• Journal of Environmental Health Sciences
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• v.32 no.5 s.92
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• pp.440-445
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• 2006

Acetaminophen (paracetamol), generally used as a pain reducing agent, has good analgesic efficacy in toothaches and headaches, but is of little use in inflammatory and visceral pain. This study was performed to analyze the level of acetaminophen in the Kyongahn river and to investigate the ecological risks of target compounds. Sampling sites were Haesil, Soopyo, Wangsan, Kyongahn, Jiwol, Kwangdong, Paldang and they were analyzed in June and August, 2005. Acute toxicity of acetaminophen wwas evaluated for Daphnia magna. From the ecotoxicological results, environmental risk assessments were performed for acetaminophen residues in Kyongahn river to predict their potential adverse effect. Acetaminophen was detected at Kyonahn river, $0.439{\mu}g/l$). The toxic concentration of acetaminophen calculated with 48-h $LC_{50}$ values as 16.9 mg/l. These results indicated that acetaminophen had no significant ecotoxicological impact on short-term acute exposure.

• Herbal Formula Science
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• v.17 no.2
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• pp.123-132
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• 2009

Acetaminophen (AP) is widely used as an over-the-counter analgesic and antipyretic drug. AP-induced hepatotoxicity is a common consequence of AP overdose and may lead to acute liver failure. In this study, we investigated the liver damage in mice using single dose (300 mg/kg) of AP and the possible protective effects of administration (50-200 mg/kg body weight) of Joo-Juk on acetaminophen-induced liver damage in mice. The alanine aminotransferase (ALT), and aspartate aminotransferase (AST) activities were determined in the plasma of mice. The effect of Joo-Juk on lipid peroxidation product thiobarbituric reacting substances (TBARS) and some antioxidant enzymes superoxide dismutase (SOD), catalase, d-aminolevulinate dehydratase ($\sigma$-ALA-D) activities, and gluthathione peroxidase (GPx), were also evaluated in the mouse liver homogenate. AP caused liver damage as evident by statistically significant increased in plasma activities of AST and ALT. There were statistically significant losses in the activities of SOD, catalase, $\sigma$-ALA-D, and GPx and an increase in TBARS in the liver of AP-treated group compared with the control group. However, Joo-Juk was able to counteract these effects. These results suggest that Joo-juk can act as hepato-protectant against AP toxicity and is a good candidate for further evaluation as an effective chemotherapeutic agent.

• Herbal Formula Science
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• v.16 no.2
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• pp.183-191
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• 2008

Acetaminophen (N-acety1-p-aminophenol, paracetamol) is widely used as an over-the-counter analgesic and antipyretic drug. Intake of a over dose of acetaminophen may result in severe hepatic necrosis. In this study, we investigated the liver damage in mice using single dose (300 mg/kg) of acetaminophen and the possible protective effects of administration (50-200 mg/kg body weight) of SB-Ex on acetaminophen-induced liver damage in mice. The alanine aminotransferase (ALT), and aspartate aminotransferase (AST) activities were determined in the plasma of mice. The effect of SB-Ex on lipid peroxidation product thiobarbituric reacting substances (TBARS) and some antioxidant enzymes superoxide dismutase (SOD), catalase, d-aminolevulinate dehydratase (${\sigma}$-ALA-D) activities, and gluthathione peroxidase (GPx), were also evaluated in the mouse liver homogenate. Acetaminophen caused liver damage as evident by statistically significant increased in plasma activities of AST and ALT. There were general statistically significant losses in the activities of SOD, catalase, ${\sigma}$-ALA-D, and GPx and an increase in TBARS in the liver of acetaminophen-treated group compared with the control group. However, SB-Ex was able to counteract these effects. These results suggest that SB-Ex can act as hepatoprotectives against acetaminophen toxicity and is a good candidate for further evaluation as an effective chemotherapeutic agent.

