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1.
Acta Pharmaceutica Sinica ; (12): 1059-1068, 2023.
Article in Chinese | WPRIM | ID: wpr-978746

ABSTRACT

1-Deoxy-D-xylulose-5-phosphate synthase (DXS), the first key enzyme in 2-methyl-D-erythritol-4-phosphate (MEP) pathway, catalyzes the condensation of glyceraldehyde-3-phosphate with pyruvate to 1-deoxy-xylose-5-phosphate (DXP). In this study, PgDXS1, PgDXS2, and PgDXS3 genes were cloned from the root of Platycodon grandiflorum (P. grandiflorum). The open reading frame (ORF) of PgDXS1, PgDXS2, and PgDXS3 were 2 160, 2 208, and 2 151 bp in full length, encoding 719, 735, and 716 amino acids, respectively. Homologous alignment results showed a high identity of PgDXSs with DXS in Hevea brasiliensis, Datura stramonium and Stevia rebaudiana. The recombinant expression plasmids of pET-28a-PgDXSs were constructed and transformed into Escherichia coli (E. coli) BL21 (DE3) cells, and the induced proteins were successfully expressed. Subcellular localization results showed that PgDXS1 and PgDXS2 were mainly located in chloroplasts, and PgDXS3 was located in chloroplasts, nucleus and cytoplasm. The expression of three DXS genes in different tissues of two producing areas of P. grandiflorum were assayed via real-time fluorescence quantitative PCR, and the results showed that all of them were highly expressed in leaves of P. grandiflorum from Taihe. Under methyl jasmonate (MeJA) treatment, the expression levels of three PgDXS genes showed a trend of first decreasing and then increasing at different time points (3 - 48 h), and the activity of DXS showed a trend of first increasing and then decreasing in three tissues of P. grandiflorum. This study provides a reference for further elucidating the biological function of PgDXS in terpenoid synthesis pathway in P. grandiflorum.

2.
Journal of Southern Medical University ; (12): 448-456, 2022.
Article in Chinese | WPRIM | ID: wpr-936337

ABSTRACT

RNA binding protein (RBP) plays a key role in gene regulation and participate in RNA translation, modification, splicing, transport and other important biological processes. Studies have shown that abnormal expression of RBP is associated with a variety of diseases. The Musashi (Msi) family of mammals is an evolutionarily conserved and powerful RBP, whose members Msi1 and Msi2 play important roles in the regulation of stem cell activity and tumor development. The Msi family members regulate a variety of biological processes by binding and regulating mRNA translation, stability and downstream cell signaling pathways, and among them, Msi2 is closely related to embryonic growth and development, maintenance of tumor stem cells and development of hematological tumors. Accumulating evidence has shown that Msi2 also plays a crucial role in the development of solid tumors, mainly by affecting the proliferation, invasion, metastasis and drug resistance of tumors, involving Wnt/β-catenin, TGF-β/SMAD3, Akt/mTOR, JAK/STAT, Numb and their related signaling pathways (Notch, p53, and Hedgehog pathway). Preclinical studies of Msi2 gene as a therapeutic target for tumor have achieved preliminary results. This review summarizes the molecular structure, physiological function, role of Msi2 in the development and progression of various solid tumors and the signaling pathways involved.


Subject(s)
Animals , Hedgehog Proteins , Mammals/metabolism , Neoplasms/genetics , Neoplastic Stem Cells , RNA-Binding Proteins/metabolism , Signal Transduction
3.
Acta Pharmaceutica Sinica ; (12): 1712-1718, 2021.
Article in Chinese | WPRIM | ID: wpr-881565

