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Biomedical subjects

H Li

Publications and source records attributed to H Li.

At least 1,351 records · Page 75Linked to original sources

Absorption, distribution, elimination of tea polyphenols in rats.

Tea polyphenols-including (-)-epigallocatechin-3-gallate (EGCG), (-)-epigallocatechin (EGC), and (-)-epicatechin (EC)-are believed to be responsible for the beneficial effects of tea. This study was conducted to investigate the absorption, distribution, and elimination of EGCG, EGC, and EC in rats after administration of decaffeinated green tea (DGT). For comparison, pure EGCG was also studied. The plasma and tissue levels of EGCG, EGC, and EC were quantified by HPLC, and the results were analyzed by the PCNONLIN program. Following intravenous injection of DGT (25 mg/kg), the plasma concentration-time curves of EGCG, EGC, and EC were fitted in a two-compartment model. The beta-elimination half-lives (t1/2beta) were 212, 45, and 41 min for EGCG, EGC, and EC, respectively; the clearances were 2.0, 7.0, and 13.9 ml x min/kg, and the apparent distribution volumes (V(d)) were 1.5, 2.1, and 3.6 dl/kg. When pure EGCG (10 mg/kg) was given, however, a shorter t1/2beta (135 min), a larger clearance (72.5 ml x min/kg), and a larger V(d) (22.5 dl/kg) for EGCG were observed, suggesting that other components in DGT could affect the plasma concentration and elimination of EGCG. After intragastric administration of DGT (200 mg/kg), approximately 13.7% of EGC and 31.2% of EC were shown in the plasma, but only 0.1% of EGCG was bioavailable as judged by the ratio of AUC(i.g.)/AUC(i.v.). After intravenous administration of DGT (25 mg/kg), the level of EGCG was found to be the highest in the intestine samples, and the intestinal EGCG level declined with a t1/2 of 173 min. The highest levels of EGC and EC were observed in the kidney, and the levels declined rapidly with t1/2 of 29 and 28 min, respectively. The AUC of EGCG in the intestine was 4-fold higher than that in the kidney, but the AUCs of EGC and EC in the intestine were similar to those in the kidney. The liver and lung levels of EGCG, EGC, and EC were generally lower than those in the intestine and the kidney. The distribution results suggest that EGCG is mainly excreted through bile, and that EGC and EC are excreted through both the bile and urine.

Administration, Oral↗

Ethanol inhibits inducible nitric oxide synthase transcription and post-transcriptional processes in vivo.

The effects of ethanol (ETOH) on post-transcriptional regulation of inducible nitric oxide synthase (iNOS) in vivo has not been demonstrated. We examined the effect of ETOH on iNOS mRNA, protein, and the production of the nitrate and nitrite anion (RNI) in rat lung alveolar macrophages (AM) in vivo when stimulated by lipopolysaccharide (LPS) and dibutyryl cyclic AMP (DB-cAMP). Sprague-Dawley rats (225-250 g) (n = 5-7/gp) were given intratracheal LPS (0.6 mg/kg) or DB-cAMP (0.1 and 1 mg/kg) 30 min after ETOH (4 mg/kg, intraperitoneally (ip)) or phosphate-buffered sterile saline (PBS) (5 ml/kg, ip) or pyrrolidine dithiocarbamate (PDTC 10 mg/kg, intratracheally) or 15 min after diethyl dithiocarbamate (DETC) (5 mg/kg, intratracheally). At selected times after administration of LPS or DB-cAMP, the animals were anesthetized, the lungs with the heart attached were removed and the lungs subjected to bronchoalveolar lavage (BAL). The BAL fluid was assayed for tumor necrosis factor alpha (TNF alpha) and RNI. The BAL fluid AM were isolated and analyzed for iNOS mRNA and protein with competitor-equalized polymerase chain reaction (PCR) and Western blots, respectively. The ex vivo incubates of AM were assayed for RNI and TNF alpha. LPS and DB-cAMP each increased iNOS mRNA and protein in AM and RNI in the BAL fluid and ex vivo incubates of AM. However, the peak of the increase of iNOS mRNA occurred at 2 hr for DB-cAMP and 4 to 6 hr for LPS. Only LPS increased the concentrations of TNF alpha in BAL fluid and ex vivo incubates of AM. ETOH attenuated LPS-mediated up-regulation of iNOS mRNA and TNF alpha and iNOS protein and RNI produced by the AM. In contrast, pretreatment of rats with ETOH did not affect DB-cAMP-mediated increases of iNOS mRNA in AM at any time but suppressed the amount of iNOS protein and RNI produced in DB-cAMP-stimulated AM. DETC, but not PDTC, attenuated LPS-mediated up-regulation of iNOS mRNA without effects on that produced by DB-cAMP. Since ETOH and DETC, but not PDTC, suppressed LPS-mediated but not DB-cAMP-mediated transcription of iNOS, we conclude that two distinct pathways exist for induction of iNOS mRNA by these agonists. ETOH and DETC may inhibit the LPS-mediated activation pathway by acting as antioxidants. Also, since ETOH inhibited DB-cAMP-mediated increases in iNOS protein without affecting iNOS mRNA ETOH also acts at a post-transcriptional or translational site to inhibit iNOS protein in rat AM in vivo.

