Isolated marrow reticuloendothelial activation and erythropoietic response following an acute blood loss.

The radioassay technique with the 113mIndium-iron chondroitin sulfate colloid, developed in our laboratory, revealed that an isolated marrow reticuloendothelial activation takes place after bleeding 15 to 30 ml of blood per kg body weight from a rabbit. It parallels the erythropoietic response very well. The present stimulation method might deserve testing for studies where marrow reticuloendothelial function is important such as in cancer-bearing patients, the effects of anticancer chemotherapy and gross antigenization.     

Structures of Angular Pyranocoumarins of Bai-Hua Qian-Hu, the Root of Peucedanum praeruptorum1

Three new angular-type dihydropyranocoumarins, peucedanocoumarin I ( 1), peucedanocou-marin II ( 2), peucedanocoumarin III ( 3), and a known coumarin having the same skeleton, pteryxin ( 4), were isolated from the crude drug "Bai-Hua Qian-Hu" of the Q-II type series, which is the root of PEUCEDANUM PRAERUPTORUM Dunn. (Umbelliferae). The chemical structures of 1, 2, and 3 have been established by physicochemical methods to be 3' ( S)-2-methylbutyryloxy-4'-( R)-acetoxy-3',4'-dihydroseselin, 3'( S)-acetoxy-4'( R)-angeloyloxy-3',4'-dihydroseselin, and 3'( S)-acetoxy-4'( R)-tigloyloxy-3',4'-dihydroseselin, respectively.     

The medicine chest handed down in the Takaya family, doctors of Sendai-han

There is a medicine chest with design of Chrysanthemums in Makie made for Edo-era and handed down in the Takaya family, doctors of Sendai-han. Many kinds of crude drugs, named by one Chinese character, are kept in this chest. They were classified into three types, namely, [Japanese characters]. Identification of these crude drugs was carried out and the meaning of the classification was brought up as a question.     

Iodine-123-MIBG scintigraphy in neuroblastoma; relationship between the intensity of uptake and tumor characteristics

Iodine-123-MIBG (123I-MIBG) scintigraphy were performed for 23 patients with neuroblastoma at diagnosis. The intensity of MIBG activity in the primary tumor was evaluated visually (grade 3; intense uptake-grade 0; no definite uptake), and its relationship to the size, degree of tumor spread, urinary catecholamine metabolites (VMA, HVA), and histological types were investigated. The results of 123I-MIBG uptake grade were as follows: grade 3; 44% (10/23), grade 2; 30% (7/23), grade 1; 17% (4/23), grade 0; 9% (2/23). The grade was not associated with the tumor size, or the degree of tumor extension to the distant lesion, either. The more catecholamine metabolites were excreted in the urine, the tumor tended to have more intense uptake. The tumors of neuroblastoma rosette fibrillary type, and ganglioneuroblastoma poorly differentiated type had more intense uptake than neuroblastoma round cell type and ganglioneuroblastoma well differentiated type. The case of ganglioneuroma did not have definite MIBG uptake. The intensity of MIBG uptake is not relevant to the pathological grade of neuroblastoma, but considering the electromicroscopical features of neuroblastoma reported previously, it is thought to reflect the histological type.     

Design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine sigma ligands as potential antipsychotic drugs

sigma Receptor antagonists may be effective antipsychotic drugs that do not induce motor side effects caused by ingestion of classical drugs such as haloperidol. We obtained evidence that 1-(2-dipropylaminoethyl)-4-methoxy-6H-dibenzo[b,d]pyran hydrochloride 2a had selective affinity for sigma receptor over dopamine D2 receptor. This compound was designed to eliminate two bonds of apomorphine 1 to produce structural flexibility for the nitrogen atom and to bridge two benzene rings with a -CH2O- bond to maintain the planar structure. In light of the evidence, N, N-dipropyl-2-(4-methoxy-3-benzyloxylphenyl)ethylamine hydrochloride 10b was designed. Since compound 10b had eliminated a biphenyl bond of 6H-dibenzo[b,d]pyran derivative 2a, it might be more released from the rigid structure of apomorphine 1 than compound 2a. The chemical modification of compound 10b led to the discovery that N, N-dipropyl-2- [4-methoxy-3-(2-phenylethoxyl)phenyl]ethylamine hydrochloride 10g (NE- 100), the best compound among arylalkoxyphenylalkylamine derivatives 3, had a high and selective affinity for sigma receptor and had a potent activity in an animal model when the drug was given orally. We report here the design, synthesis, structure-activity relationships, and biological characterization of novel arylalkoxyphenylalkylamine derivatives 3.     

Flavonoids from Cleome droserifolia suppress NO production in activated macrophages in vitro.

The effect of an Egyptian medicinal plant, Cleome droserifolia (Forssk.) Del. on nitric oxide (NO) production in bacillus Calmette-Guérin-induced mouse peritoneal macrophages activated by lipopolysaccharide was investigated in vitro. The methanol extract of C. droserifolia reduced the NO production, and two flavonoids were isolated as the active components. The new one was determined to be 5,4'-dihydroxy-6,7,8,3',5'-pentamethoxyflavone (1) and the other was identified as 5,4'-dihydroxy-6,7,8,3'-tetramethoxyflavone (8-methoxycirsilineol; 2). Compound 1 concentration-dependently suppressed the NO production and was effective at a non-toxic concentration (12.5 micrograms/ml). The suppressive activity of 2 was weaker than that of 1.     

The fertilizing ability of human epididymal sperm

Purpose: Membrane cofactor protein (MCP), CD46, whose primary function is to protect host cells from homologous complement, has been presumed to serve as a sperm adhesion molecule for oocytes. The purpose of this study was to clarify the relationship between the properties of MCP expressed on epididymal sperm and their fertilizing ability in a recently developed strategy for assisted reproduction. Methods: We collected ejaculated sperm from normal subjects and epididymal sperm from vasectomized subjects and patients with congenital absence of the vas deferens. Western blotting and cofactor activity assay were performed to investigated the structural and functional properties of MCP. Results: Epididymal spermatozoa which showed a reduced fertilizing ability tended to react poorly with antibodies against MCP and also showed low cofactor activity, indicating weak complement regulatory activity compared to that of ejaculated spermatozoa. Conclusions: MCP is sufficiently expressed in ejaculated sperm in men with a normally developed epididymis but is diminished in epididymal sperm from men with congenital or acquired obstruction of the vas deferens.