권호 표지

Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology

  • Bimonthly
  • /
  • 1976-9148(pISSN)
  • /
  • 2005-4483(eISSN)

Domain

  • Health Sciences ＞ Biomedical Sciences

Aim & Scope

Biomolecules & Therapeutics (Biomolecules & Therapeutics) (Print ISSN 1976-9148, Online ISSN 2005-4483) is an international, peer-reviewed, open access journal that covers pharmacological and toxicological fields related to bioactive molecules and therapeutics. It was launched in 1993 as "The Journal of Applied Pharmacology (ISSN 1225-6110)", and renamed "Biomolecules & Therapeutics" (Biomol Ther: abbreviated form) in 2008 (Volume 16, No. 1). It is published bimonthly in January, March, May, July, September and November. All manuscripts should be creative, informative, and contribute to the development of new drugs. Articles in the following categories are published: review articles and research articles. The articles published in this journal are indexed and/or abstracted in: Science Citation Index Expanded®, PubMed/PubMed Central® (PMC), BIOSIS Previews®, Biological Abstracts® (Thomson ISI), and SCOPUS (Elsevier). Each article is made available under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/by-nc/4.0/) which permits unrestricted non-commercial use, distribution, and reproduction in any medium, provided the original work is properly cited. Papers focusing on clinical pharmacy or clinical pharmacology are not appropriate for Biomolecules & Therapeutics. Manuscripts based on experiments conducted with crude extracts will not be considered for peer review unless the manuscript provides the chemical profiles, specifications, and concentrations to assure the consistency of the quality of the crude extract using its authentic standard compound(s) together with its patent information (patented or applied for a patent).

