• Bulletin of the Korean Chemical Society
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• v.31 no.3
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• pp.620-623
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• 2010

A brush type chiral stationary phase (CSP 2) derived from ${\alpha}$-amino ${\beta}$-lactam was prepared for the separation of the enantiomers of ${\beta}$-blockers. Compared to the CSP derived from ${\alpha}$-amino phosphonate (CSP 1), in general, the conformationally rigid CSP 2 showed greater scope and much enhanced enantioselectivity for the resolution of ${\beta}$-blockers. The effect of various salt additives on enantioseparation of ${\beta}$-blockers in the mobile phase was investigated. The unusual effect of temperature on the chromatographic behaviors was observed on CSP 2. It also afforded appreciable increases in enantioselectivity without significantly affecting resolution, as the column temperature was reduced.

• Asian Pacific Journal of Cancer Prevention
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• v.15 no.22
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• pp.9567-9574
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• 2014

${\beta}$-Blockers have been one of the most widely used and versatile drugs for the past half a century. A new potential for their use as anti-cancer drugs has emerged in the past few years. Various retrospective case control studies have been suggestive that use of ${\beta}$-blockers before the diagnosis of cancer could have preventive and protective effects against non-small cell lung carcinoma, melanoma, and breast, pancreatic and prostate cancers. Experimental and clinical observations are still inconclusive with some inconsistent findings. However, indications are pointing toward a positive role of some ${\beta}$-blockers against certain forms of cancers. This mini review is an effort to present the up to date published results of case-control studies and experimental findings.

• Analytical Science and Technology
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• v.6 no.4
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• pp.375-381
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• 1993

The efficiencies of four different solid absorbents were evaluated for the simultaneous solid-phase extraction of six ${\beta}$-blockers from biological sample. Chromosorb 107 using methanol as the eluting solvent gave the highest solid-phase extraction yield. From the breakthrough studies of ${\beta}$-blockers, the excellent sorption and desorption properties of the Chromosorb 107 column were verified. The usefulness of Chromosorb 107/methanol was examined for the simultaneous solid-phase extraction of the ${\beta}$-blockers from serum in the concentration range of 2~8ppm.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.249.2-250
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• 2003

${\beta}$-blockers are considered as standard therapy for patients with stable chronic heart failure (CHF) and to prolong survival and reduce hospitalizations. We examined the effects of the ${\beta}$-blocker on mortality, hospitalization and symptoms in patients with CHF and the related factors to the use of ${\beta}$-blockers. Patients in New York Heart Association class II-IV were included if they were treated for heart failure from January 2002 to June 2002. At baseline, 6 months, and 12 months, they were assessed for the change of NYHA class and all deaths and hospital admissions. (omitted)

• Archives of Pharmacal Research
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• v.29 no.11
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• pp.1061-1065
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• 2006

A new chiral derivatization agent with sugar moiety, 2,3,4,6-tetra-O-acetyl-${\beta}$-D-galactopyranosyl isothiocyanate (GATC) was synthesized. Several ${\beta}-blockers$ were investigated for the possible separation of the enantiomers by reversed-phase HPLC after derivatization with this new chiral derivatization agent (GATC). GATC was reacted readily with ${\beta}-blockers$ at room temperature and the reaction mixture could directly be injected into the HPLC system. The corresponding diastereomers were well resolved on an ODS column with acetonitrile-ammonium acetate buffer as a mobile phase and monitored at UV 254 nm. The optimization of the derivatization procedure (concentration of GATC, reaction temperature and time) and HPLC conditions (pH and ionic strength of mobile phase) were investigated and compared with GITC.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.18
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• pp.8031-8039
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• 2016

