The study is to investigate the pharmacokinetics of S-1 capsule (tegafur, gimeracil and potassium oxonate capsule) in patients with advanced gastric cancer after single and multiple oral administration. Twelve patients with advanced gastric cancer were recruited to the study. The dose of S-1 for each patient was determined according to his/her body surface area (BSA). The dose for single administration was 60 mg every subject. The dose for multiple administration for one subject was as follows: 100 mg x d(-1) or 120 mg x d(-1), 28-days consecutive oral administration. The pharmacokinetic parameters of tegafur, 5-fluorouracil, gimeracil, potassium oxonate and uracil after single oral administration were as follows: (2,207 +/- 545), (220.0 +/- 68.2), (374.9 +/- 103.0), (110.5 +/- 100.8) and (831.1 +/- 199.9) ng x mL(-1) for Cmax; (11.8 +/- 3.8), (4.4 +/- 3.3), (7.8 +/- 5.1), (3.1 +/- 0.9) and (8.8 +/- 4.1) h for t1/2, respectively. After six days oral administration, the average steady state plasma concentrations (Cav) of tegafur, 5-fluorouracil, gimeracil, potassium oxonate and uracil were (2,425 +/- 1,172), (73.88 +/- 18.88), (162.6 +/- 70.8), (36.89 +/- 29.35) and (435.3 +/- 141.0) ng x mL(-1), respectively, and the degree of fluctuation (DF) were (1.0 +/- 0.2), (2.5 +/- 0.4), (3.1 +/- 0.8), (2.4 +/- 0.8) and (1.5 +/- 0.3), respectively. The cumulative urine excretion percentage of tegafur, 5-fluorouracil, gimeracil and potassium oxonate in urine within 48 h were (4.2 +/- 2.8) %, (4.7 +/- 1.6) %, (18.5 +/- 6.0) % and (1.7 +/- 1.2) %, repectively, after single oral administration of S-1. The results exhibited that tegafur had some drug accumulation observed, and gimeracil, potassium oxonate, 5-fluorouracil and uracil had no drug accumulation observed.

Carbon-nitrogen lyases (E.C.4.3) are a group of enzymes that release ammonia, amidine or amino group etc, and also show ability to form double bond or ring structure. Specifically, enzymes forming amino group are called amine-lyases (E.C.4.3.3), which are critical in the industrial production of many medicine intermediates. In this review is a summary of four major amine-lyases in terms of their source, enzymatic characteristics and their applications in preparation of pharmaceutical intermediates.

The study is to investigate the pharmacokinetics of S-1 capsule (tegafur, gimeracil and potassium oxonate capsule) in patients with advanced gastric cancer after single and multiple oral administration. Twelve patients with advanced gastric cancer were recruited to the study. The dose of S-1 for each patient was determined according to his/her body surface area (BSA). The dose for single administration was 60 mg every subject. The dose for multiple administration for one subject was as follows: 100 mg x d(-1) or 120 mg x d(-1), 28-days consecutive oral administration. The pharmacokinetic parameters of tegafur, 5-fluorouracil, gimeracil, potassium oxonate and uracil after single oral administration were as follows: (2,207 +/- 545), (220.0 +/- 68.2), (374.9 +/- 103.0), (110.5 +/- 100.8) and (831.1 +/- 199.9) ng x mL(-1) for Cmax; (11.8 +/- 3.8), (4.4 +/- 3.3), (7.8 +/- 5.1), (3.1 +/- 0.9) and (8.8 +/- 4.1) h for t1/2, respectively. After six days oral administration, the average steady state plasma concentrations (Cav) of tegafur, 5-fluorouracil, gimeracil, potassium oxonate and uracil were (2,425 +/- 1,172), (73.88 +/- 18.88), (162.6 +/- 70.8), (36.89 +/- 29.35) and (435.3 +/- 141.0) ng x mL(-1), respectively, and the degree of fluctuation (DF) were (1.0 +/- 0.2), (2.5 +/- 0.4), (3.1 +/- 0.8), (2.4 +/- 0.8) and (1.5 +/- 0.3), respectively. The cumulative urine excretion percentage of tegafur, 5-fluorouracil, gimeracil and potassium oxonate in urine within 48 h were (4.2 +/- 2.8) %, (4.7 +/- 1.6) %, (18.5 +/- 6.0) % and (1.7 +/- 1.2) %, repectively, after single oral administration of S-1. The results exhibited that tegafur had some drug accumulation observed, and gimeracil, potassium oxonate, 5-fluorouracil and uracil had no drug accumulation observed.
Administration, Oral ; Adult ; Aged ; Antimetabolites, Antineoplastic ; pharmacokinetics ; Capsules ; Drug Combinations ; Female ; Fluorouracil ; blood ; urine ; Humans ; Male ; Middle Aged ; Neoplasm Staging ; Oxonic Acid ; blood ; pharmacokinetics ; urine ; Pyridines ; blood ; urine ; Stomach Neoplasms ; blood ; metabolism ; pathology ; urine ; Tegafur ; blood ; pharmacokinetics ; urine ; Uracil ; blood ; urine

