POLYMERIC 2-MERCAPTOPYRIDINE AND 2-MERCAPTO-NITROBENZENE DERIVATIVES: New Reagents for Peptide Synthesis

Insoluble 2-mercaptopyridine and 2-mercapto-nitrobenzene derivatives were prepared by modification of commercially available polystyrene. Applicability of these polymers as reagents for the thiolytic removal of the 2-nitrophenyl-sulphenyl amino-protecting group and as supports for preparation of polymeric active esters was evaluated. Polymeric 2-mercaptopyridine (PMP) was found efficient for both purposes. It was used in the stepwise synthesis of Leu-enkephalin via the polymeric reagent approach, serving as an Nps-cleaver. Polymeric esters derived from PMP and Boc-amino acids proved to be excellent acylators. Their usefulness is exemplified in the preparation of two dipeptides, which were produced rapidly and in high yields and purity.     

Hemoglobin Switching in Nonanemic Sheep. III. Evidence for Presumptive Identity between the Ararr C Factor and Erythropoietin

The degree of A C hemoglobin switching following administration of a humanurine erythropoietin preparation to anon-anemic sheep was compared, in thesame animal, with the switching obtainedwith administration of anemic sheepplasma containing known amounts oferythropoietin. A strong correlationemerges between the dosage of erythropoietin given and the degree of A Cswitching observed. This correlation between erythropoietin dose and A Cresponse is maintained despite the use ofmaterials that originated in different species (man and sheep), were assayed forerythropoietin in yet another species(mouse), and had grossly different specific activities (units/mg.) of erythropoietin, so that the specific activity of thehuman urine preparation was approximately 400 to 1600 times that of anemicsheep plasma. We believe these observations provide substantial evidence fora provisional hypothesis of identity between erythropoietin and the A Cswitching factor.

Submitted on December 22, 1969 Revised on June 15, 1970 Accepted on June 24, 1970     

Unidentified Reticuloendothelial Cell Storage Disease

1. An abnormal cell of probably reticuloendothelial origin with prominentcytoplasmic granules was observed in the bone marrow, liver and a lymphnode of an adult white female with incidentally discovered, asymptomatichepatosplenomegaly.

2. Histochemical studies revealed the granules to consist of a chemical complex which contained bound lipid and protein.

3. The cells differed from those of Gaucher’s disease, Niemann-Pick’s diseaseand other storage diseases. The significance of these cells remains unknown.

Submitted on February 8, 1961 Accepted on March 17, 1961     

Increased Serum FSH Levels Correlated with Low and High Sperm Counts in Male Infertile Patients

Serum FSH, LH and testosterone were measured in 57 (42) normal men and in 80 male infertile patients. In the former, mean (x) FSH was found to be 2.5 ng/ml with a range (x +/- 2 SD) from 0.25 ng/ml to 5.3 ng/ml, mean LH was 2.2 ng/ml with a range from 0.5 ng/ml to 5.6 ng/ml, and mean testosterone was 540 ng/100 ml with a range from 190 mg/ml to 890 ng/100 ml. Immunoassayable FSH was found to be elevated in 17 out of 42 presumably infertile males with sperm counts below 20 million/ml, and in 5 out of 12 men with sperm counts above 120 million/ml. There was no correlation between testosterone and sperm number, motility, and seminal fructose content. The concurrence of depressed spermatogenesis and elevated FSH levels seems to be a relatively good indicator for the presence of organic disorders of the testis.     

Hyperalimentation in Alcoholic Hepatitis

Enteral hyperalimentation in four patients with severe alcoholic hepatitis and anorexia increased spontaneous food intake, increased their nitrogen balance and the patients improved clinically. Seven patients with alcoholic hepatitis, who were clinically ill and able to eat only 410-1,100 calories per day, were given a 900 mosM/l. parenteral "hyperalimentation" solution by a peripheral vein (P-900). The intravenous nutrition provided daily 51.6-77.4 gm. amino acids in addition to oral intake. All patients improved. None developed detectable encephalopathy after 16-42 days of P-900 therapy. Five additional patients had ascites and alcoholic hepatitis. The daily infusion of 2,000 ml. P-900 was not associated with hyponatremia, renal failure or encephalopathy in four of these five patients who improved and continued their diuresis. P-900 therapy was discontinued in one because of progressive hyponatremia. The observations indicate that over and above the maximum tolerable oral nutrition, intravenous nutrition can be effectively utilized by clinically ill, jaundiced patients with alcoholic hepatitis without precipitating encephalopathy or interference with standard therapy of ascites.     

Induction in Rabbits of Activity Against Human Blood Thromboplastin

Rabbits were injected with sedimented human blood thromboplastin, andtwo animals developed serum activity against human blood thromboplastinin significant excess over naturally occurring inhibitor. This antithromboplasticactivity was specific against human reagent, failed to affect thromboplastinprecursors and had no activity against tissue thromboplastin.