonates is continuously synthesized and evaluated for their antimicrobial efficacies against Gram-negative bacteria. Compound 33a (IMBZ18G) is highly effective in vitro and in vivo against clinically intractable multi-drug-resistant (MDR) Gram-negative strains, with a highly druglike nature. The checkerboard assay reveals its significant synergistic effect with β-lactamase inhibitor avibactam, and the MIC values against MDR enterobacteria were reduced up to 4-512 folds. X-ray co-crystal and chemoproteomic assays indicate that the anti-MDR bacteria effect of 33a results from the dual inhibition of the common PBP3 and some class A and C β-lactamases. Accordingly, preclinical studies of 33a alone and 33a‒avibactam combination as potential innovative candidates are actively going on, in the treatment of β-lactamase-producing MDR Gram-negative bacterial infections.