ABSTRACT

Methotrexate (MTX) injection has a short half-life and significant toxic side effects. In order to overcome the demerits of MTX injection, MTX@COF was prepared for subcutaneous injection by loading MTX in crosslinked cyclodextrin metal-organic framework (COF) in this study. The cationic lipid material (2, 3-dioleoyl-propyl)-trimethylamine (DOTAP) was then coated on the MTX@COF surface by solvent evaporation. Different surface charge characteristics were observed in the coated MTX@COF@DOTAP with no significant change in particle morphology. The in vitro release behaviors of sustained-release particles were investigated in water and phosphate buffer (pH 7.4), and the in vivo release characteristics were evaluated for pharmacokinetics in rats. The in vitro release results showed that the cumulative release of MTX, MTX@COF and MTX@COF@DOTAP within 6 h was 92.70%, 36.31% and 18.19% in water, respectively; the cumulative release of MTX, MTX@COF and MTX@COF@DOTAP within 4 h was 90.82%, 79.37% and 58.30% in phosphate buffer, respectively; the results showed that MTX@COF can significantly delay the release of MTX, the modification to MTX@COF by DOTAP can further delay the release of MTX. Pharmacokinetic studies in rats showed that the mean retention time [MRT(0-t)] and the time to peak (Tmax) of the subcutaneous injection of MTX@COF@DOTAP group were significantly prolonged compared with the MTX@COF group and the MTX group. The area under the concentration-time curve [AUC(0-t)] of the MTX@COF@DOTAP subcutaneous injection group was 1.8 times high as that of the MTX group. In this study, MTX@COF@DOTAP particles had a certain sustained-release effect, and could prolong the bioavailability of MTX by subcutaneous injection, which provided a new idea for the development of new MTX dosage forms.

4.
Chinese Journal of Experimental Traditional Medical Formulae ; (24): 147-156, 2021.
Article in Chinese | WPRIM | ID: wpr-906405

ABSTRACT

Objective:To study the distribution characteristics of mineral elements in <italic>Gastrodia elata </italic>samples<italic> </italic>with different grades and specifications (variants) from diverse producing areas and their classification and identification evidences. Method:Fourteen mineral elements in 31 batches of <italic>Gastrodia elata</italic> samples of different grades and specifications (variants) from diverse producing areas were determined by atomic absorption spectrophotometry, Mo-Sb colorimetry, and curcumin colorimetry, and then subjected to correlation analysis (CA), discriminant analysis (DA), and principal component analysis (PCA). Result:The content of K, N, and P in <italic>G. elata</italic> was the highest, enabling them to serve as the nutritional limiting factors affecting its growth. The <italic>G. elata</italic> samples could be identified by the variation trend of elements (K>N>P>Mg>Ca>Fe>B>Zn>Mn>Cu>Ni>Cr>Pb>Cd). The comparison of <italic>G. elata</italic> samples from multiple producing areas showed that <italic>G. elata</italic> from Zhaotong has the highest P, Fe, and Cd content, that from Lijiang the highest K content, that form Luotian the highest Zn and Cr content, and that from Jinzhai the highest Cu and Pb content. The content of Mg, B, Pb, and Cr in <italic>G. elata</italic> f. <italic>elata</italic> was higher than that in <italic>G. elata </italic>f. <italic>glauca</italic>. It was found that the content of P, Cu, and Cd in commercially available <italic>G. elata </italic>products gradually increased with the decrease in the commercial grade, while that of Mg, Fe, B, and Ni mostly decreased. As revealed by CA, Fe was positively correlated with Mg, Cr, and B. The producing areas of <italic>G. elata</italic> samples could be effectively identified by DA with Cd, Pb, Cr, Cu, B, and Ni as the main variables, and the accuracy reached up to 85.71%. According to the PCA of mineral elements in <italic>G. elata</italic> f. <italic>glauca</italic> from Zhaotong, Yunnan Province, Fe, Cr, Mg, Cd, P, Mn, B, Pb, and Cu exerted a greater influence on <italic>G. elata</italic>. Conclusion:The determination of mineral elements in <italic>G. elata</italic> samples contributes to identifying their authenticity and origin due to the easy operation, accurate results, and good stability.

