Studies on the Chinese crude drug "Forsythiae Fructus." VI. The structure and antibacterial activity of suspensaside isolated from Forsythia suspensa.
Explore the source record for details and available documents.
Biomedical subjects
Publications and source records attributed to K Okabe.
Explore the source record for details and available documents.
Mitochondrial respiratory function of the liver is disturbed in biliary obstruction, especially in that caused by tumours in the hepatobiliary system. This study aimed to clarify whether a glucocorticoid, prednisolone succinate, is effective to improve the reduced mitochondrial function of the rat liver in obstructive jaundice. Five doses of 5 mg/kg or 25 mg/kg prednisolone succinate were administered at 5 consecutive days to the rats after 1, 3 or 6 weeks of biliary obstruction and to the rats without obstruction, and the hepatic mitochondrial function and contents of cytochromes of these rats were investigated. With 25 mg/kg prednisolone, hepatic mitochondrial function was improved in rats with biliary obstruction of 3- or 6-weeks duration as compared with the prednisolone-untreated group. Compensatory increase or recuperation of the once decreased cytochrome A(+a3) and/or turnover number of phosphorylation was also observed in 25 mg/kg group. Hepatic mitochondrial function of obstruction-free animals was rather impaired by treatment with 25 mg/kg prednisolone. In 5 mg/kg group, above mentioned effects were scarcely observed. It was concluded that the hepatic mitochondrial function in animals with prolonged biliary obstruction, as same as in animals with short-term obstruction, can be improved by the administration of adequately large amounts of prednisolone.
AMSA, an acridine derivative with significant antitumor activity in experimental tumors, was administered to 17 patients with advanced tumors refractory to standard chemotherapies. A phase I study was undertaken in 10 patients with solid tumors and lymphomas. Dose-limiting toxicity was myelosuppression. With a median dose of 90 mg/m2 (75-148 mg/m2), median lowest WBC count was 1,000/mm3 (100-3,200) on day 11 and its recovery up to 4,000/mm3 was seen on day 21, while lowest platelet count was 42 X 10(3)/mm3 (7-300 X 10(3) on day 12 and its recovery up to 100 X 10(3)/mm3 was on day 20. Non-hematological toxicities were nausea (39%), vomiting (11%) and phlebitis (17%) in 18 courses of therapy. The result indicated that the recommended dose schedule for a phase II evaluation was 90 mg/m2, every three weeks. Therapeutic activity was observed in patients with non-Hodgkin's lymphoma (one partial response and two minor responses out of four). Two out of five breast, one ovarian, and one melanoma patients showed stable diseases. Five leukemic patients (three AMLs, one MoL, and one blastic CML) were treated with AMSA, and in these cases cytoreduction of peripheral and bone marrow blasts was seen, but it was not adequate to induce remission. Further clinical trials with this agent are warranted, especially in patients with acute leukemia, lymphoma and breast cancer.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Human fibroblast interferon(HFIF) was used in 26 patients with various malignant diseases, most of whom had previous chemotherapy. The dosages used were 3 X 10(6) IU or 6 X 10(6) IU of HFIF i. v. daily. Out of 24 evaluable patients, there were 2 partial remissions (CLL 1 and multiple myeloma 1), and 7 stable diseases (multiple myeloma 2, stomach cancer 2, non-Hodgkin's lymphoma 1, CLL 1 and malignant melanoma 1). The majority of the patients experienced fever exceeding 38 degrees C and chills, which became uncommon within several days of treatment. Other side effects included myelosuppression, general malaise, anorexia, hepatic dysfunction and renal dysfunction, which were mild and tolerable.
Several immunological studies were performed in patients with various malignant diseases under treatment of human fibroblast interferon (HFIF). Lymphocyte natural killer (NK) activity against culture cell lines was measured before and at various time after HFIF treatment. The majority of patients reached the highest level of NK activity at 18-24 hours, mostly at 24 hours after initiating HFIF. In one group of patients, thereafter, NK activity remained the highest level during HFIF treatment, and in another group of patients, NK activity declined even with daily infusion of HFIF but usually remained above pre-treatment level. There seemed to be no correlation between NK activity and clinical activity. In contrast to NK activity against culture cell lines, an increase in lymphocyte cytotoxic activity against autologous tumor cells was not observed following HFIF treatment. Mixed lymphocyte tumor cell reaction performed in 6 patients showed that a slight increase of 3H-thymidine uptake was seen in one patient, but the rest of them had no change. In vitro sensitization to assess the in vitro generation of cytotoxic cells were negative in all 6 patients. Lymphocyte blastogenic responses to non-specific mitogens showed no significant change. Delayed type hypersensitivity reaction to recall antigens was increased in about half of the patients after HFIF treatment.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Renal functions and the clinical courses of 14 patients with renal disturbances associated with obstructive jaundice were studied. All patients had high concentrations of serum bilirubin, long durations of jaundice and episodes of shock due to massive hemorrhage or severe inflammation. In an experimental study on jaundiced rats, effects of hypotension or bilateral renal artery occlusion on renal function and renal cortical mitochondrial respiration at 1 week, 3 or 6-weeks after biliary obstruction were investigated. In jaundiced rats, there was no remarkable difference in renal function, but the renal mitochondrial respiration indices decreased with prolongation of the biliary obstruction. In hypotensive rats with prolonged biliary obstruction, the mitochondrial function was impaired, and in the rats with renal artery occlusion, the mitochondrial impairment was more severe. Based on these clinical and experimental data, it is tentatively suggested that patients with prolonged jaundice should be considered in a prodromal state of renal failure and that any minute circulatory failure may induce acute renal failure.
Explore the source record for details and available documents.
The peptide antibiotic siomycin-A was transformed into half-esters with dicarboxylic acids with the intention of making siomycin-A soluble in water. Sodium salts of the half-esters were also prepared. Some of the salts showed antibacterial activities comparable to siomycin-A against Gram-positive bacteria in vitro and exhibited better therapeutic effects in infected mice than siomycin-A. The chemical structures of siomycin-A hemiadipate-II and -III were elucidated by comparing their 13C and 1H NMR spectra with those of siomycin-A. Their physicochemical properties are described.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.