The iv is a new hepatograp the authors, accordi of the reticulo-endo suspension of TABAChic agent, designed by ng to the phagocytosis thelial tissue. In this paper, we localized the distribution of sus-pension particles of [iasI]TABAC in rat liver by autoradiography. The silver grains produced by[125I]TABAC were concen-trated in and around Kupffer cells. This is a direct evidence to prove our design a successful one. The ratio of numbers of Ag grains with 2 doses (3.1)was smaller than that of 2 initial doses (4). The values of [125I]TABAC_positive Kupffer cells vs time (from 15 s t0 6 d) coincided with that of TABAC content in liver vs time deter-mined by a previous pharmacokinetic study.
To study the antitumor activity of sobuzoxane (Sob) in combination with doxorubicin (Dox) and the effect of Sob on Dox-induced cardiotoxicity.DBA/2 mice bearing transplanted leukemia P388 were given i.v. Dox 2 mg.kg-1.d-1 for 3 d, 4 mg.kg-1.d-1 for 1 d combined with ig Sob 20, 40 mg.kg-1.d-1 for 7 d. The increase in life span (ILS) of each group was recorded in 30 d. The myocardium of moribund mice was examined by transmission electron microscopy.The ILS of combination therapeutic groups of Sob with Dox was 48.7%, 57.3%, 59.0%, and 62.4% respectively, which were 30%-90% higher than the sum of ILS of two groups treated with Dox and Sob separately (P < 0.01). The ultrastructural injury of cardiomyocytes of P388-bearing mice caused by combination chemotherapy with Dox plus Sob was markedly attenuated compared with Dox alone.Sob with Dox exhibited an antitumor synergistic effect on leukemia P388, and the cardiotoxicity of Dox was reduced by Sob.
Mice were given ig L-4-oxalysine (I-677) 10, 50, and 100 mg.kg-1.d-1 for 7 d. On d 8 the hepatocytes showed accumulation of lipid droplets followed by loss of matrices in cytoplasm. The total area of lipid droplets was far less than 25% of mean section of hepatocytes. The injury of mitochondria and RER was only found in the groups of medium and high dose. The lipidoses and regional topolysis of cytoplasm graduated away at same pace. After 4 wk the hepatocytes were restored to normal. Such finding suggests that the site of action of I-677 be at the cytoplasmic ground substance. The inhibition of protein synthesis causes a decrease in albumin carrier, that may be the main mechanism of steatosis of liver cells induced by I-677.
When Schistosoma japonicum was exposed to culture medium containing [3H]ATP and praziquantel 0.1, 1 or 10μg/ml for 1—4 h, the [3H]ATP uptake decreased significantly in male worms, but not in females. If male schistosomes were exposed to praziquantel 1 or 10μg/ml for 1—4 h and then transferred to drug-free culture medium, the [3H]ATP uptake recovered to normal only in lower drug concentration group. The [3H]ATP uptake of male worms markedly decreased 1 h after intragastric gavage of praziquantel100 mg/kg to infected mice and recovered to normal 4 h later. However, [3H]ATP uptake of male worms was steadily inhibited 24 h after 300 mg/kg to infected mice. No effect on [3H]ATP uptake of female worms was seen.
Praziquantel promoted the transformation of [3H]ATP uptaken by male worms to [3H]AMP, while the incorporation of [3H]ATP to RNA of male worms was markedly inhibited. No apparent changes were observed in female worms.
Laurocapram (Lau), 1-dodecyl-hexahydro-2 H-azepin-2-one, (azone) is a new percutaneous penetration enhancer. However, the mechanism of its action for absorption promoter of other agents is still unknown. In this paper the effect of Lau on ultrastructures of skin surface and tumor cell membrane were studies. Lau (2%) suspension was applied to abdominal skin of ICR/JCL, C 57 BL mice or one side of abdominal skin of nude mouse with drug and other side with the vehicle solvent once daily for 2-3 d. The skin was excised at 4 h after the final medication for examination under scanning electron microscope (SEM). The results showed the numerous small infolding lines which divided the skin surface into small areas with vesiculation and peeled the epidermal surface to form a few minor holes. The cuticles of the hair shaft dropped off and became thinner. Numerous desquamated cells around the orifice of the hair were fractured, detached and widened. Sarcoma 180 cells were incubated with Lau 25 micrograms/ml at 37 degrees C for 4 h. The microvilli of some cells dropped off and the size of villi became thinner and shorter. The top of some villi of the cells appeared occasionally thick to make the profile as a bat. The surface of numerous naked cells became rugged and rough and showed many black minor holes in the area of denuded cell membrane or dropped microvilli. More than 100 holes in the exposed surface of the naked cell were seen. It seemed that the Lau drilled holes on the biomembrane and enlarged the orifice of hair follicles and thus enhanced the transdermal absorption.
When pairs of Schistosoma japonicum were exposed to culture medium containing praziquantel 1 or 10 microg/ml for 4 h, the glycogen content, [1-14C]glucose uptake, and incorporation of [1-14C]glucose into the glycogen were markedly decreased. Male schistosomes seemed to be more affected.
After bisexual worms had been maintained in praziquantel 1 and 10 microg/ml for 4 h, and then transferred to drug-free culture medium for 4-18 h, the glycogen content and [1-14C]glucose uptake of female worms recovered promptly. In male worms the changes caused by praziquantel 1 microg/ml were reversible, while those caused by 10 microg/ml were not.
Infected mice were given intragastrically praziquantel 20 mg/kg. After 2-4 h the glycogen content of the bisexual worms decreased markedly, but recovered in 48 h. After ig 100-300 mg/kg, no apparent recovery of glycogen content was seen 72 h later. When the worms perfused out from the mice 8 h after ig 100-300 mg/kg were maintained in vitro, the glycogen conent, [1-14C]glucose uptake and incorporation of [1-14C]glucose into the glycogen of the female worms could recover, but the recovery was not significantly in male worms.
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