Bryophyllin B [1], a potent cytotoxic bufadienolide, has been isolated from Bryophyllum pinnatum and its structure confirmed by the use of 2D-nmr techniques and difference nOe method. Transformation of bryotoxin C [2] to 1 with acid is also discussed.

Antineoplastic Agents, Phytogenic↗

PubMedDate not supplied

Antitumor agents, 115. Seselidiol, a new cytotoxic polyacetylene from Seseli mairei.

Seselidiol [1], a new polyacetylene, has been isolated from the roots of Seseli mairei. On the basis of chemical and spectroscopic evidence, its structure has been established as heptadeca-1,8(Z)-diene-4,6-diyne-3,10-diol. Seselidiol and its acetate have been demonstrated to show moderate cytotoxicity against KB, P-388, and L-1210 tumor cells.

Acetylene↗

PubMedDate not supplied

Antitumor agents, 116. Cytotoxic triterpenes from Maytenus diversifolia.

The known triterpenes 3-oxofriedelan-29-oic acid [1], 3-oxofriedelan-28-oic acid [2], and 28,29-dihydroxyfriedelan-3-one [3] have been isolated from Maytenus diversifolia. Compounds 1-3 demonstrated cytotoxicity against the A-549 lung carcinoma cells with ED50 values of 0.21, 1.18, and 0.64 micrograms/ml, respectively.

Antineoplastic Agents, Phytogenic↗

PubMedDate not supplied

Antitumor agents, 118. The isolation and characterization of bruceanic acid A, its methyl ester, and the new bruceanic acids B, C, and D, from Brucea antidysenterica.

The known bruceanic acid A [1] and its methyl ester 2, as well as the new bruceanic acids B [3], C [4], and D [5], have been isolated from Brucea antidysenterica. The structures of 1-5 were elucidated by spectral data. Compound 1 demonstrated cytotoxicity against KB and TE671 tumor cells. Compound 5 was cytotoxic against P-388 lymphocytic leukemia cells.

Animals↗

PubMedDate not supplied

The crystal structure and cytotoxicity of goniodiol-7-monoacetate from Goniothalamus amuyon.

The styrylpyrone, goniodiol-7-monoacetate [1] [6R-(7R,8R-dihydro-7-acetoxy-8-hydroxystyryl)-5, 6-dihydro-2-pyrone], has been isolated from Goniothalamus amuyon, and its detailed molecular structure has been determined by X-ray crystallographic analysis. Goniodiol-7-monoacetate showed potent (ED50 values less than 0.1 microgram/ml) cytotoxicities against KB, P-388, RPMI, and TE671 tumor cells.

Animals↗

PubMedDate not supplied

Isolation and activation of inactive renin from human kidney and plasma. Plasma and renal inactive renins have different molecular weights.

Inactive renin and active renin from human kidney and human plasma were prepared in highly purified forms by three steps of chromatography on Octyl-Sepharose, immunoaffinity chromatography, and pepstatin-amino hexyl Sepharose CL-4B. The inactive renin and active renin from human kidney had molecular weights of 51,000 and 44,000 as measured by a calibrated gel filtration column run with internal molecular weight standards. Molecular weights of plasma inactive renin and active renin were 56,000 and 51,000 respectively. Both inactive and active renins were found to be heterogeneous, consisting of several components with different isoelectric points. Renal inactive renin has higher pI values of 6.40, 6.10, 5.90, 5.61, and 5.40. Renal active renin has pI values of 5.73, 5.40, 5.25, and 5.13. The pI values of plasma inactive renin were 6.37, 6.08, 5.77, 5.36, and 5.25; of plasma active renin, 5.68, 5.40, 5.33, and 5.25. Trypsin activation and plasmin activation of plasma inactive renin produced an active enzyme with similar molecular weight but lower pI values. Acid activation of inactive renin did not change the molecular weight and pI values.

Chromatography, Affinity↗

PubMedDate not supplied

Apolipoproteins A-I and B in non-insulin-dependent diabetes mellitus.

In recent years apolipoproteins A-I and B examinations have been performed on patients with coronary artery disease as a better predictor of the severity of atherosclerosis. In the present study, 21 treated male and 22 treated female patients with non-insulin-dependent diabetes mellitus (NIDDM) were examined and compared with controls of the same sex, age and body mass (23 males, 21 females). Cholesterol, triglyceride, LDL-cholesterol in male and female patients with NIDDM were significantly higher than in male and female controls. HDL-cholesterol in male and female patients with NIDDM was not different from those of male and female controls. Apolipoproteins A-I and B in male and female patients with NIDDM were higher than in male and female controls. [Apolipoproteins A-I (g/L) male 1.40 +/- 0.21 vs 1.25 +/- 0.15, p less than 0.005; female 1.56 +/- 0.23 vs 1.42 +/- 0.24, p less than 0.025. Apolipoproteins B (g/L) male 1.29 +/- 0.30 vs 0.97 +/- 0.22, p less than 0.001; female 1.34 +/- 0.34 vs 0.98 +/- 0.35, p less than 0.001.] Discrepancy between the higher apolipoprotein A-I and the normal HDL-cholesterol in in NIDDM supports the theory of altered composition of HDL particles in diabetic patients. The controversy between the higher apolipoprotein A-I and the higher incidence of atherosclerosis in patients with NIDDM makes the clinical usefulness of this laboratory measurement doubtful in these patients.

Adult↗

PubMedDate not supplied

Serum thyrotropin-binding inhibiting immunoglobulin and thyroperoxidase antibody in Graves' hyperthyroidism after 131I therapy.

Seventeen patients who received radioiodine (131I) therapy for Graves' hyperthyroidism had serial blood samples taken before therapy and after therapy for a period of at least 1 year. At 1 year post-therapy, six patients were hypothyroid. Seven patients were euthyroid, and four patients were hyperthyroid. Prior to isotope administration, 14 patients had detectable serum thyrotropin-binding inhibiting immunoglobulin (TBII) and 16 patients had detectable serum thyroperoxidase antibody (TPOAb). Three to 6 months after therapy, 11 of 14 TBII-positive patients demonstrated a marked increase (> 10%) in serum TBII activity. Four patients out of 11 developed hypothyroidism and six of the 11 developed euthyroidism. A decrease in TBII was observed in three patients who developed hyperthyroidism. In the three patients with undetectable TBII prior to therapy, two had high titers of TPOAb. Seven patients demonstrated a marked increase in TPOAb 3 to 6 months after therapy. Of these, four developed hypothyroidism and three developed euthyroidism, whereas three of the four patients who had a marked decrease in TPOAb developed hyperthyroidism. This study demonstrated that an increase in serum TBII and TPOAb activity 3 to 6 months after 131I therapy, may be useful in predicting which patients may develop euthyroidism or hypothyroidism after 1 year of 131I therapy.

Adult↗