1.1. Immature mice were induced to ovulate by pregnant serum gonadotropin and human chorionic gonadotropin.2.2. The ribosome inactivating proteins luffaculin, luffin-a, luffin-b and momorcochin were administered i.p.3.3. It was found that all four ribosome inactivating proteins elicited a reduct...

1. Possible teratogenic activity in the ribosome inactivating proteins luffaculin, luffin-a, luffin-b and momorcochin was tested using cultured mouse embryos.2. At a dosage of 200 μg/ml culture medium, luffin-a and momorcochin did not affect organogenesis in embryos.3. Luffin-b at a dosage of 1...

The present study describes the liposome-mediated delivery of the type 1 ribosome-inactivating protein luffin to human melanoma cells in vitro. Luffin from Luffa cylindrica seeds has been successfully incorporated into lecithin/cholesterol and lecithin/cholesterol/dicetylphosphate negatively cha...

We purified and characterized a novel RIP (ribosome inactivating protein), Luffin-S from the seeds of Luffa cylindrica. Different from Luffin-A and B, which are RNA N-glycosidases with molecular weights of 27 and 28 kDa, respectively, Luffin-S has an M.W. of only approx. 10 kDa, much smaller tha...

A peptide designated Luffin P1 was purified from the seeds of Luffa cylindrica. Its molecular mass was determined to be 5226.1 Da by MALDI-TOF MS analysis. The purified Luffin P1 shows a strong inhibitory activity on protein synthesis in the cell-free rabbit reticulocyte lysate with IC50 of 0.88...

Luffin P1, the smallest ribosome-inactivating peptide from the seeds of Luffa cylindrica was found to have anti-HIV-1 activity in HIV-1 infected C8166 T-cell lines and be able to bind with HIV Rev Response Element. Nuclear magnetic resonance spectroscopy revealed that the Luffin P1 comprises a h...

Determination of DNA dephosphorylation is of great value due to its vital role in many cellular processes. Here we report a surface-extended DNA nanotail strategy for simple and ultrasensitive detection of DNA 3′-phosphatases by terminal deoxynucleotidyl transferase (TdT) mediated signal amplif...

DNA methylation inhibitors are being extensively studied as potential anticancer agents. In the present study, we compared the capability of alpha anomer of 5-aza-2′-deoxycytidine (α-5-azadCyd) to induce down-regulation of hTERT expression in HL-60 cells with other nucleoside analogs that act ...

New aromatic and aliphatic 3′-O-acyl-5-fluoro-2′-deoxyuridine derivatives were synthesized and evaluated as candidates for prodrugs against various cancer cell lines. As the most promising candidate for antimalignant therapeutics was found a dual-acting acyl derivative 7h, which apparently rel...

From the proton and fluorine NMR spectra of 3′,5′-di-O-acetyl-2′fluoro-2′-deoxyuridine, its thiouracil analogue and 2′-fluoro-2′-deoxycytidine at 250 MHz, it was concluded that these compounds are preferentially in a 3′-endo—4′-exo conformation (N-form) with only about 10–20% 2′-endo ...

An efficient approach to 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-ethyl-1,3-dihydro-benzimidazol-2-one (J-113397) Figure 1, Scheme 1, the first non-peptide ORL-1 receptor antagonist described in literature, is outlined. After construction of the piperidine framework through D...

1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-[11C]ethyl-1,3-dihydro-2H-benzimidazol-2-one ([11C]CPEB) was synthesized by [11C]N-ethylation and evaluated as a potential brain ORL1 receptor imaging agent by positron emission tomography. The uptake of [11C]CPEB in the mouse brain wa...

A new chiral synthesis of the ORL-1 antagonist 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (2, J-113397) was developed. J-113397 has a Ke = 0.85 nM in an ORL-1 calcium mobilization assay and is 89-, 887-, and 227-fold selective for the O...

For the synthesis of metalloproteinase inhibitors the (R,R)- and (S,S)-monoethyl esters of N-Boc-pyrrolidine-3,4-dicarboxylic acid were prepared as key intermediates from the trans-diester racemate by two consecutive, highly selective enzymatic reactions. Reduction of the formed acids to the cor...

The results after the first 6 months of the 1 -year treatment of this multicenter, randomized, open, parallel-group design study of delapril versus enalapril in patients with congestive heart failure (CHF), New York Heart Association (NYHA) classes II and III, are presented. The initial dose of ...

In this controlled trial, 30 elderly patients with congestive heart failure, New York Heart Association (NYHA) classes II and III, were randomly assigned to treatment with captopril 25 mg three times daily or delapril 15 mg twice daily. At the end of an 8-week treatment period, clinical symptoms...

The renin–angiotensin system is an important modulator of arterial blood pressure and inhibitors of the angiotensin-converting enzyme (ACE-Is) and are currently used in the treatment of hypertension. The pleiotropic actions exerted by angiotensin II (AngII) on the functionality of the vessel wa...

Thirty-nine hypertensive patients with type 2 diabetes mellitus were followed under long-term treatment (mean, 20.7 months) with manidipine hydrochloride, a Ca antagonist, or delapril hydrochloride, an ACE inhibitor, at nine institutions. Both the treatments showed similar antihypertensive effec...

Background: Failure to achieve good blood pressure (BP) control is probably the most important reason for high rates of morbidity and mortality in patients with hypertension. Combination therapy has been shown to increase the percentage of patients in whom BP control is achieved. One combination...

Background:The use of coombination therapy is required to achieve blood pressure targets in 40% to 75% of patients with hypertension. There have been few studies comparing the efficacy and tolerability of the new fixed combination of the angiotensin-converting enzyme (ACE) inhibitor delapril 30 ...