1.Kinase modulators approved by FDA in 2022
Acta Pharmaceutica Sinica 2024;58(1):61-75
The FDA approved a total of 37 new drugs in 2022, including 22 new molecular entities and 15 new biological products. This is the year with the lowest number of new drugs approved by the FDA since 2017. Among these approved drugs, 21 new drugs belong to the "first-in-class" category, accounting for 56% of the total approved drugs, which is the highest ratio in the past 10 years. Among the drugs approved in 2022, there are 5 small molecule kinase modulators, including the tyrosine kinase 2 (TYK2) allosteric inhibitor deucravacitinib, the first oral pyruvate kinase (PK) activator mitapivat, the Janus kinase 1 (JAK1) selective inhibitor abcrocitinib, the JAK2 selective inhibitor pacritinib and the broad-spectrum fibroblast growth factor receptor (FGFR) inhibitor futibatinib. This review briefly describes the discovery background, research and development process, synthesis routes and clinical efficacy and safety of small molecule kinase modulators approved by the FDA in 2022, hoping to provide ideas and methods for further research on kinase modulators.
2.Large-scale expansion of clinical-grade human adipose-derived stem cells using the extracellular matrix
Yuehan SU ; Chao WEI ; Pinlei LV ; Yun CAO ; Yun QIU ; Qing ZHENG ; Shudong XIAO ; Zheng WANG
Chinese Journal of Tissue Engineering Research 2014;(10):1521-1531
BACKGROUND:Large-scale expansion of undifferentiated and multipotential adipose-derived stem cells using serum-free culture system is a difficult issue to be resolved. OBJECTIVE:To establish an in vitro culture system combined with the extracellular matrix in order to investigate the efficiency, effectiveness and security of extracellular matrix on expanding adipose-derived stem cells. METHODS:In vitro isolated adipose-derived stem cells were seeded in traditional two-dimensional plastic plates and extracellular matrix-coated plates supplemented with serum-free medium respectively. After in vitro expansion, total cellnumber, expression of cellsurface markers, cellsenescence degree and multipotent differentiation ability (adipogenic, osteoblastic and chondrogenic differentiation) of adipose-derived stem cells cultured under both conditions were detected and compared. Moreover, the clinical safety of adipose-derived stem cells expanded in extracellular matrix-coated plates was investigated. RESULTS AND CONCLUSION:Total cellnumber of passage 5 adipose-derived stem cells cultured in extracellular matrix-coated plates was 10 times more than that in traditional two-dimensional plastic plates. Flow-cytometric analysis showed that adipose-derived stem cells cultured with extracellular matrix expressed stem cellsurface markers. cellular senescence examination showed that almost al of passage 15 adipose-derived stem cells cultured with extracellular matrix showed no aging, while most passage 5 adipose-derived stem cells cultured by the two-dimensional system aged and lost their proliferation ability. Multidirectional induction of adipose-derived stem cells showed that passage 15 adipose-derived stem cells cultured with extracellular matrix could stil differentiate into adipocytes, osteoblasts and chondrocytes as passage 5 adipose-derived stem cells did, which performed much better than the induced differentiations of passage 5 adipose-derived stem cells cultured by the two-dimensional system. Karyotype analysis and in vivo invasion experiment insured the clinical safety of adipose-derived stem cells expanded with extracellular matrix. Al above results suggest a safe and more efficient expansion system of extracellular matrix for clinical application using the serum-free culture system combined with extracellular matrix.
3.Efficacy observation of Guan's quadruple therapy for kidney disease on the treatment of chronic renal failure.
Zheng ZUO ; Xiao-Mei CHEN ; Yun-Wu JIANG ; Xiao-Yun TANG ; Zun-Xin GUAN
Chinese Acupuncture & Moxibustion 2014;34(7):641-645
OBJECTIVETo compare the differences in the clinical efficacy between Guan's quadruple therapy for kidney disease and the conventional western medication in the treatment of chronic renal failure (CRF).
METHODSEighty patients were randomized into an observation group and a control group, 40 cases in each one. In the observation group, besides the physician instruction of low protein and low phosphorus diet in the two groups, Guan's quadruple therapy for kidney disease was applied, including (1) the isolated herbal moxibustion at Shenshu (BL 23) and Pishu (BL 21), or Ganshu (BL 18), Zusanli (ST 36) and Guanyuan (CV 4) alternatively; (2) acupuncture at the auricular points such as shen (CO10), jiaogan (AHR6), Shenshangxian (TG2), fei (CO14) and pizhixia (AT4); (3) injection of mixture of astragalus injection and lidocaine injection at Feishu (BL 13), Pishu (BL 21), Shenshu (BL 23) and the others; (4) modified Shenshuai Yihao decoction according to syndrome differentiation. In the control group, the conventional western medication was used. After 6 months of treatment, the differences were observed between the two groups in the clinical efficacy, serum creatinine (Scr), blood urea nitrogen (BUN), endogenous creatinine (Ccr) and 24 h urine protein quantitation (UPQ).