5.
China Journal of Chinese Materia Medica ; (24): 2702-2707, 2020.
Article in Chinese | WPRIM | ID: wpr-828028

ABSTRACT

Gastrodia Rhizoma, as a precious Chinese materia medica, has attracted the attention of Chinese materia medica experts in the past dynasties for the commercial specification and experimental identification, and has gradually formed a wealth of terms concerning commercial specification and experimental identification. Through combing the literatures of successive dynasties, this paper discussed the change of the commercial specification of the Gastrodiae Rhizoma and formation of its identifying terms. It has found that the Gastrodiae Rhizoma mainly came from the dried rhizomes of the Gastrodia elata f.elata before the Qing Dynasty. Since the Qing Dynasty, G. elata in Yunnan and Guizhou gradually arose and become one of sources of mainstream commodities. After that, G. elata f. glauca and G. elata f. elata were becoming the main sources of Gastrodiae Rhizoma. Before the large-scale cultivation of G. elata in the 1970 s, there is only wild G. elata over the country. In terms of commercial specification, they were often classified into Chunma and Dongma according to their harvest time. With the successful promotion of cultivation technology and the endangered wild resources of G. elata, the Dongma became the mainstream in the market. The adulterants of G. elata increased significantly in the 1960 s and 1970 s, in this period, the terms of experimental identification for G. elata also increased obviously. Experimental identification is distinctive in different times, therefore, studying experimental identification of medicinal materials helps to promote the development of the Chinese materia medica.


Subject(s)
China , Drugs, Chinese Herbal , Gastrodia , Materia Medica , Rhizome
6.
Tianjin Medical Journal ; (12): 288-291, 2018.
Article in Chinese | WPRIM | ID: wpr-698026

ABSTRACT

Objective To investigate the effect of red light irradiation therapy on postherpetic neuralgia and the improvement in the life quality of patients.Methods Ninety patients with postherpetic neuralgia diagnosed and treated in our hospital from January 2013 to August 2016 were randomly divided into red light irradiation group (n=45) and control group(n=45).The control group was given gabapentin 400 mg once daily for 14 days.On the basis of routine drug treatment, the red light irradiation group was treated with red light irradiation for 15-30 minutes, once daily for 10 days. The serum levels of interleukin(IL)-2,IL-6 and IL-10 were detected by enzyme-linked immunosorbent assay(ELISA).The intensity of pain was evaluated by VAS score,and the quality of life was assessed by DLQI. Results Before treatment,there were no significant differences in serum levels of IL-2,IL-6 and IL-10 between two groups.After treatment,the serum levels of IL-2 and IL-10 were significantly higher in red light irradiation group than those of the control group(P<0.05),and the level of IL-6 was significantly lower in red light irradiation group than that of the control group(P<0.05).Before treatment,there was no significant difference in the VAS score between the two groups.After treatment,the VAS score was significantly lower in the red light irradiation group than that of the control group (P<0.05). Before treatment, there were no significant differences in DLQI scores between the two groups.After treatment,the DLQI scores were significantly lower in the red light irradiation group than those in the control group(P<0.05).Conclusion The treatment of postherpetic neuralgia with red light irradiation can provide effective relief of pain and improve the life quality of patients.

7.
China Journal of Chinese Materia Medica ; (24): 2522-2530, 2018.
Article in Chinese | WPRIM | ID: wpr-687424

ABSTRACT

Three different kinds of sinomenine in situ liquid crystal were prepared for different prescriptions, to investigate the rheological properties before and after in situ treatment and evaluate its feasibility for embolization. Rheological experiments were carried out with cone plate fixtures. Both the steady-state rheological and non-steady-state rheological properties of in-situ gels and the swelling gels were studied and compared. Steady-state rheological study results showed that all the three liquid embolic agents were non-newtonian fluid before and after in situ treatment, which would become less ropy when they were pressed with shear stress; their viscosities differed by 2-5 orders of magnitude. It had a yield value of about 10 Pa before in situ treatment and about 4 500 Pa after in situ treatment. All the six systems had thixotropy while their dynamic viscosities were not influenced by the shear rate, all less than 0.3 Pa·s before in situ treatment more than 1 Pa·s after in situ treatment, differing by an order of magnitude. The results of temperature sweeping showed a slight decrease with a steady rate in viscosity within the range of 10-50 °C, differing by 3-4 orders of magnitude. The results of unsteady rheology showed that there was no obvious linear viscoelastic region in the three kinds of agents, indicating the properties of liquid. After in situ treatment, their linear viscoelastic range γ<1% (No.3 was 5%), and their elastic modulus G' was larger than the viscous modulus G", indicating the properties of solid. Frequency scanning results showed that for the systems at low frequencies, G">G', system viscosity in a dominant position; while at high frequencies, G'>G", system elasticity in a dominant position. The results of compound viscosity test also proved that the liquid embolic agent in situ can form a cubic liquid crystal (the structure of No. 3 was destroyed after in situ treatment). The DHR-2 rheometer was used to investigate the rheological properties of in situ gels with three different prescriptions. The method is simple and the result is reliable, which can provide more theoretical reference for the evaluation and practical application of the product.