Animals↗

Phase I clinical trial of cefditoren pivoxil (ME1207). Tolerance in healthy volunteers.

A tolerance study to ME1207 was conducted in healthy volunteers using five single doses administered before a meal (50, 100, 200, 300 and 500 mg), a single 200 mg dose administered after a meal, and 200 mg administered every 12 h for 7 days. No subjective symptoms or changes in haematological and biochemical examinations and urinalysis were observed after single administration of 50 to 500 mg Four subjects complained of minimal upper abdominal discomfort when 200 mg was administered every 12 h for 7 days, but this symptom disappeared without remedial action in all cases. Therefore ME1207 was thought to be safe when orally administered at the above-mentioned doses by the above-mentioned administration methods.

Administration, Oral↗

The study of the relationship between the activity of phospholipase A2 and acute hypoxic pulmonary arterial pressure.

The role of phospholipase A2 (PLA2) and related inflammatory mediators in the mechanism of hypoxic pulmonary arterial hypertension was studied. Thirty Sprague-Dawley rats were equally divided into three groups at random: group A was the normal control group; group B was given 10% oxygen ventilation; group C was given 10% oxygen ventilation too and, at the same time, dexamethasone was injected into the external jugular vein. The pulmonary arterial pressure (PAP) was measured by inserting a microcatheter into pulmonary artery. After 30 minutes of hypoxia, the activity of PLA2, platelet activating factor (PAF), prostaglandin E2 (PGE2) and tromboxane B2 (TXB2) were measured in blood and lung tissue. After hypoxia, the mean pulmonary arterial pressure (mPAP), the PLA2 activity, PGE2, TXB2 and PAF in blood and lung tissue of group B were significantly higher than in group A; in group C the same parameters were lower than in group B. In hypoxia, a positive correlations was found between the PLA2 activity and mPAP, PAF, PGE2, TXB2 respectively; positive correlations were also found between PAF, PGE2, TXB2 and mPAP. PLA2 induced release of inflammation mediators, plays an important role in the mechanism of the acute hypoxic pulmonary arterial hypertension.

Acute Disease↗

Phase I clinical trial of cefditoren pivoxil (ME 1207): pharmacokinetics in healthy volunteers.

Pharmacokinetics of ME1207 were evaluated in 5 groups of healthy adult male volunteers given single preprandial administration of 100, 200 and 300 mg; postprandial administration of 200 mg; and administration of 200 mg every 12 h for 7 consecutive days. Blood drug concentrations were determined by HPLC and bioassay after oral single administration of 100, 200 and 300 mg before meals. Serum concentrations and major pharmacokinetic parameters (Cmax, Tmax, AUC and T1/2 Ke) determined by these two methods were comparable. Cmax and AUC determined by bioassay after postprandial administration were greater than those determined after preprandial administration. Blood concentrations determined 1.5 and 12 h after each administration, during repeated administration of 200 mg every 12 hours for 7 days, were always about 2.5 and 0 mg/l, respectively, indicating that the drug is not accumulated in the body. Within 24 hours after administration of 100, 200 and 300 mg, 19.93 +/- 5.20, 20.24 +/- 3.72 and 21.29 +/- 5.47%, respectively, of the dose were excreted into urine in an unchanged form.

Absorption↗

Ultrastructural investigation of calcification and ossification in experimental fracture healing with special reference to osteogenic role of fibroblasts.

OBJECTIVE: To investigate ultrastructurally the process of calcification and ossification in experimental fracture healing. METHODS: A standardized fracture of the radius was made in rabbits. Undecalcified callus tissues from different fracture regions were subjected to ultrastructural observation under transmission electron microscope. RESULTS: In the mitochondria and membrane-bound vesicles of the fibroblasts, osteoblasts and chondrocytes, high electron density calcium granules were seen. These granules provided raw materials for the deposition of calcium salt crystals. Around these cells, round, oval or irregularly shaped matrix vesicles could also be discerned, and they became calcified and formed flocculent calcospherules. Then in the Type I collagen fibrils around the fibroblasts and osteoblasts, and in the Type II collagen fibrils around the chondrocytes, calcium salt crystals also appeared. Innumerable flocculent calcospherules and calcified collagen fibrils coalesced together, expanded and finally turned into pieces of bone tissues. The fibroblasts also possessed the indispensable prerequisites for calcification and ossification in fracture healing. They either transformed into osteocytes or degenerated, perished and eventually were replaced by bone tissues. CONCLUSIONS: Sequence of events taking place in calcification and ossification in experimental fracture healing was depicted. Calcification of matrix vesicles and collagen fibrils triggered these processes. Evidence of osteogenic role played by fibroblasts was provided.