Objective To investigated the effects of combined arsenic trioxide(ATO) and resveratrol(Res)on the viability of NB4 human leukemia cells. Methods NB4 human leukemia cell was used in this experiment.Cells were cultured in ATO (0,0.1875,0.3750,0.7500, 1.1250, 1.5000,2.2500,3.0000,5.0000 μmol/L) and Res (0, 1.5625,3.1250,6.2500, 12.5000, 18.7500,25.0000,37.5000,50.0000 μmol/L). Cell viabilities were measured by MTT in different treatment groups. Half inhibitory concentration(IC50) was calculated. The ratio of concentration of ATO and Res 1.5∶ 18,1.5∶ 25,1.5∶ 35 was added to cells, and the combination index(CI) was calculated. The level of ROS in control, ATO( 1.5000 μmol/L), Res(25.0000 μmol/L) and ATO(0.9000 μmol/L) + Res( 12.5000μmol/L) groups was measured by chemiluminescence assay. Results ①ATO( ≥0.7500 μmol/L) reduced the viability of NB4 cells in a concentration-dependent manner(P ＜ 0.05 ), and IC50 was (1.78 ± 0.11 )μmol/L. ②)Res (≥18.7500 μ mol/L) dose-dependently decreased the viability of NB4 cells (P ＜ 0.05 ), and IC50 was ( 18.71 ±0.18)μ mol/L. ③Combination of ATO and Res showed an antagonistic effect on NB4 cells viability. ④The ROS in Res group( 1670.55 ± 13.97) was significantly lower than that in control group(2345.88 ± 14.48,P ＜ 0.05). The ROS in ATO group (3092.42 ± 94.84) was significantly higher than that in control group(P ＜ 0.05). The ROS in ATO + Res group (1860.27 ± 15.99) was significantly lower than that in ATO group(P ＜ 0.05). Conclusions NB4 cell survival rate can be decreased by ATO and Res. The combination of arsenic trioxide and Res presents an antagonistic effect on NB4 cell viability, in part by reducing intracellular ROS formation.

Objective: : The present study aimed to investigate the clinical characteristics of electrolyte imbalance in patients with moderate to severe traumatic brain injury (TBI) who underwent craniotomy and its influence on prognosis. Methods: : A total of 156 patients with moderate to severe TBI were prospectively collected from June 2019 to June 2021. All patients underwent craniotomy and intracranial pressure (ICP) monitoring. We aimed to explore the clinical characteristics of electrolyte disturbance and to analyze the influence of electrolyte disturbance on prognosis. Results: : A total of 156 patients with moderate and severe TBI were included. There were 57 cases of hypernatremia, accounting for 36.538%, with the average level of 155.788±7.686 mmol/L, which occurred 2.2±0.3 days after injury. There were 25 cases of hyponatremia, accounting for 16.026%, with the average level of 131.204±3.708 mmol/L, which occurred 10.2±3.3 days after injury. There were three cases of hyperkalemia, accounting for 1.923%, with the average level of 7.140±1.297 mmol/L, which occurred 5.3±0.2 days after injury. There were 75 cases of hypokalemia, accounting for 48.077%, with the average level of 3.071±0.302 mmol/L, which occurred 1.8±0.6 days after injury. There were 105 cases of hypocalcemia, accounting for 67.308%, with the average level of 1.846±0.104 mmol/L, which occurred 1.6±0.2 days after injury. There were 17 cases of hypermagnesemia, accounting for 10.897%, with the average level of 1.213±0.426 mmol/L, which occurred 1.8±0.5 days after injury. There were 99 cases of hypomagnesemia, accounting for 63.462%, with the average level of 0.652±0.061 mmol/L, which occurred 1.3±0.4 days after injury. Univariate regression analysis revealed that age, Glasgow coma scale (GCS) score at admission, pupil changes, ICP, hypernatremia, hypocalcemia, hypernatremia combined with hypocalcemia, epilepsy, cerebral infarction, severe hypoproteinemia were statistically abnormal (p<0.05), while gender, hyponatremia, potassium, magnesium, intracranial infection, pneumonia, allogeneic blood transfusion, hypertension, diabetes, abnormal liver function, and abnormal renal function were not statistically significant (p>0.05). After adjusting gender, age, GCS, pupil changes, ICP, epilepsy, cerebral infarction, severe hypoproteinemia, multivariate logistic regression analysis revealed that hypernatremia or hypocalcemia was not statistically significant, while hypernatremia combined with hypocalcemia was statistically significant (p<0.05). Conclusion : The incidence of hypocalcemia was the highest, followed by hypomagnesemia, hypokalemia, hypernatremia, hyponatremia and hypermagnesemia. Hypocalcemia, hypomagnesemia, and hypokalemia generally occurred in the early post-TBI period, hypernatremia occurred in the peak period of ICP, and hyponatremia mostly occurred in the late period after decreased ICP. Hypernatremia combined with hypocalcemia was associated with prognosis.