8.
China Journal of Chinese Materia Medica ; (24): 1637-1640, 2017.
Article in Chinese | WPRIM | ID: wpr-350135

ABSTRACT

Platycodon grandiflorum, a traditional Chinese medicine commonly used for coughing and eliminating phlegm to relieve asthma, has gained great attention to its quality evaluation in ancient and modern herbal books. This paper investigated the methods of quality evaluation in the ancient herbal books systematically, and the results showed that there were bitter and sweet P. grandiflorum, south and north P. grandiflorum. Those distributed in east China were called south P. grandiflorum, with bitter taste; and those distributed in north China, northeast China were called north P. grandiflorum, with sweet taste. There was a common sense that P. grandiflorum with a bitter taste had good quality in the ancient herbal books, namely those produced in east China. P. grandiflorum of better quality were characterized by thicker and longer root, white color, solid texture and bitter taste in properties. In addition, the quality of P. grandiflorum was also affected by its germplasm, collecting and processing. This paper summarized the formation and development of the "assessing the quality by distinguishing features of traditional Chinese medicinal materials" views of P. grandiflorum, providing the herbalism basis for its present quality evaluation.

9.
Chinese Journal of Information on Traditional Chinese Medicine ; (12): 44-47, 2017.
Article in Chinese | WPRIM | ID: wpr-657360

ABSTRACT

Objective To compare the effects of moxibustion at different temperatures on blood lipid and TRPV1 in dorsal root ganglion with hyperlipidemia rats; To verify the correlation between efficacy of adjusting fat of moxibustion with activating of TRPV1. Methods The rat model of hyperlipidemia was made by high fat diet. 60 SD mice were randomly divided into four groups: control group, model control group, the 38 ℃ moxibustion group and the 45 ℃ moxibustion group, with 15 mice in each group. Acupoints Shenque and Zusanli were chosen under moxibustion for 10 minutes each time, once another day, for 4 weeks, in the 38 ℃ moxibustion group and the 45 ℃moxibustion group. Blood was taken after intervention, and blood TC, TG, LDL-C and HDL-C of the mice were detected by oxidase method; the dorsal root ganglion was taken to detect the expression of TRPV1 mRNA by real-time fluorescence quantitative PCR. Results Compared with model group, blood lipid indexes in moxibustion groups had different changes, with statistical significance compared with 45 ℃ moxibustion group (P<0.05, P<0.01), and there was statistical significance between 38 ℃ moxibustion group and 45 ℃ moxibustion group (P<0.01); there was statistical significance in TRPV1 mRNA of dorsal root ganglion among 45 ℃ moxibustion group and other three groups (P<0.01). Conclusion The correlation between efficacy of adjusting fat of moxibustion with activating of TRPV1 has been confirmed.

10.
Chinese Journal of Information on Traditional Chinese Medicine ; (12): 44-47, 2017.
Article in Chinese | WPRIM | ID: wpr-659345

ABSTRACT

Objective To compare the effects of moxibustion at different temperatures on blood lipid and TRPV1 in dorsal root ganglion with hyperlipidemia rats; To verify the correlation between efficacy of adjusting fat of moxibustion with activating of TRPV1. Methods The rat model of hyperlipidemia was made by high fat diet. 60 SD mice were randomly divided into four groups: control group, model control group, the 38 ℃ moxibustion group and the 45 ℃ moxibustion group, with 15 mice in each group. Acupoints Shenque and Zusanli were chosen under moxibustion for 10 minutes each time, once another day, for 4 weeks, in the 38 ℃ moxibustion group and the 45 ℃moxibustion group. Blood was taken after intervention, and blood TC, TG, LDL-C and HDL-C of the mice were detected by oxidase method; the dorsal root ganglion was taken to detect the expression of TRPV1 mRNA by real-time fluorescence quantitative PCR. Results Compared with model group, blood lipid indexes in moxibustion groups had different changes, with statistical significance compared with 45 ℃ moxibustion group (P<0.05, P<0.01), and there was statistical significance between 38 ℃ moxibustion group and 45 ℃ moxibustion group (P<0.01); there was statistical significance in TRPV1 mRNA of dorsal root ganglion among 45 ℃ moxibustion group and other three groups (P<0.01). Conclusion The correlation between efficacy of adjusting fat of moxibustion with activating of TRPV1 has been confirmed.