Animals↗

Preliminary study of the effects of metoprolol and propafenone on ventricular arrhythmia with positive ventricular late potential.

OBJECTIVE: To compare the effects of metoprolol and propafenone in patients with ventricular arrhythmia (VA) of positive ventricular late potential (VLP) and to discuss the effect of medicine on high risk VA. METHODS: 30 A total of 128 patients (78 males and 50 females) with VA of positive VLP were randomly divided into 3 groups. Groups A and B were given metoprolol and propafenone respectively, group C was given vitamin C as placebo. Twenty-four hours dynamic electrocardiogram and VLP were examined before treatment and 4 weeks after treatment. RESULTS: Propafenone could effectively control VA but could not reverse positive VLP to negative meanwhile it had proarrhythmia effect (2/40), metoprolol could effectively control VA (38/46) and reverse positive VLP to negative (39/46) with no obvious side effects. The dosage from 50 to 100 mg/day made no difference. VA and VLP had no significant changes in group C. CONCLUSIONS: Metoprolol is superior to other medicine for VA of positive VLP when the patients have no contraindication of preceptor blocking agents.

Adult↗

Genital Ureaplasma urealyticum infection in varicocele-related infertility.

OBJECTIVE: To assess the existence of a possible infectious factor in varicocele-related infertility. METHODS: A total of 925 seminal plasmas from 590 infertile men with varicocele and 335 infertile patients without palpable varicocele were cultured for Ureaplasma urealyticum infection, and routine semen analysis was made. RESULTS: The infection rate of Ureaplasma urealyticum in seminal plasmas was 48.22%. The asymptomatic genital infection of Ureaplasma urealyticum was traced in 329 (55.76%) varicocele men and 117 (34.93%) infertile patients without varicocele (control group). A significant quantitative difference in the incidence of genital Ureaplasma urealyticum infection between the varicocele and control group was observed (P < 0.005) and asthenozoospermia was significantly more prevalent in the patients with varicocele than in the other patients (P < 0.05). CONCLUSIONS: Genital Ureaplasma urealyticum infection may play a role in varicocele-related infertility. To prevent future infertility, men with both varicocele and genital Ureaplasma urealyticum infection may benefit from early evaluation and treatment.

Adult↗

[Effects of TIMP-2 gene transfection on biological behaviors of a metastatic human lung carcinoma cell line].

OBJECTIVES: To explore the suppressive effects of tissue inhibitor of metalloproteinase 2 (TIMP-2) on malignant phenotype of human carcinoma cells and to evaluate its potential application in cancer gene therapy. METHODS: A man malian expression vector containing TIMP-2 cDNA was constructed and transfected into a metastatic human lung carcinoma cell line PG. In vitro and in vivo tests such as Northern blotting, immunohistochemistry as well as x enografting in nude mice experiment were used to analyse expression levels of TIMPs and MMPs, in vitro and in vivo behaviors of the tumor cells before and after the gene transfection. RESULTS: After transfection, the TIMP-2 mRNA expression was upregulated significantly. Changes, in some malignant phenotypes of the transfectants were seen. For instance, the abilities of in vitro invasion through Matrigel, colony formation on soft agar, tumorigenecity as well as spontaneous metastasis in nude mice were remarkably decreased. Immunohistochemical staining and in situ hybrydization showed that MMP2, MMP9, TIMP-1 and TIMP-2 were expressed by both tumor cells and stromal cells, with stronger staining at the site of tumor invasion. CONCLUSION: Up-regulation of TIMP-2 in tumor cells could suppress their expression of malignant phenotype and could be used for cancer therapy.

Animals↗

[Elimination of cholesterol in human endothelial cells].

