Objective　To study the effects of domestic incadronate(ICD) on osteoclastic bone resorbing lacunae. Methods　Rabbit's osteoclastes were coincubated with bone slices and microphotographed,microdensitometric scanned and analyzed by computer image analysis system. Results　ICD (0.5，5 and 50 μmol/L) caused dose-dependent reduction in the number of osteoclastic bone resorbing lacunae. The inhibitory effect ICD (5 μmol/L) was more remarkable than that of aminopropanediphosphonate (APD). Both ICD and APD reduced the surface area of osteoclastic bone resorbing lacunae. The effect of ICD was stronger than that of APD. Conclusion　ICD directly suppresses osteoclastic bone resorption and may be effective in osteoporosis.

AIM\ To study whether total astragalosides(TA) induces apoptosis in human hepatoma cells and its mechanism of action. METHODS\ The human hepatoma HepG2 and Bel 7404 were cultured with TA (20,40 and 80 mg?L -1 ) for 6 days and DNA fragmentation and the expression of wtp53 protein were determined by flow cytometry. RESULTS\ HepG2 and Bel 7404 cell apoptosis induced by TA(20,40 and 80 mg?L -1 ) were found by flow cytometry. The apoptotic peak of HepG2 cells increased in dose dependent manner in the range from 4 1% to 74 5%; The apoptotic peak of Bel 7404 cells also increased from 4 5% to 50 5%. The expression of wtp53 in HepG2 cells and Bel 7404 cells treated with TA (80 mg?L -1 ) were upregulated. CONCLUSION\ TA may induce apoptosis in HepG2 cells and Bel 7404 cells, its mechanism of action might be associated with upregulating the expression of wtp53.

Influences of the concentrations of luminol, zymosan & cells and opsonizing time of zymosan on luminol-dependent chemiluminescence( LDCL ) of peritoneal macrophages ( PM?) in rats were investigated by the method of orthogonal analysis. The result showed that the best levels were 100?mol/L of luminol, 10 mg/ml of zymosan, 5? 10~6/ml of cells and 45 min for opsonizing time. The LDCL of PM? was enhanced by incubation with TGP for 12 h in a concentration-dependent manner in the range of 0.09-2.25 ?g/ml of TGP, but LDCL was diminished with the concentration of 11.25 ?g/ml of TGP . The concentration-effect curve seems to be bell-shaped. The data suggested that TGP had two-sided regulatory effects on the LDCL of PM? in rats, depending on the concentration used.

Using the fluorescence method, the effect of Luteolin ( Lut) on H2O2 release of peritoneal macrophages(M(?)s) in rat was studied. The results showed that H2O2 release of peritoneal M(?)s stimulated by op-sonized Zymosan was reduced by in vitro treatment of Lut. The inhibitory effect of Lut is in a concentration-dependent manner over the range of 4 ? 10-7-10-5mol/L. When M(?)s was cultivated with Lut for 4 h, the inhibitory effect of Lut was the most obvious.

AimTo study the effect of the total extract of astragalosides(TEA) on the growth, AFP secretion and γ-GT activity of human hepatoma cells invitro.Methods The human hepatoma HepG2 and Bel-7404 cells were cultured with TEA 5～160 mg · L-1 for 6 days. Anti-hepatoma activity was measured by MTT method. AFP was assaysed by ELISA and γ-GT was determined by enzyme-substrate method. Results The growth of the human hepatoma HepG2 and Bel-7404 cells and the secretion of AFP of HepG2 cells were reduced significantly by TEA 5～160 mg· L-1. The γ-GT activity of HepG2 cells was inhibited and its ALB content was increased by TEA 20, 40 and 80 mg · L-1. The γ-GT activity of Bel-7404 cell was inhibited and its ALB content was increased byTEA 40 and 80 mg · L-1 Conclusion These results suggest that TEA has inhibitory effects on the growth, AFP secretion and γ-GT activity of human hepatoma cells.

Total glucosides of paeony (TGP, 50 mg/kg 7d, ig) could enhance the episode duration of slow-wave sleep (SWS) in normal rats, and restore the sleep parameters in the insomniac rats induced by caffeine ( 1 2. 5 mg/kg 7 d,ip)nearly to the normal level. It (50 mg/kg 3 d,ig) also increased significantly thetotal time of SWS and paradoxical sleep (PS) in the swimming rats (water temperature 25?1℃, swimming time 30 min). These results suggest that TGP probably improve the sleep of rats under the different states.