11.
International Journal of Pediatrics ; (6): 291-293, 2017.
Article in Chinese | WPRIM | ID: wpr-608603

ABSTRACT

Objective To evaluate the levels of pulmonary surfactant protein D (SP-D) and 56-kD human type Ⅰ protein(HTI-56) in bronchoalveolar lavage fluid and serum of children with mycoplasma pneumoniae pneumonia,as well as their potential as biomarkers of mycoplasma pneumoniae pneumonia.Methods A retrospective study was conducted in 57 children with mycoplasma pneumoniae pneumonia from June 2011 to June 2016 in our hospital.In this study,the levels of SP-D and HTI-56 in bronchoalveolar lavage fluid and serum were determined and compared between unilateral lung infection and bilateral lung infection.Results SP-D and HTI-56 levels were significantly higher in bronchoalveolar lavage fluid samples (P < 0.05)compared with bronchoalveolar lavage fluid samples from uninfected lungs (P < 0.05).However,the serum levels of SP-D and HTI-56 in children with unilateral lung infection and bilateral pulmonary infection were not significantly different (P >0.05).Conclusion High levels of SP-D and HTI-56 in bronchoalveolar lavage fluid samples from infected lungs may reflect damage to alveolar epithelial cells caused by mycoplasma pneumoniae.

12.
Chongqing Medicine ; (36): 4526-4528,4532, 2017.
Article in Chinese | WPRIM | ID: wpr-668504

ABSTRACT

Objective To investigate the correlation between three sperm indexes and the outcome of in vitro fertilization and embryo transfer(IVT-ET) before and after semen treatment.Methods The semen derived from 298 male patients treated with IVT-ET from the Affiliated Hospital of Southwest Medical University was retrospectively analyzed.Routine analysis of semen before treatment was performed according to the WHO standard.Vitrolife density gradient centrifugation combined with upstream method was used to analyze sperm parameters after sperm analysis,and the observation and statistics were performed after fertilization and sequential culture to day 3.Results The total viability of spermatozoa before and after semen treatment,the percentage of normal spermatozoa,sperm density,and other differences were statistically significant (P<0.05);The normal sperm morphology rate was positively correlated with fertilization rate(r=0.487,P<0.01) and cleavage rate(r=0.250,P<0.05);The sperm vitality of post-processed semen was positively related to the fertilization rate (r =0.249,P<0.05,);and significantly cleavage rate (r =0.272,P<0.05);After treatment,sperm density was positively correlated with 2 PN(r=0.609,P<0.01) and multiple PN fertilization rates(r=0.243,P<0.05).Conclusion Our experimental results indicate that the parameters of post-processed sperm treated at the day when the oocytes were collected may be more helpful in predicting the fertilization rate and cleavage rate of IVF-ET.Therefore,the IVF-ET treatment protocols should be chose based on the normal sperm morphology rate and sperm vitality after semen treatment.