OBJECTIVE: To investigate what role the endothelial cell interfacing with blood components to play in cholesterol metabolism. METHODS: Isotopelabeling technique, Gas Chromatography/Mass Spectrometry and Western blotting were used to measure the presence of 27-oxygenated cholesterol in medium and the presence of sterol 27-hydroxylase in endothelium. RESULTS: When human endothelial cells were cultured in a medium containing fetal calf serum, there was a significant accumulation of 27-hydroxycholesterol and 3 beta-hydroxy-5-cholesteneic acid, products of cholesterol metabolism, in the medium. The rate of formation of these products almost increased linearly with time of cultivation. After addition of 100 micrograms of extraneous cholesterol to the medium, the accumulation of 27-hydroxy-cholesterol and 3 beta-hydroxy-5-cholesteneic acid increased significantly. Addition of more cholesterol did not further increase the formation of 27-hydroxy-cholesterol and caused a decrease in the formation of 3 beta-hydroxy-5 cholesteneic acid. The presence of sterol-27-hydroxylase in the endothelium was demonstrated by Western blotting. CONCLUSION: Cultured human endothelium from umbilical veins are able to convert exogenous cholesterol into 27-hydroxy-cholesterol and 3 beta-hydroxy-5-cholesteneic acid. Furthermore, the cells are able to transport these products from the cells into the medium.

Cells, Cultured↗

[A study on the setting-up a high-risk scoring system for neonatal adverse outcomes].

In order to popularize the technique of risk approach to neonates among child health care providers in rural areas, data of surveillance for risk factors of the three major adverse outcomes in 1,116 neonates in rural areas of Zhangye prefecture, Gansu Province, China were analyzed, and two comprehensive scoring method of "whole risk factors" and "significant risk factors", to identify neonates at high-risk, were established and compared with standardized partial coefficient weighting of multiple logistic regression. The "whole risk factors" method of comprehensive scoring is recommended by this study as criteria for identification of high-risk neonates.

Female↗

O6-Methylguanine-DNA methyltransferase protein levels in pediatric brain tumors.

Chloroethylnitrosoureas (CENUs) are commonly used in the treatment of pediatric and adult central nervous system (CNS) tumors. The antitumor activity of CENUs has been hypothesized to be due to an alkylation occurring at the O6-position of guanine in DNA. The DNA repair protein O6-methylguanine-DNA methyltransferase (MGMT) is responsible for the repair of these potentially cytotoxic lesions and may underlie tumor resistance to CENUs. The current study is the largest report of MGMT levels among newly diagnosed pediatric CNS tumors and the only study that has quantitated MGMT by both biochemical and Western immunoblot assays. Our results show a good correlation between the two methods (r = 0.66). Medulloblastoma/primitive neuroectodermal tumor and ependymoma had the highest level of MGMT, followed by high-grade glioma and low-grade glioma. These data may provide a guide to the use of CENUs in the treatment of pediatric CNS tumors.

Adolescent↗

In vitro antineoplastic activity of a novel lanthionine-containing peptide.

It has been a long-term goal to discover peptides that can kill tumor cells while sparing normal tissues. Lan-7 is a novel, chemically stable peptide structurally related to somatostatin that contains a lanthionine bridge between the two cysteines in the peptide; TT-232 is a less stable analogue containing a disulfide bridge. The antitumor activity of Lan-7 was examined, relative to that of TT-232 and the clinically used analogue octreotide, against a panel of malignant human tumor cell lines and normal human hematopoietic precursors. Lan-7 was cytotoxic to all four tumor cell lines, with IC50 values ranging over a 2-fold range from 16 to 36 microM. The potency of Lan-7 was comparable to that of TT-232, and both of these agents were two to three times more potent than octreotide. At concentrations that were highly cytotoxic to tumor cells, Lan-7 produced no significant toxicity to normal human hematopoietic precursors. Lan-7 induced apoptosis in human ovarian carcinoma 2008 cells over the same concentration range at which it produced cytotoxicity, but it did so without activating G1, S, or G2 checkpoints, given that it produced no perturbation of cell cycle phase distribution. Cells engineered to overexpress P-glycoprotein were not more resistant to Lan-7 than isogeneic cells not expressing the mdr1 gene. These results make Lan-7 of interest as a potential cancer chemotherapeutic agent.

ATP Binding Cassette Transporter, Subfamily B, Mem↗

[Study of dermatomycosis and survey of pathogens in troops of Hainan area].

Subtropical area is the prevalent area of dermatomycosis with natural conditions suptable for the growth and proliferation of fungi causing suterficial dermatomycosis. Dermatomycosis not only brings about certain sufferings to the military personnel in peacetime, but also causes nonbattle loss in manpower in war time. In the present work, a survey of dermatomycosis in Hainan subtropical area of China and isolation of the pathogens were carried out. The results were as follows: The morbidity of superficial dermatomycosis was 34.1% and it was manifested clinically as tinea pedis, tinea versicolor, tinea corporis, tinea axillaris, tinea cruris, etc.; The main pathogen causing dermatomycosis in this area was Trichophyton rubrum which accounted for 50.4% of the pathogens isolated and the next was Trichophyton gypseum which accounted for 20.3%; Trichophyton rubrum could cause dermatomycosis of many sites of the body in this area, but the main lesious were tinea corporis and tinea cruris.

Adult↗