Objective: To study the effect of total flavonoids of astragalus (TFA) on adjuvant arthritic (AA) rats and its mechanism. Methods: The volume of non-injected hind paw of AA rats, serum malondialdehyde (MDA) content, interleukin-1(IL-1) and nitrite (NO - 2) produced from articular synoviocytes were measured. Results: It was obseved that serum levels of MDA and the levels of IL-1 and NO - 2 from synoviocytes increased in AA rats, and the degree of the secondary inflammatory reaction of AA rats appeared to be directly correlated with serum levels of MDA and IL-1. Treatment of whole (d0～27) or partial (d12-18 or d18-24) course of AA rats with TFA (20 mg/kg/d,ig) could not only markedly inhibit the inflammatory reaction in AA rats, but also reduce their enhanced serum lipid peroxides (LPO), IL-1 and NO production from synoviocytes. Conclusion: TFA has significant therapeutic effects on AA rats, which might be related to both of anti-oxidative effect and the reduced production of IL-1 and NO from synoviocytes.

The pharmacokinetics of Luteolin ( Lut ) solution in rabbits and rats was investigated. Lut in plasma, bile and urine as well as protocatechuic acid (which is a product of Lut) in plasma and urine were determined by fluorescence spectrophotometry. A curve with multiple peaks was fitted to the data of plasma concentration versus time, employing a nonlinear program developed with an IBM-PC computer. The results indicated that the data set obtained with 30 mg /kg doses by iv fitted well to a peculiar open 3 compartment model involved in the enterohepatic recirculation of the drug and the undulations of the drug concentration.The essential pharmacokinetics parameters (mean?SD) were as follows; The t1/2 values for the ?-phase and ?-phase were about 0.18?0.01 h and 1.66?0.24 h respectively. The apparent volume of distribution ( Vd) was about 1.43? 0.45 L?kg-1. The reabsorption rate constant ( Ka ) was 0.465? 0.08 h-1 The reabsorption percent ( F' ) was about 6.9? 2.1% . The elimination rate constant was 1.124?0.35 h-1. The clearance was 588?113 ?g?h-1?kg-1. This study indicated that Lut was rapidly removed from the blood by both kidney and liver where Lut was excreted by way of the bile into intestine from which it Was reabsorbed. The 12 h urine excretion of Lut in rabbits was in the order of 37.7% of total iv dose. In rats, the 6 h bile excretion of Lut was about 11.2% of that total iv dose. A comparison of the C-T curve of PCA with of Lut suggested that PCA was the one of the products of Lut.In rats, the 3H-Lut orally administered was widely distributed in the tissues, the concentrations being higher in liver and kidney.

Aim To study the effects of total extract of astragalus(TEA) on activating the primary cultured hepatic stellate cells(HSC) and synthesizing collagen. Methods Livers of adult rats were perfused by pronase E and collagenase in situ, HSC and Kupffer cell (KC) were isolated by centrifugation with 18% Nycodenz. The subcultured HSC were induced by Kupffer cell conditioned medium(KCCM) and were incubated with 5～ 80 mg?L -1 TEA for 6 days. The proliferation of the cells was measured by 3H TdR and the production of collagen by 3H Proline.Results TEA (10～ 40 mg?L -1 ) could suppress the proliferation of hepatic stellate cells and TEA(40～ 80 mg?L -1 ) could suppress the production of collagen. Conlusion The suppression of hepatic stellate cell proliferation and the collagen's production by the TEA may be one of the mechanisms for depressing the hepatic fibrosis by the TEA.

The acute iv and ig LD50 of sudoxicam synthesized by Shanyan Ph-armaceutic College was calculated to be 135?10. 7 and 320 ? 96 mg/kg in mice. In polyarthritic rats, Sud at 2 and 4 mg/kg/d for 28 days did not induce changes in serum AKP, SGPT, BUN the morphal-ogic characteristics of the gastrointestinal tract, liver and kidney. In 3 dogs orally given Sud 16 mg/kg/d for 5 consecutive days, 2/3 died at days 10 to 13. In other 3 dogs given Sud 16 mg/kg/d every other day, plasma concentrations of Sud were determined by ultra violet spectrophotometry. It was found that on the days 10 to 20 , the concentration time curves had attained a intoxicant steady state with plasma sudoxicam concentrations as high as 44. 9 ? 73. 9?g/ml ,and all of them died after 17~25 days. Their bleeding time and coagu- lation time were prolonged to 2 or 3 times of the control and serum BUN was increased. In one dog autopsy revealed the interstitial inflammation of the kidney and small local necrosis of the live, but not in other dogs.Gastric ulceration in rats can be produced by the oral administration of verious doses of Sud. The UD50 of Sud was 15.47mg/kg. It was found that the gastric ulceration in rats is related to the plasma levels