13.
Chinese Journal of Current Advances in General Surgery ; (4): 684-686,691, 2017.
Article in Chinese | WPRIM | ID: wpr-665862

ABSTRACT

Objective:To retrospectively analyze the therapeutic effect of subtotal parathyroidectomy (sT-PTX) on uremic patients with secondary hyperparathyroidism (SHPT).Methods:Seventy two SHPT patients treated with sT-PTX in our hospital were enrolled in this study.Serum parathyroid hormone(PTH),calcium(Ca) and phosphorus(P) obtained in the preoperative,postoperative and followup periods were collected and compared.Their symptoms,postoperative complications and relapse were recorded.Results:(1)sT-PTX operation performed successfully in 70/72 patients(97.2%).(2)After sT-PTX,bone pain and itching improved rapidly,with the improvement of nutritional status,Partial patients with renal hypertension were remitted compared with preoperative.Thirteen cases can walk without wheelchair after sT-PTX.(3)Serum PTH,Ca,and P decreased significantly after sT-PTX for one week,one month and 6 months as compared with those before sT-PTX(P<0.05).(4)Postoperative hypocalcemia was frequently seen(53/72,53.6%) but could be effectively controlled by intravenous calcium infusion.(5)SHPT recurred in the 6 months after sT-PTX in 4 cases (5.7%).Conclusions:T-PTX can effectively decrease PTH level and improve symptoms,and is a safe measure for the treatment of uremic patients with SHPT.

14.
Acta Pharmaceutica Sinica ; (12): 132-139, 2016.
Article in Chinese | WPRIM | ID: wpr-320004

ABSTRACT

Phytantriol (PT), ethanol (ET) and water were used to prepare in situ cubic liquid crystal (ISV2). The pseudo-ternary phase diagram of PT-ET-water was constructed and isotropic solution formulations were chosen for further optimization. The physicochemical properties of isotropic solution formulations were evaluated to optimize the composition of ISV2. In situ hexagonal liquid crystals (ISH2) were prepared based on the composition of ISV2 with the addition of vitamin E acetate (VitEA) and the amount of VitEA was optimized by in vitro release behavior. The phase structures of liquid crystalline gels formed by ISV2 and ISH2 in excess water were confirmed by crossed polarized light microscopy and small angle X-ray scattering, respectively. Rheological properties of ISV2 and ISH2 were studied by a DHR-2 rheometer. In vitro drug release studies were conducted by using a dialysis membrane diffusion method. Pharmacokinetics was investigated by determination of sinomenine hydrochloride (SMH) concentration in synovial membrane after intra-articular injection of SMH-loaded ISH2 in adjuvant-induced arthritis rats. The optimal ISV2 (PT/ET/water, 64 : 16 : 20, w/w/w) loaded with 6 mg x g(-1) of SMH showed a suitable pH, injectable and formed a cubic liquid crystalline gel in situ with minimum water absorption in the shortest time. The optimal ISV2 was able to sustain the drug release for 144 h. The optimal ISH2 system was prepared by addition of 5% VitEA into PT in the optimal ISV2 system. This ISH2 (PT/VitEA/ET/water, 60.8 : 3.2 : 16 : 20, w/w/w/w) was an injectable isotropic solution with suitable pH. The new ISH2 was able to sustain the drug release for more than 240 h. Local pharmacokinetics study indicated that the retention time and AUC(0-∞) of ISH2 group were increased significantly compared with that of SMH solution group and the AUC(0-∞) of ISH2 group was 6.01 times higher than that of SMH solution group. The developed ISH2 was suitable for intra-articular injection that may apply to patients in the treatment of rheumatoid arthritis.


Subject(s)
Animals , Rats , Chemistry, Pharmaceutical , Diffusion , Ethanol , Fatty Alcohols , Gels , Injections, Intra-Articular , Liquid Crystals , Morphinans , Chemistry , Rheology , Water , alpha-Tocopherol
15.
Acta Pharmaceutica Sinica ; (12): 469-2016.
Article in Chinese | WPRIM | ID: wpr-779194