RESULTSIn the observation group, after treatment, the remarkably effective rate was 50.0% (20/40) and the total effective rate was 82.5% (33/40), which were superior to 25.0% (10/40) and 45.0% (18/40) in the control group (both P < 0.05). After treatment, the levels of Scr, BUN and 24 h UPQ were reduced apparently (all P < 0.05), and the level of Ccr was increased apparently in the two groups (both P < 0.05). After treatment, the levels of Scr, BUN and 24 h UPQ were reduced much more apparently in the observation group as compared with those in the control group (all P < 0.05).
CONCLUSIONGuan's quadruple therapy for kidney disease achieves a better efficacy on CRF compared with the conventional western medication. This therapy improves renal functions, relieves clinical symptoms and physical signs and benefits the life quality of patients.
Acupuncture Therapy ; Adult ; Combined Modality Therapy ; Drugs, Chinese Herbal ; administration & dosage ; Female ; Humans ; Kidney Failure, Chronic ; drug therapy ; physiopathology ; therapy ; Kidney Function Tests ; Male ; Middle Aged ; Young Adult
4.Effect of oral administration of prednisone on prevention of moderate and severe ovarian hyperstimulation syndrome
zhong, ZHENG ; xiao-ming, ZHAO ; yan, HONG ; yun, SUN
Journal of Shanghai Jiaotong University(Medical Science) 2006;0(03):-
0.05). Conclusion Oral administration of prednisone can prevent modrate and severe OHSS and may have no effect on pregnant rate of IVF.
6.Melatonin and Spinal Cord Injury(review)
Hongxia DING ; Zheng YANG ; Yun TIAN ; Xiao ZHANG
Chinese Journal of Rehabilitation Theory and Practice 2010;16(6):546-548
Clinical studies show that melatonin has a unique biochemical characteristics. This article reviewed the specific role of melatonin in the region, antioxidant, anti-apoptosis, calcium antagonistic effect of melatonin treatment of the aspects of the effectiveness of spinal cord injury, and medication for a brief description.
7.Advance in Neurotrophin-3 Repairing Spinal Cord Injury(review)
Yanli DANG ; Juncen LI ; Zheng YANG ; Yun TIAN ; Xiao ZHANG
Chinese Journal of Rehabilitation Theory and Practice 2010;16(2):140-142
: The recovery of spinal cord injury(SCI) is a difficult problem in neuroscience research field, one of the reasons is that the ability of injured spinal cord regeneration is limited. Recent years many experiments prove that neurotrophin-3 is very important in SCI regeneration recovery, the gene transplantation is effective. This article makes a summary of SCI treatment research advancement.
8.Analysis of PM2.5 pollution in Urumqi City from 2016 to 2023 and construction of a prediction model
CHEN Peidi ; XIAO Tingting ; LI Xinxiu ; ZHENG Shuaiyin ; HUANG Yun
Journal of Preventive Medicine 2024;36(6):510-513
Objective:
To analyze the characteristics of fine particulate matter (PM2.5) pollution in Urumqi City, Xinjiang Uygur Autonomous Region from 2016 to 2023 and establish a prediction model, so as to provide the reference for air pollution prevention and control.
Methods:
PM2.5 monitoring data of Urumqi City from 2016 to 2023 were collected through the website of Ministry of Ecology and Environment of China. The changing trend of PM2.5 concentration was analyzed using temporal chart and seasonal index. PM2.5 monthly average concentrations from 2016 to 2023 were used to establish an autoregressive integrated moving average (ARIMA) model, and the data in 2023 was fitted and compared with the actual values, using mean absolute percentage error (MAPE) to evaluate the effectiveness of the model, and PM2.5 monthly average concentration from 2024 to 2025 was predicted.
Results:
PM2.5 daily average concentration in Urumqi City showed a decreasing trend from 2016 to 2023 (rs=-0.239, P<0.001), with high seasonal indexes in January, February and December, indicating certain seasonal characteristics. The optional model was ARIMA (1, 0, 0) (1, 1, 0)12, with the value of Akaike information criterion, corrected Akaike information criterion, and Bayesian information criterion being 727.38, 727.88 and 737.10, respectively. PM2.5 monthly average concentration in 2023 was fitted and compared with the actual values, with an absolute error range of 0.31-7.45 μg/m3, a relative error range of 0.01-0.53, and MAPE of 14.42%. PM2.5 monthly average concentration in Urumqi City from 2024 to 2025 was predicted to be consistent with the trend from 2016 to 2023.