OBJECTIVETo evaluate the clinical value of (89)SrCl(2) (Ke xing Inc, Shanghai) as a palliative therapy modality for cancer patients with bone metastasis.

METHODSIn 504 cancer patients with painful limitation of movement due to bony metastasis, a dose of 1.48-2.22 MBq/kg (40-60 uCi/kg) iv infusion of (89)SrCl(2) was given.

RESULTSIn 97 patients (19.2%) there was no improvement in pain and life quality, 298 patients (59.1%) showed mild to moderate improvement (moderately effective), 109 patients (21.6%) became free of pain and were subsequently fully ambulatory (markedly effective). The pain relief appeared from D1-D46 after (89)SrCl(2) administration, most frequently from D5-D14. The palliative effect could last for about 56 days to 13 months. Repeated bone scans of some patients showed that the metastatic foci in the bone became smaller or even disappeared gradually after the administration of (89)SrCl(2). Approximately 55% of patients experienced grade I approximately III bone marrow depression attributable to (89)SrCl(2), which would return to the pre-treatment level within 3 approximately 9 months.

CONCLUSION(89)SrCl(2) is effective and safe for the relief of bone pain and improvement of quality of life in cancer patients with painful bony metastasis.

Adult ; Aged ; Aged, 80 and over ; Bone Neoplasms ; complications ; radiotherapy ; secondary ; Breast Neoplasms ; pathology ; Female ; Humans ; Lung Neoplasms ; pathology ; Male ; Middle Aged ; Pain Measurement ; Pain, Intractable ; etiology ; radiotherapy ; Quality of Life ; Strontium Radioisotopes ; therapeutic use

OBJECTIVETo assess the value of fluorine-18 fluorodeoxyglucose (FDG)-positron emission tomography (PET) in carcinoma of the esophagogastric junction.

METHODSFrom December 1998 to April 2002, 27 patients were imaged with FDG-PET and FDG avid masses in the esophagogastric junction were found in every patient. FDG-PET data was analyzed by visual method and standardized uptake value (SUV). FDG-PET results were compared with pathological results and follow-up survey.

RESULTS16 carcinomas of the esophagogastric junction and 11 non-specific FDG-avid masses of normal stomach were all considered malignant by visual method. Maximum and mean Standard uptake value (SUV) of cancer were 6.71 +/- 2.75 and 5.46 +/- 2.31, respectively; SUVmax and SUVmean of non-specific FDG avid mass were 2.99 +/- 0.67 and 2.38 +/- 0.51 respectively; SUV of cancer was higher than that of non-specific FDG avid mass (Z = -4.171, Z = -4.195, P < 0.01).

CONCLUSIONSFDG-PET has limited value in differentiating carcinoma of the esophagogastric junction from non-specific FDG avid mass of normal stomach.

Adult ; Aged ; Diagnosis, Differential ; Esophagogastric Junction ; diagnostic imaging ; Female ; Fluorodeoxyglucose F18 ; Humans ; Male ; Middle Aged ; Positron-Emission Tomography ; Radiopharmaceuticals ; Retrospective Studies ; Stomach Neoplasms ; diagnostic imaging

OBJECTIVETo explore whether there exists coincidence of the most appearing time of clinical features of liver cancer at different longitude and latitude, according to the law of field equation and the theory of warpage of space time by Einstein.

METHODSThree regions with different longitude and latitude were selected randomly and sampled. There were 36 items altogether, including 12 clinical items, which were used to imitate the yearly cycle cosine curve. The acorphases and the ratioes of amplitudes and means were compared to justifying whether they were in the same range.