ABSTRACT

In this study, the Pickering emulsions were prepared using medium chain triglycerides (MCT) and α-cyclodextrin (α-CD) and the formation mechanism was studied by means of several physicochemical techniques. The MCT/α-CD microparticles, which stabilized the emulsions, were characterized by the measurement of interfacial tension and the contact angle (θow), powder X ray diffraction (XRD), scanning electron microscope (SEM), high performance liquid chromatography (HPLC), differential interference microscope (DIM), Cryo-scanning electron microscopy (Cryo-SEM). The physical stability of emulsions with different α-CD content in the continuous aqueous phase was investigated by determination of the droplet size and sedimentation rate, combined with the observation of droplet morphologies by the inverted phase contrast microscope. As a result, it was observed that the amphiphilic supramolecule of MCT and α-CD were indeed formed. Furthermore, MCT/α-CD microparticles formed by the aggregation of MCT/α-CD supramolecule absorbed at the oil/water interface, and then forming a membrane structure to stabilize emulsion. In addition, the average θow for the MCT/α-CD microparticles was (46.1±3.4)° which stabilized O/W emulsion. When the content of α-CD was increased in the continuous phase, there were more microparticles formed at the oil/water interface and in the continuous aqueous phase, which resulted in smaller particle size of droplet and higher viscosity of the continuous phase. In summary, the study suggest that α-CD/MCT/water emulsions were of O/W Pickering emulsions and the physical stability was better for emulsions with higher content of α-CD in the continuous phase.

16.
Acta Pharmaceutica Sinica ; (12): 132-2016.
Article in Chinese | WPRIM | ID: wpr-779147

ABSTRACT

Phytantriol (PT), ethanol (ET) and water were used to prepare in situ cubic liquid crystal (ISV2). The pseudo-ternary phase diagram of PT-ET-water was constructed and isotropic solution formulations were chosen for further optimization. The physicochemical properties of isotropic solution formulations were evaluated to optimize the composition of ISV2. In situ hexagonal liquid crystals (ISH2) were prepared based on the composition of ISV2 with the addition of vitamin E acetate (VitEA) and the amount of VitEA was optimized by in vitro release behavior. The phase structures of liquid crystalline gels formed by ISV2 and ISH2 in excess water were confirmed by crossed polarized light microscopy and small angle X-ray scattering, respectively. Rheological properties of ISV2 and ISH2 were studied by a DHR-2 rheometer. In vitro drug release studies were conducted by using a dialysis membrane diffusion method. Pharmacokinetics was investigated by determination of sinomenine hydrochloride (SMH) concentration in synovial membrane after intra-articular injection of SMH-loaded ISH2 in adjuvant-induced arthritis rats. The optimal ISV2 (PT/ET/water, 64:16:20, w/w/w) loaded with 6 mg·g-1 of SMH showed a suitable pH, injectable and formed a cubic liquid crystalline gel in situ with minimum water absorption in the shortest time. The optimal ISV2 was able to sustain the drug release for 144 h. The optimal ISH2 system was prepared by addition of 5% VitEA into PT in the optimal ISV2 system. This ISH2 (PT/VitEA/ET/water, 60.8:3.2:16:20, w/w/w/w) was an injectable isotropic solution with suitable pH. The new ISH2 was able to sustain the drug release for more than 240 h. Local pharmacokinetics study indicated that the retention time and AUC0-∞ of ISH2 group were increased significantly compared with that of SMH solution group and the AUC0-∞ of ISH2 group was 6.01 times higher than that of SMH solution group. The developed ISH2 was suitable for intra-articular injection that may apply to patients in the treatment of rheumatoid arthritis.

17.
Chinese Journal of Endemiology ; (6): 434-436, 2008.
Article in Chinese | WPRIM | ID: wpr-642471

ABSTRACT

Objective To assess the fluorine (F), arsenic (As) and selenium (Se) levels in hair of residents from the fluorosis area of Zhaotong and provide reference basis for the evaluation of the health status of populations in fluorosis areas as well as the prevention and control of fluorosis in Zhaotong. Methods Sixty-five hair samples were collected in fluorosis areas(Zhenxiong, Weixin County), including. 41 samples from 6 endemic townships and 24 samples from a non-endemic township. Fluorine content in hair was determined by combustion- hydrolysis-ion selective electrode method. Arsenic and selenium contents in hair were determined by atom- fluorescence method. Results The average contents of hair fluorine, arsenic and selenium contents were (15.1807±15.2397), (2.1806±1.9601), (2.3162±2.4535)mg/kg in the 41 patients with fluorosis and were (18.7703±17.1067), 0.3283±0.2466), (1.2805±0.6970) mg/kg in the 24 inhabitants (control). The difference of fluorine content in hair between patients in fluorosis and control inhabitants was not statistically significant (P 0.05), but the difference in arsenic and selenium content was statistically significant (P<0.05). Conclusions Mild arsenic pollution exists in Zhaotong fluorosis areas, which aggravates the prevalence of fluorosis. Food roasted with blended coal contains high fluorine. Meanwhile it may bring in the supplement of selenium for the inhabitants in Zhaotong fluorosis areas.