Conclusions
PM2.5 concentration in Urumqi City showed a tendency towards a decline from 2016 to 2023, and was relatively high in winter. ARIMA (1, 0, 0) (1, 1, 0)12 can be used for short-term prediction of PM2.5 pollution in Urumqi City.
9.Clinical research of traditional Chinese medicine for the treatment of high myopia with macular hemorrhage
Ming-Fu, GONG ; Zheng, REN ; Qian-Feng, XIAO ; Yan, LIANG ; Xiao-Yun, HUANG
International Eye Science 2015;(7):1263-1265
AlM:To study the treatment effect of traditional Chinese medicine in the treatment of high myopia macular hemorrhage, using Chinese medicine etiology and pathogenesis, syndrome differentiation treatment, and provide the basis for the clinical treatment. METHODS: Eighty patients ( 135 eyes ) with high myopia macular hemorrhage were selected in the hospital from January 2012 to september 2014 as treatment group, and applied traditional Chinese medicine treatment. Forty-five patients (64 eyes) with the same period, as the control group, received routine western medicine treatment. After 1mo treatement, the treatment effect and vision improvement situation of two groups were observed, and after 6mo follow-up, the relapse was observed.RESULTS: The total effective rate of treatment group was 85. 19% (115/135), higher than the control group 78. 13% (50/64) (P<0. 05). The average corrected visual acuity of treatment group was 0. 48±0. 11, higher than the control group 0. 36 ± 0. 09, the difference was statistically significant (P<0. 05). The average diopter and macular bleeding scope of the treatment group were -9. 81±0. 85D and 0. 51 ± 0. 27PD, lower than the control group -10. 76 ± 0. 91D and 0. 78 ± 0. 23PD, the differences were statistically significant ( P < 0. 05 ). The eye ground hemorrhage absorption time of treatment group was 25. 34±2. 28d, less than the control group 29. 72 ± 2. 13d, the difference was statistically significant (P<0. 05). The bleeding again of the control group 7. 81% ( 5/64 ), higher than the treatment group was 5. 19% (7/135), the difference was statistically significant (P<0. 05).CONCLUSlON: Evidence-based treatment of traditional Chinese medicine for high myopia macular hemorrhage has good clinical effect, can shorten the treatment time, and is beneficial to the recovery of postoperative vision, worthy of clinical popularization and application.
10.Simultaneous determination of seven constituents in Lamiophlomis rotata by HPLC.
Shi-hong ZHONG ; Rui GU ; Ling-xin WANG ; Yan-feng LIAO ; Xiao-huat ZHENG ; Xin ZHENG ; Yun CAO
China Journal of Chinese Materia Medica 2014;39(22):4373-4378
OBJECTIVETo establish a new method for simultaneous determination of shanzhiside methyl ester, chlorogenic acid, 8-O-acetyl shanzhiside methylester, forsythiaside B, rutin, acteoside and galuteolin in Lamiophlomis rotata.
METHODSeparation was performed on a Welchrom-C18 chromatographic column with acetonitrile-0.1% orthophosphoric acid as mobile phasewith gradient elution. The flow rate was 1.0 mL x min(-1). The column temperature was 30 degrees C, and the detection wavelength was set at 238 nm, 330 nm and 350 nm.
RESULTThe seven compounds were well separated with good linear correlations. The mean recoveries of seven compounds were 96.47%-102.2% (RSD 0.70%-2.2%).
CONCLUSIONThere were good correlations among the seven compounds in the samples of aerial parts. The mean sum of shanzhiside methyl ester and 8-O-acetyl shanzhiside methylester in samples of aerial parts is 1.44%. The aerial parts have more kinds of composition and with higher content than that of underground parts in L. rotata, which was reasonable for the resonable use of the aerial part as medicinal part. The method was simple, repeatable and stable, which could be used for identification and quality evaluation of L. rotata.
Chlorogenic Acid ; chemistry ; Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; chemistry ; Glucosides ; chemistry ; Glycosides ; chemistry ; Lamiaceae ; chemistry ; Methyl Ethers ; chemistry ; Phenols ; chemistry ; Plant Components, Aerial ; chemistry ; Plants, Medicinal ; chemistry ; Pyrans ; chemistry ; Rutin ; chemistry