2.The technological innovation strategy for quality control of Chinese medicine based on Big Data.
Zhen-hao LI ; Zhong-zhi QIAN ; Yi-yu CHENG
China Journal of Chinese Materia Medica 2015;40(17):3374-3378
The evolution of the quality control concepts of medical products within the global context and the development of the quality control technology of Chinese medicine are briefly described. Aimed at the bottlenecks in the regulation and quality control of Chinese medicine, using Big Data technology to address the significant challenges in Chinese medicine industry is proposed. For quality standard refinements and internationalization of Chinese medicine, a technological innovation strategy encompassing its methodology, and the R&D direction of the subsequent core technology are also presented.
Data Mining
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Databases, Factual
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Drug Industry
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organization & administration
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standards
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Drugs, Chinese Herbal
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analysis
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pharmacology
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standards
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Humans
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Quality Control
4.Chemically mediated 14-3-3 protein post-translational modification interference: design of molecular glue and the application in cancer treatment
Liu-yi WU ; Long-jing LI ; Yu-cheng TIAN ; Qian-qian XU ; Wei WEI ; Zhi-yu LI ; Jin-lei BIAN
Acta Pharmaceutica Sinica 2024;59(11):2953-2961
Protein-protein interactions (PPIs) are not only crucial for the assembly of protein complexes but also fundamental for maintaining normal biological functions. These interactions are vital for protein structure and biological functionality and play a central role in cellular signaling, metabolic pathways, and regulatory networks. The 14-3-3 protein, highly conserved and widely expressed in eukaryotes, primarily recognizes and binds to its partner proteins to participate in essential life processes such as cell cycle control, signal transduction, and energy metabolism. This review discusses the role of dysregulated PPIs between 14-3-3 proteins and their partner proteins such as estrogen receptor
5.Relevant Research on ACE Gene Single Nucleotide Polymorphisms and Premature Coronary Heart Disease Patients with Blood Stasis Syndrome.
Lin LI ; Jie LI ; Zhi-xi HU ; Wei-xiong JIAN ; Jian-auo WANG ; Wen-xin YU ; Zhi LING ; Qian YUAN
Chinese Journal of Integrated Traditional and Western Medicine 2015;35(6):686-690
OBJECTIVETo explore the relationship between angiotensin converting enzyme (ACE) gene single nucleotide polymorphisms (SNP) and premature coronary heart disease (PCHD) patients with blood stasis syndrome (BSS).
METHODSrs4343, rs4293, and rs4267385 were selected at SNP from ACE gene. Allele and genotype were detected. Frequencies of allele and genotype were compared by using time-of-flight mass spectrometry technique (TOF-MS).
RESULTSCompared with the healthy control group, genotype of rs4293 and rs4267385 in ACE gene were similar, but there was statistical difference in polymorphisms and allele frequencies of rs4343 in the I and II group (P < 0.05, P < 0.01). The frequency of G allele was higher in the 3 groups than in the healthy control group (P < 0.05, P < 0.01). The relative risk analysis showed that the risk for PCHD occurrence in G allele carriers at rs4343 (GG +AG) was 3. 6 times the risk in non-G allele carriers (95% CI: 1.224-10.585, P = 0.02). There was also statistical difference in sex, age, TC, and TG after adjusted Logistic regression analysis (OR = 3.994, 95% CI: 1.230-12.974, P = 0.021).
CONCLUSIONThe polymorphism at rs4343 (G2350A) might be one of risk factors for PCHD occurrence, but not a predisposing factor for PCHD patients of BSS.