KSCI KCI SCOPUS SCI SCIE

Volume 8 Issue 4

  1. 이경은;배영숙 285
    PDF
    The effects of the members of the same nuclear receptor superfamily (all-trans retinoic acid (RA), thyroid hormone(T3) or hydrocortisone) on proliferation and differentiation in the SK-N-SH neuroblastoma (NB) cell lines were studied. NB cells were treated with RA, T3, or hydrocortisone at concentration of 10$^{-6}$ M or 10$^{-8}$ M for 3 days or 7 days. RA induced concentration- and time-dependent morphologic differentiation(neurite outgrowth and microtubule-associated protein expression) and growth inhibition in NB cells. Treatment of 10$^{-7}$ M T3 for 7 days increased viability and differentiation of NB cells. Treatment of 10$^{-6}$ M hydrocortisone for 7 days increased viability of NB cells. Although these three effectors are members of the same receptor superfamily, the regulation of brain development may be carried out in a different manner.
  2. 임화경;김학성;최종원 293
    PDF
    Bergenin is a C-glucoside of 4-O-methyl gallic acid that has been isolated from the cortex of Mallotus japonicus (Euphorbiaceae). Acetylbergenin was synthesized by acetylation from bergenin to increase lipophilic and physiological activities. The therapeutic effects of bergenin and acetylbergenin were evaluated against carbon tetrachloride ($CCl_4$)-induced hepatotoxicity in rats. Bergenin and acetylbergenin were administered orally once daily for successive 5 days, after the intraperitoneal injection of a mixture 0.5 m1/kg of $CCl_4$ in olive oil (1:1). The substantially elevated serum enzymatic activities of alanine/aspartate aminotransferase, sorbitol dehydrogenase and ${\gamma}$-glutamyltransferase induced by $CCl_4$ were restored towards normalization by posttreatment with bergenin and acetylbergenin. Bergenin and acetylbergenin also significantly prevented the elevation of hepatic malondialdehyde formation and depletion of glutathione content induced by $CCl_4$ in a dose dependent fashion. In addition, the decreased activities of glutathione S-transferase and glutathione reductase were restored towards normalization. These results suggest that therapeutic effects of bergenin and acetylbergenin may be related complex mechanisms that involve prevention of lipid peroxidation and preservation of hepatic GSH. The results of this study clearly indicate that bergenin and acetylbergenin have potent hepatothrapeutic action against $CCl_4$-induced hepatotoxicity in rats. In addition, acetylbergenin 50 mgHg showed almost the same levels of hepatoprotective activity as those of bergenin 100 mgAg, indicating the fact that lipophilic acetylbergenin is more effective in the hepatoprotective action against $CCl_4$ than bergenin.
  3. 최병기;신혜주 299
    PDF
    The modulation of cytochrome P450(P450) activities and glutathione S-transferase (GST) was investigated after i.p. administration of glucose-diethyldithiocarbamate (Glu-DDTC) to rats. P450 1 A2 and 2El activities were inhibited by 60% 4 hr after the administration of 200 mg Glu-DDTC/kg and those activities were recovered to original levels 24 hr after dosing. In contrast, GST activities were enhanced up to 24 hr after dosing. These results seem to be due to the bifunctional activity of Glu-DDTC. Glu-DDTC acts as an inhibitor of P450 enzymes as well as inducer of GST enzyme. Glu-DDTC inhibited PNP hydroxylation (P450 2El) and ethoxycoumarin O-deethylation (P450 1A2) in a dose-dependent manner up to 200 mg/kg wherease it did not affect testosterone 6$\beta$-hydroxylation (P450 3A) and pentoxyresorufin O-dealkylation (P450 2B) activities. Induction of GST activity toward 1-chloro-2,4-dinitrobenzene (CDNB) and 1,2-dichloro-4-nitrobenzenen (DCNB) was dependent on the dose of Glu-DDTC and no species difference in the GST induction was seen between rat and mouse. Amoung GST subunits, Ya, Yb1 and partially Yb2 were induced by Glu-DDTC as conjugated by western blotting. The levels Yp, Yk and Yc subunits were not affected by Glu-DDTC treatment. Therefore the enhanced activity of GST toward CDNB and DCNB might be due to the induction of Ya, Ybl and partially Yb2 subunits. In conclusion, Glu-DDTC selectively inhibited P45O 1A2 and P450 2El activities whereas it enhanced Ya, Ybl subunits and partially Yb2 subunits of GST and the antimutagenic activity of this compound might be attributed from the modulation of these enzyme activities in animals.
  4. 정수연;정수연;정수연;강주희;최기환;김주일 305
    PDF
    The present study examined the effect of a methanol extract of Evodiae Fructus on the blood pressure in spontaneously hypertensive rats (SHR). The systolic blood pressure was measured after rats were pretreated with phentolamine, propranolol, or $N_{\omega}$-nitro-$_{L}$-arginine methyl ester(NAME) and subsequently received methanol extract of Evodiae Fructus. In SHR, intraperitoneal administration of methanol extract of Evodiae Fructus (0.5 mg/kg) produced antihypertensive effect that lasted for at least 4 hours. Antihypertensive effect of Evodiae Fructus was more stronger than that with $\alpha$-adrenergic receptor antagonist phentolamine and was not affected by $\beta$-adrenergic receptor antagonist propranolol. The antihypertensive effect of Evodiae Fructus was abolished by pretreatment of NAME. Our findings suggest Evodiae Fructus has an hypertensive effect, which may be mediated through nitric oxide synthesis.s.
  5. 권영혜;이윤욱;김해리 311
    PDF
    In this study we fed control diet and tryptophan supplemented diets containing 0.1,0.2,0.35% tryptophan to ICR mice for 1∼3 weeks to investigate the effects of tryptophan supplemented diet on pain sensitivity and the analgesic mechanism of serotonin. Animals fed tryptophan supplemented diets displayed increased antinociception when measured with hot plate and phenylquinone-writhing tests. And animals with typtophan supplemented diet had higher brain serotonin and 5-HIAA concentration than the control animals.
  6. 이영욱;김일웅;정지훈;라현오;최경범;이남인;손의동;허인회 318
    PDF
    We have examined inhibitory erects on gasritis using omeprazole-cholestyramine resinate, which has been developed to increase the stability of omeprazole, the well-known proton pump inhibitor, in an acidic condition. To test the pharmacological action of this, we investigated the effect of omeprazole-cholestyramine resinate on indomethacin-induced gastritis in rats. Omeprazole was used as a reference drug. Orally administered omeprazole-cholestyramine resinate inhibited the indomethacin-induced gastritis in a dose-dependent manner. The inhibitory effect of omeprazole-cholestyramine resinate on the gastritis was similar to that of reference drug. In addition, rectal adminstration of the omeprazole-cholestyramine resinate inhibited the indomethacin-induced gastritis in a dose-dependent manner. The inhibitory effect of omeprazole-cholestyramine resinate was equipotent to reference drug. The basal gastric acid secretion was decreased when it was administered either orally or rectally. This inhibition of omfprazole-cholestyramine resinate was similar to that of omeprazole. These data suggest that omeprazole-cholestyramine resinate inhibit the gastritis in rats, and are comparable to omeprazole available in market.