Background: Preclinical studies have demonstrated that ${\beta}$-adrenergic receptor antagonists could improve the prognosis of breast cancer. However, the conclusions of clinical and pharmacoepidemiological studies have been inconsistent. This review was conducted to re-assess the relationship between beta-adrenoceptor blockers and breast cancer prognosis. Materials and Methods: The literature was searched from PubMed, EMBASE and Web of Nature (Thompson Reuters) databases through using key terms, such as breast cancer and beta-adrenoceptor blockers. Results: Ten publications met the inclusion criteria. Six suggested that receiving beta-adrenoceptor blockers reduced the risk of breast cancer-specific mortality, and three of them had statistical significance (hazard ratio (HR)=0.42; 95% CI=0.18-0.97; p=0.042). Two studies reported that risk of recurrence and distant metastasis (DM) were both significantly reduced. One study demonstrated that the risk of relapse-free survival (RFS) was raised significantly with beta-blockers (BBS) (HR= 0.30; 95% CI=0.10-0.87; p=0.027). One reported longer disease-free interval (Log Rank (LR)=6.658; p=0.011) in BBS users, but there was no significant association between overall survival (OS) and BBS (HR= 0.35; 95% CI=0.12-1.0; p=0.05) in five studies. Conclusions: Through careful consideration, it is suggested that beta-adrenoceptor blockers use may be associated with improved prognosis in breast cancer patients. Nevertheless, larger size studies are needed to further explore the relationship between beta-blocker drug use and breast cancer prognosis.

• Archives of Pharmacal Research
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• v.27 no.12
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• pp.1290-1294
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• 2004

The ${\beta}$-blockers possess at least one chiral center and the S(-)-enantiomer shows higher affinity for binding to the ${\beta}$-adrenergic receptors than antipode. The stability constants of acebutolol, celiprolol, propranolol and terbutaline in the inclusion complexes with single-isomer heptakis (2,3-dimethyl-6-sulfato)- ${\beta}$-cyclodextrin (HDMS-${\beta}$-CD) were determined by capillary electrophoresis. The approximation and linear double reciprocal methods were adapted with comparable results. Among the ${\beta}$-blockers studied, propranolol had the lowest stability constant but the highest enantioselectivity, indicating that the magnitudes of the stability constants carried little information about enantioseparation. The magnitudes of enantioselectivities between the enantiomer pair were in the order of propranolol > celiprolol > terbutaline > acebutolol.

• YAKHAK HOEJI
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• v.28 no.5
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• pp.265-273
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• 1984

The effects of cinnarizine, $Ca^{2+}-antagonist$, on the antihypertensive effect of coadministered ${\beta}-blockers$, propranolol and metoprolol, were investigated in SHR. Drugs were coadministered orally for 4 weeks. Hemodynamic and biochemical changes induced by above drugs were determined to elucidate their mechanism of action. a) Cardiohypertropy of SHR was significantly improved by the treatment of ${\beta}-blockers$ as well as combination with cinnarizine and ${\beta}-blockers$. b) $Mg^{2+}-contents$ were increased in ventricle and decreased in plasma and aorta in all of the groups, especially in the group of propranolol with cinnarizine. c) c-GMP contents in ventricle were increased when cinnarizine was coadministered with propranolol, and c-GMP contents in aorta were increased when cinnarizine was coadministered with metoprolol, camparing with propranolol or metoprolol alone-treated group. d) Plasma renin activity appeared to be increased in cinnarizine treated alone, but reduced by combination with ${\beta}-blockers$. e) Triglycerides and $Na^+$ contents in serum were decreased in the group of metoprolol with cinnarizine, comparing with metoprolol alone-treated group. Increased $K^+\;and\;Ca^{2+}$excretions in urine by ${\beta}-blockers$ were inhibited by cinnarizine, so $Na^+/K^+$ excretion ratios were increased. Diuretic effects was showed in metoprolol alone treated group, but reduced when coadministered with cinnarizine.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.398.1-398.1
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• 2002

A new chiral derivatization agent with sugar moiety. 2, 3.4, 6-tetra-O-acetyl-D-galactopyranosyl isothiocyanate (GATC) was synthesized. Several $\beta$-blockers were investigated for the possible separation of the enantiomers by reversed-phase HPLC after derivatization with this new chiral derivatization agent (GATC). GATC was reacted readily with $\beta$-blockers at room temperature and the reaction mixture could directly be injected into the HPLC system. (omitted)

• Archives of Pharmacal Research
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• v.22 no.6
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• pp.608-613
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• 1999

Optimum conditions of chiral derivatization reaction of $\beta$-blockers (acebutolol, arotinolol, betaxolol, bisoprolol, celiprolol, metoprolol and pindolol) with (-)-menthyl chloroformate were investigated for the resolution by HPLC. With more than 30 times molar excess of (-)-methyl chloroformate chiral derivatization reactions were completed within one hour at room temperature except arotinolol and celiprolol. Diastereomeric derivatives of $\beta$-blockers were well resolved on the ODS column using acetonitrile-methanol-water as a mobile phase.