Alleles ; Case-Control Studies ; Coronary Artery Disease ; genetics ; Gene Frequency ; Genotype ; Humans ; Medicine, Chinese Traditional ; Peptidyl-Dipeptidase A ; genetics ; Polymorphism, Single Nucleotide ; Risk Factors
6.Effect of Kangnaoye on angiogenesis in rats after cerebral ischemic reperfusion
Zhi-Min ZHAO ; Zhi-Juan XIAO ; Qian XUE ; Yu-An ZOU ; Li-Qiang XING
The Chinese Journal of Clinical Pharmacology 2014;(5):429-431
Objective To observe the effect of Kangnaoye on angiogene-sis in rats after focal cerebral ischemia reperfusion.Methods The male SD rats were randomly divided into 6 groups: sham operation group , model group, Kangnaoye high, middle and low dosages groups (24,12,6 g· kg -1· d-1), and nimodipine group(1 mg· kg -1· d -1).The mod-els of cerebral ischemia reperfusion were established in rats by methods of middle cerebral artery occlusion ( MCAO).Immunohistochemical method was used to observe the change of the microvessel density ( MVD ) after cerebral ischemic and the expression of vascular endothelial growth ( VEG), HGF and CD31 protein of rats which were killed at the 0.5, 3, and 7 d of reperfusion injury respectively 2 h after cerebral ischemia.The nervous function deficit scores were evaluated at the 2 , 24 , and 48 h af-ter reperfusion.Results Compared with model group , the neurological behavior performance in Nimodipine and Kangnaoye treatment groups were significantly improved , with an increased number of MVD , and en-hanced vascular endothelial growth factor ( VEGF) and hepatocyte growth factor( HGF) protein levels ( P<0.05 or P<0.01 ) , especially in the Kangnaoye middle dosage group.Conclusion Kangnaoye has neuropro-tective effect against focal cerebral ischemic injury by improving the ex-pression of VEGF and HGF , which is one of possible anti -ischemic mechanisms.
7.Effect of crocetin on cardiac hypertrophy induced by overloading pressure in rats.
Acta Pharmaceutica Sinica 2004;39(3):172-175
AIMTo study the influence of crocetin on cardiac hypertrophy induced by overloading pressure in rats.
METHODSThe model of cardiac hypertrophy was produced by overloading pressure in rats. The animals were divided into five groups: sham-operation group (0.5% CMC-Na, ig), model group (operation + 0.5% CMC-Na, ig), captopril group (operation + 50 mg x kg(-1), ig), crocetin I (100 mg x kg(-1), ig) and crocetin II (50 mg x kg(-1), ig). All animals were treated for 30 d by ig. Then, cardiac indexes were examined. The activity of ATPase and the hydroxyproline content in heart were assayed by colorimetric analysis. Matrix metalloproteinases (MMPs) activity was assayed by SDS-PAGE zymography.
RESULTSCompared with the model group, crocetin was found to significantly reduce the cardiac indexes and the content of hydroxyproline in heart, increase the activity of Na+ , K+ -ATPase, Ca2+, Mg2+ -ATPase and inhibit MMPs activity.
CONCLUSIONThe activity of MMPs may play a key role in the cardiac hypertrophy induced by overloading pressure, and proprably as a result of decreasing the activity of MMPs. Crocetin was shown to prevent remodeling of cardiac hypertrophy induced by overloading pressure.
Animals ; Ca(2+) Mg(2+)-ATPase ; metabolism ; Cardiomegaly ; enzymology ; metabolism ; Carotenoids ; pharmacology ; Hydroxyproline ; metabolism ; Male ; Matrix Metalloproteinase 2 ; metabolism ; Matrix Metalloproteinase 9 ; metabolism ; Myocardium ; enzymology ; Organ Size ; drug effects ; Rats ; Rats, Sprague-Dawley ; Sodium-Potassium-Exchanging ATPase ; metabolism
8.Mitochondria-targeted antioxidant Mitoquinone protects post-thaw human sperm against oxidative stress injury.
Li LIU ; Mei-jiao WANG ; Ting-he YU ; Zhi CHENG ; Min LI ; Qian-wen GUO
National Journal of Andrology 2016;22(3):205-211
OBJECTIVETo investigate the potential protective effect of the mitochondria-targeted antioxidant Mitoquinone (MitoQ) on post-thaw human sperm.