  7. 문삼영;신현진;신인철;고현철;엄애선;박정로;김범수;강주섭 325
    PDF
    The present study was designed to assess the role of spinal adenosine $A_2$ receptor in the regulation of cardiovascular functions such as mean arterial pressure (MAP) and heart rate (HR) in male Sprague-Dawley rats. Rats (250~300 g) were anesthetized with urethane and paralyzed with d-tubocurarine and artificially ventilated. blood pressure and HR were continuously monitored via a femoral catheter connected to a pressure transducer and a polygraph. Drugs were administered intrathecally using injection cannula through guide cannula which was inserted inthrathecally at lower thoracic level through a puncture of an atlantooccipital mombrane. Intrathecal injection of an adenosine $A_2$ receptor agonist, 5'-(N-cyclopropyl)-carboxamaidoadenosine (CPCA; 1, 2 and 3 nmol, respectively), produced a dose-dependent decrease in MAP and HR. Pretreatment with $N^{G}$-nitro-L-arginine methyl ester (L-NAME), a nitric oxide synthase inhibitor or 10 nmol of MDL-12,330, an adenylate cyclase inhibitor blocked significantly the depressor and bradycardic effect of 2 nmol of CPCA. But, Pretreatment with 3 nmol of bicuculline, gamma-aminobutyric acid A (GAB $A_{A}$) receptor antagonist, or 50 nmol of 5-aminovaleric acid, GAB $A_{B}$ receptor antagonist did not inhibit the depressor and bradycardic effect of 2 nmol of CPCA. These results indicate that adenosine $A_2$ receptor in the spinal cord plays an inhibitory role in the regulation of cardiovascular function and that the depressor and bradycardic action of adonosine $A_2$ receptor are mediated via the synthesis of nitric oxide and the activation of adenylate cyclase in the spinal cord of rats.s.s.s.
  8. 곽혜선;전인구 332
    PDF
    Physicochemical properties of aspalatone (acetylsalicylic acid maltol ester, AM), which has been recently found to have an antithrombotic effect, were studied in terms of solubility, dissolution, partition coefficient (Pc) and stability. The solubility of AM at 37$^{\circ}C$ was about 1.2 mg/ml and the P$_{c}$ value for n-octanol/water and chloroform/water was 11.4 and 382.6, respectively. Dissolution rates of AM at pH 1.2 and 6.8 were more than 80% within 30 min. The degradation of AM followed apparent first-order kinetics, and was dependent on temperature, pH and ionic strength. From the pH-rate profile, the optimal pH was found to be at around 4.0. Half-lives at pH 1.2 and 6.8 were 33.5 and 44.4 hr, respectively. The degradation rate of AM at pH 1.2 was somewhat faster than that of aspirin, but at pH 7.0, the degradation rate of AM was slower than that of aspirin.n.
  9. Lim, Dong-Yoon;Oh, Hyeong-Geun;Woo, Seong-Chang 338
    PDF
    The present study was attempted to determine the effect of 5'-(N'-ethylcarboxamido) adenosine (NECA), which is an potent $A_2$-adenosine receptor agonist, on catecholamine (CA) secretion evoked by cholinergic stimulation, membrane depolarization and calcium mobilization from the isolated perfused rat adrenal gland. NECA (20 nM) perfused into the adrenal vein for 60 min produced a time-related inhibition in CA secretion evoked by ACh (5.32x10$^{-3}$ M), high $K^{+}$(5.6x10$^{-2}$ M), DMPP (10$^{-4}$ M for 2 min), McN-A-343 (10$^{-4}$ M for 2 min), cyclopiazonic acid (10$^{-5}$ M for 4 min) and Bay-K-8644 (10$^{-5}$ M for 4 min). Also, in the presence of $\beta$,${\gamma}$-methylene adenosine-5'-triphosphate (MATP), which is also known to be a selective $P_{2x}$-purinergic receptor agonist, showed a similar inhibition elf CA release evoked by ACh, high potassium, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid. However, in adrenal glands preloaded with 20$\mu$M NECA for 20 min under the presence of 20$\mu$M 3-isobutyl-1-methyl-xanthine (IBMX), an adenosine receptors antagonist, CA secretory responses evoked by ACh, high potassium, DMPP, McN-A-343, Bay-K-8644 and cyclopiazonic acid were much recovered in comparison to the case of NECA-treatment only. Taken together, these results indicate that NECA causes the marked inhibition of CA secretion evoked by stimulation of cholinergic (both nicotinic and muscarinic) receptors as well as by membrane depolarization. This inhibitory effect may be mediated by inhibiting influx of extracellular calcium and release in intracellular calcium in the rat adrenomedullary chromaffin cells through the adenosine receptor stimulation. Therefore, it is suggested that the inhibitory mechanism of adenosine receptor stimulation may play a modulatory role in regulating CA secretion.n.n.
  10. Cha, Bae-Cheon 349
    PDF
    Mefenamic acid has been widely used as clinical drug for anti-inflammatory and analgesic. This drug was known to non-steroidal anti-inflammatory drugs (NSAIDs) such as aspirin, ibuprofen and indomethacin. Although the drugs which comprise this group are of diverse chemical structures, they all share the antipyretic, analgesic and anti-inflammatory actions which are characteristic of aspirin. Action of this drugs is caused by inhibitory effect of biosynthesis of prostaglandin that are synthesized from arachidonic acid via the endoperoxide biosynthesis pathway, the initial step of which is catalysed by cyclooxygenase. Mefenamic acid has more potent inhibitory action of prostaglandin biosynthesis than aspirin. Therefore, mefenamic acid is expected to have anticoagulant activity as aspirin-like drugs. This study was carried out to investigate the sinthesis of mefenamic acid derivatives from mefenamic acid and aromatic compound of antioxidant and its antioxidative and anticoagulant activities. Synthesis of mefenamic acid derivatives was conformed by conjugation as using esterification method. Biological activities was examined using effect of anticoagulant on bleeding time and effect of antioxidant by TBA method. As a result, SJ-202 showed strong antioxidative activity and anticoagulant activity among tested 4 compounds and exhibited similar activity to aspirin at anticoagulant activity.