RESULTSAll the acorphases of 36 items appeared between -90.1degrees to -207.5 degrees (from april to july), existing in one third of the same range, in which 13 items occurred rhythmly (P<0.05). The image acorphases of liver cancer at the early and middle stage and gamma-glutamyl transpeptidase acorphase appeared between -98.5 degrees to -148.2 degrees (from april to may), in which 5 items occurred rhythmly (P<0.05).

CONCLUSIONIt is the same mode of the yearly biologcal cycle for liver cancer malignant growth within the most appearing time (from april to july). It will increase the detecting rate of liver cancer at the early and middle stage during this time (especially from april to may).

Carcinoma, Hepatocellular ; pathology ; Cell Cycle ; physiology ; Chronobiology Phenomena ; Hepatocytes ; physiology ; Humans ; Liver Neoplasms ; pathology ; Mathematical Computing ; Periodicity

BACKGROUNDIntermediate filament (IF) proteins have been thought to play a role in nuclear centration, organelle movement and maintenance of cell shape. dl-praeruptorin A (Pd-Ia), a novel Ca2+-influx blocker and K+-channel opener isolated from Chinese traditional herbal medicine Qian-Hu, has been demonstrated to inhibit expression of apoptosis related proteins and reduce the level of proinflammatory factors in ischemia/reperfusion myocardiocytes. Morphologically, whether Pd-Ia effects myocardiocyte IFs remains unclear. The purpose of this study was, for the first time, to evaluate the in vivo effects of Pd-Ia on IF desmin and vimentin content in order to further explore its cardioprotection against ischemia and elucidate its mechanism of action.

METHODSRats underwent a 30 minutes coronary occlusion followed by 120 minutes reperfusion. Assessment of desmin and vimentin content of myocardiocytes was performed by immunohistochemistry, Western blot, Hematoxylin-Eosin staining and densitometry.

RESULTSPretreatment with i.v. infusion of Pd-Ia prior to ischemia significantly increased desmin and vimentin content and alleviated defects caused by the ischemia/reperfusion insult, e.g. with Pd-Ia at a dose of 0.5 or 1.0 mg/kg, integrated density values of desmin were increased from 61 478 +/- 10 074 to 177 408 +/- 10 395 and 195 784 +/- 20 057, and vimentin from 59 189 +/- 19 853 to 164 781 +/- 19 543 and 185 696 +/- 20 957 (P < 0.01, vs placebo), respectively. The recovery of desmin seemed to be stronger and appeared earlier than that of vimentin.

CONCLUSIONPd-Ia protectively increased IF desmin and vimentin content in ischemia/reperfusion myocardiocytes, which might be partially responsible for its cardioprotection against ischemia.

Animals ; Blotting, Western ; Calcium ; metabolism ; Coumarins ; pharmacology ; Desmin ; analysis ; Dose-Response Relationship, Drug ; Drugs, Chinese Herbal ; pharmacology ; Female ; Immunohistochemistry ; Male ; Myocardial Ischemia ; drug therapy ; metabolism ; Myocardial Reperfusion Injury ; prevention & control ; Myocytes, Cardiac ; chemistry ; drug effects ; pathology ; Rats ; Rats, Wistar ; Vimentin ; analysis

Objective To investigate the relationship between the number of colonies and the luminous intensity of two kinds of platelets contamination bacteria,Escherichia coli(ECO)and Pseudomonas aeruginosa(PAE)in single platelets, plasma and phosphate buffered salines(PBS), and to explore their growth and proliferation in different biological fluid media.Methods The two luminescent bacteria were constructed before the correlations between the number of colonies and the luminous intensity in different media in vitro were observed with a small animal bioluminescence imaging instrument, and correlation analysis was carried out.By recording the luminous intensity at serial time points in different media, a growth curve was drown to reflect the proliferation of bacteria.Results There was a significant positive correlation between the number of colonies and luminous intensity of ECO and PAE in single platelets,plasma and PBS.The larger the number of colonies was,the stronger the luminous intensity was.The results indicated that single platelets significantly inhibited the proliferation of ECO and PAE,and that plasma also had some inhibitory effect,but not so strong.Conclusion For the two luminous bacteria,luminous intensity can represent the growth and proliferation of bacteria.Single platelets have obvious inhibitory effect on the growth of ECO and PAE, and the plasma also has some inhibitory effect, but the effect is not so strong as that of single platelets.