METHODSSemen samples were collected from 60 normal fertile men, each divided into six parts of equal volume to be incubated at 37 °C in normal saline (G0, control) or in the extender with 2 nmol/L (G1), 20 nmol/L (G2), 200 nmol/L (G3), 2 µmol/L (G4), and 20 µmol/L of MitoQ (G5). After one hour of incubation, the samples were subjected to computer-assisted semen analysis (CASA) for sperm motility, flow cytometry for reactive oxygen species (ROS), thiobarbituric acid assay for the concentration of malondialdehyde (MDA), and MitoTracker fluorescent staining and flow cytometry for the sperm mitochondrial membrane potential (MMP). Then, the semen were cryopreserved with none (B0), 200 nmol/L (B1), and 2 µmol/L of MitoQ (B2), followed by detection of the changes in the ROS, MDA, and MMP of the post-thaw sperm.
RESULTSThe percentage of progressively motile sperm and total rate of sperm motility were significantly higher in G3 ([30.8 ± 10.2]% and [70.6 ± 9.0]%) and G4 ([32.7 ± 13.5]% and [70.3 ± 11.9]%) than in G0 ([17.6 ± 5.0]% and [54.9 ± 11.5]%) (P < 0.05). The level of ROS dropped markedly with the increased concentration of MitoQ, 86.5 ± 31.6 in G3, 93.6 ± 42.0 in G4, and 45.1 ± 15.0 in G5, as compared with 160.8 ± 39.7 in G0 (P < 0.05). The content of MDA was remarkably lower in G3 ([0.9 ± 0.5] µmol/mg) and G4 ([0.9 ± 0.5] µmol/mg) than in G0 ([1.9 ± 1.1] µmol/mg) (P < 0.05), but not in G5 ([1.7 ± 0.7] µmol/mg), which was even higher than in G3 and G4 (P < 0.05). The MMP showed a significant reduction in G5 (1156 ± 216) in comparison with G0 (1701 ± 251) (P < 0.05) but exhibited no remarkable difference between G0 and G1 (1810 ± 298), G2 (1995 ± 437), G3 (1950 ± 334), or G4 (1582 ± 314). The percentage of progressively motile sperm and total rate of sperm motility after freezing-thawing were significantly decreased as compared with those of the fresh semen (P < 0.01), but both were remarkably higher in B1 ([3.2 ± 2.3]% and [ 43.0 ± 9.5]%) than in B0 ([0.8 ± 0.6]% and [26.5 ± 11.4]%) (P < 0.05). The ROS level was significantly lower in B1 and B2 than in B0 (34.6 ± 12. 3 and 37.0 ± 10.5 vs 56.9 ± 14.3, P < 0.05), and so was the MDA content ([1.4 ± 0.5] and [1.4 ± 0.6] µmol/mg vs [2.6 ± 1.0] µmol/mg, P < 0.05), but the MMP was markedly higher in B1 and B2 than in B0 (1010.0 ± 130.5 and 880.6 ± 128.6 vs 721.1 ± 24.8, P < 0.05).
CONCLUSIONAddition of MitoQ to the freezing extender at 200 nmol/L may effectively improve the quality of human sperm and MitoQ is a good protective addictive for human sperm cryopreservation.
Antioxidants ; Cryopreservation ; Humans ; Male ; Malondialdehyde ; analysis ; Membrane Potential, Mitochondrial ; Mitochondria ; Organophosphorus Compounds ; pharmacology ; Oxidative Stress ; drug effects ; Reactive Oxygen Species ; Semen ; Semen Analysis ; Semen Preservation ; Sperm Motility ; Spermatozoa ; drug effects ; Ubiquinone ; analogs & derivatives ; pharmacology
9.Pharmacokinetics of crocetin in rats.