18.
Progress in Modern Biomedicine ; (24): 749-753, 2007.
Article in Chinese | WPRIM | ID: wpr-737067

ABSTRACT

This paper, from the aspects of neuroendocrine, emotion, learning etc, analyzed comprehensively the characteristics of the influence of prenatal stress (PS) on offspring, including intensity of PS, timing of exposure and individual differences. Despite the variety in methodology, most studies on it indicate that the prenatal stressful events lead to offspring's increased plasma glucocorticoid (GC) level, more depressed-related behaviors and impaired learning abilities. Although mechanism of prenatal stress is still unclear, most studies show that it is concerned with hypothalamio-pituitary-adneral (HPA) axis,dopaminergic (DA-ergic) system, neuropeptide Y (NPY)and serotoninergic (5-HT ergic) system. Moreover, further studies are proposed to pay more attention to the relationship and interaction of various related substances.

19.
Progress in Modern Biomedicine ; (24): 749-753, 2007.
Article in Chinese | WPRIM | ID: wpr-735599

ABSTRACT

This paper, from the aspects of neuroendocrine, emotion, learning etc, analyzed comprehensively the characteristics of the influence of prenatal stress (PS) on offspring, including intensity of PS, timing of exposure and individual differences. Despite the variety in methodology, most studies on it indicate that the prenatal stressful events lead to offspring's increased plasma glucocorticoid (GC) level, more depressed-related behaviors and impaired learning abilities. Although mechanism of prenatal stress is still unclear, most studies show that it is concerned with hypothalamio-pituitary-adneral (HPA) axis,dopaminergic (DA-ergic) system, neuropeptide Y (NPY)and serotoninergic (5-HT ergic) system. Moreover, further studies are proposed to pay more attention to the relationship and interaction of various related substances.

20.
China Journal of Chinese Materia Medica ; (24): 1807-1810, 2006.
Article in Chinese | WPRIM | ID: wpr-315951

ABSTRACT

<p><b>OBJECTIVE</b>To study the therapeutic effects and mechanisms of SQDG on carbon tetrachloride-induced chemical liver injury in mice as well as its possible mechanisms. At the same time the pharmacodynamics of SQDG was compared with TGP or ASTs of effective dose.</p><p><b>METHOD</b>The model of carbon tetrachloride-induced chemical liver injury in mice was prepared. The levels of ALT, AST, MDA content, SOD and GSH-Px activities in liver homogenate were assayed by spectrophotometry; Meanwhile, hepatic pathological examination was observed.</p><p><b>RESULT</b>Protective effect of SQDG on carbon tetrachloride-induced chemical liver injury: SQDG was able to significantly decrease serum transaminase levels of chemical liver injury's mice induced by carbon tetrachloride, decreased MDA content and improved the reduced SOD and GSH-px levels in liver homogenate. Furthermore, SQDG also attenuate the area and extent of necrosis and reduce the infiltration of inflammatory cell. Compared with TGP or ASTs of effective dose, SQDG has a better effect on carbon tetrachloride-induced chemical liver injury in mice.</p><p><b>CONCLUSION</b>SQDG can protect mice injured by carbon tetrachloride-induced chemical.</p>


Subject(s)
Animals , Male , Mice , Alanine Transaminase , Blood , Antioxidants , Pharmacology , Aspartate Aminotransferases , Blood , Astragalus propinquus , Chemistry , Carbon Tetrachloride Poisoning , Chemical and Drug Induced Liver Injury , Metabolism , Pathology , Drug Combinations , Glucosides , Pharmacology , Glutathione Peroxidase , Metabolism , Liver , Metabolism , Pathology , Malondialdehyde , Metabolism , Paeonia , Chemistry , Plants, Medicinal , Chemistry , Protective Agents , Pharmacology , Superoxide Dismutase , Metabolism
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