Acta Pharmaceutica Sinica 2002;37(5):367-369
AIMTo develop an HPLC method for the determination of crocetin in rat plasma and study the pharmacokinetics in rats.
METHODSHypersil C18 column (5 microns, 4.6 mm x 200 mm) was used at column temperature 30 degrees C. The mobile phase consisted of methanol-water-acetic acid (75:24.5:0.5) at the flow rate of 1.0 mL.min-1. The UV detection wave length was 423 nm.
RESULTSThe calibration curve was linear (gamma = 0.9996) in the range from 0.49 microgram.mL-1 to 7.87 micrograms.mL-1 for crocetin. The mean recovery was 105.2%. The lowest detectable concentration of crocetin was 0.14 microgram.mL-1 (S/N = 3). The RSDs of within-day and between-day were all less than 5%. The plasma crocetin was steady. The HPLC method of determination of crocetin in the plasma was established. After single dose of 50 mg.kg-1 ig in 10 rats, the main pharmacokinetic parameters were estimated as follows: T1/2 alpha (30 +/- 6) min, Tmax(65 +/- 16) min, Cmax(5.0 +/- 1.0) microgram.mL-1, AUC0-T(845 +/- 109) microgram.min.mL-1, Vd(5.0 +/- 0.8) L.kg-1. Crocetin was shown to be absorbed into the blood through the gastrointestinal tract.
CONCLUSIONThis method is quick, precise and reliable. Crocetin was shown to be quickly absorbed in rats.
Animals ; Antineoplastic Agents, Phytogenic ; blood ; isolation & purification ; pharmacokinetics ; Carotenoids ; blood ; isolation & purification ; pharmacokinetics ; Chromatography, High Pressure Liquid ; methods ; Crocus ; chemistry ; Female ; Male ; Plants, Medicinal ; chemistry ; Rats ; Rats, Sprague-Dawley
10.Effects of crocetin on VCAM-1 expression in human umbilical vein endothelial cells and monocyte-endothelial cell adhesion.
Shu-guo ZHENG ; Meng-qiu ZHAO ; You-nan REN ; Jie-ren YANG ; Zhi-yu QIAN
Acta Pharmaceutica Sinica 2015;50(1):34-38
Crocetin, a naturally occurring carotenoid, possesses antioxidant and antiatherosclerotic properties, of which the underlying mechanism remains unclear. In the present study, we examined the effects of crocetin (0.1, 1, 10 μmol·L(-1)) on angiotensin II (Ang II, 0.1 μmol·L(-1)) induced expression of vascular cell adhesion molecule-1 (VCAM-1) in human umbilical vein endothelial cells (HUVECs) and monocyte-endothelial cell adhesion. The effects of crocetin on the activation of nuclear factor kappa B (NF-κB) and intracellular reactive oxygen species (ROS) were also observed. The results demonstrated that crocetin notably suppressed Ang II induced NF-κB activation (P<0.01) and VCAM-1 expression (P<0.05, P<0.01) in HUVECs, accompanied by a markedly reduced monocyte-endothelial cell adhesion (P<0.05, P<0.01). In addition, preincubation with crocetin resulted in a significant enhancement of cellular antioxidant capacity (P<0.05, P<0.01), while Ang II induced intracellular ROS decreased markedly (P<0.05, P<0.01). These results indicated that crocetin was capable of suppressing Ang II induced VCAM-1 expression and monocyte-endothelial cell adhesion by suppression of NF-κB activation, which might be derived from the enhancement of antioxidant capacity and subsequent reduction of intracellular ROS.
Angiotensin II
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metabolism
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Antioxidants
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pharmacology
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Carotenoids
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pharmacology
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Cell Adhesion
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drug effects
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Human Umbilical Vein Endothelial Cells
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cytology
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drug effects
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metabolism
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Humans
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Monocytes
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cytology
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NF-kappa B
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metabolism
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Reactive Oxygen Species
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metabolism
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Vascular Cell Adhesion Molecule-1
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metabolism