• Preventive Nutrition and Food Science
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• v.2 no.1
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• pp.49-54
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• 1997

The modifying effects of Chelidonium majus L/(Papaeracea)herb extract(CH) ,and analgesic traditionally prescribed for gastric and duodenal ulcer patients, on gastric tumor development given Ν-methyl-Ν'-nitro-Ν-nitrosogyanidine(MNNG) were studied in sixty-four 6 week-old male Wistar rats. Group 1 rats were ini-tially given MNNG(200mg/kg b/w.) by gavage ar days 0 and 14 as well as saturated sodium chloride solution(S-NaCI, 1ml per rat) every 3 days during weeks 0 to 3(6 times) and then placed on basal diet containing 0.1 or 0.2% CH ofr 16 weeks from week 4. Rats of Groups 2 and 3 were treated with MNNG together with S-NaCI or saline(0.9% NaCI, 21ml per rat) respectively, timed as in Group 1 but without further treatment. All survival animals were killed at week 20 and histopathologically investigate. in the glandular stomach, the number of preneoplastic pepsinogen 1 altered pyloric glands(PAPGs) in the MNNG+S-NaCI→CH(0.1%) group(Group 1) was significantly smaller than in the MNNG+S-NaCI group(Group 2)(p<0.02). The inci-dences of forestomach neoplastic lesions (Papillomas and squamous cell carcinomas)also showed a tendency for decrease with the CH treatment. The results thus indicate that C"H exerts inhibitory effects on glandular for decrease with the CH treatment. The results thus indicate that CH exerts inhibitory effects on glandular stomach carcinogenesis in the rat, so that it may have potential as a chemopreventive agent for stomach cancer in man.

• Biomolecules & Therapeutics
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• v.22 no.3
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• pp.260-266
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• 2014

This study evaluated the pharmacokinetic profile and therapeutic efficacy of piroxicam (PX), a long acting non-steroidal anti-inflammatory drug for the treatment of arthritis, following intra-articular (IA) injection in comparison to the pharmacokinetic profile and therapeutic efficacy of PX after intramuscular (IM) injection. In the pharmacokinetic study in rats, systemic exposure and pharmacokinetic parameters of PX after a single IA dose were compared with systemic exposure and pharmacokinetic parameters of PX after administration of the same dose IM (0.6 mg/kg). The anti-inflammatory and analgesic effects of IA PX were evaluated simultaneously in a monoiodoacetate-induced osteoarthritis rat model. The plasma PX concentration rapidly rose following IA injection, and it was comparable to the plasma PX concentration following IM injection, suggesting the rapid efflux of the drug molecule from the joint cavity. However, in the efficacy study, the IA PX administration significantly reduced the knee swelling by reducing the level of prostaglandin $E_2$ in the joint, compared to that following administration of IA vehicle and after administration of the IM PX dose. In addition, we found that the anti-inflammatory and anti-nociceptive efficacies of IA PX were synergistically increased upon co-treatment with hyaluronic acid (HA), a potent agent for the treatment of osteoarthritis, at the weight ratio of 1:1 or 1:2, and these effects were more pronounced than those following administration of HA or PX alone. In conclusion, this study demonstrated the efficacy of the IA use of PX alone and/or in combination with HA in osteoarthritis.

• Journal of Pharmaceutical Investigation
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• v.31 no.4
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• pp.217-224
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• 2001

To develop a novel transdermal delivery system of loxoprofen (LP), a potent antiinflammatory and analgesic agent, the effects of various vehicles and penetration enhancers on the skin permeation of LP from solution formulations were investigated. The permeation rate of LP through excised guinea pig skin was measured using a side-by-side permeation system at $32^{\circ}C$. The solubilities of LP in various vehicles were determined by the equilibrium solubility method, and partition coefficients $(P_c)$ were determined. The solubility of LP increased in the rank order of water & isopropyl myristate (IPM) & glyceryl dicaprylate/dicaprate & propylene glycol dicaprylate/caprate & propylene glycol laurate (PGL) & polyethylene glycol 400 & diethylene glycol monoethyl ether (DGME) & ethanol. n-Octanol-water $P_c$ value was 15.5. Among pure vehicles tested, IPM and PGL showed highest fluxes of $89.9{\pm}5.0$ and $45.4{\pm}0.3\;{\mu}g/cm^2/hr$ from saturated solutions, respectively. However, it was not possible to demonstrate any correlation between the solubility of LP and its permeation rate, indicating the change in the barrier property of the skin and/or carrier mechanisms by vehicles tested. The addition of DGME to IPM or PGL markedly increased the solubility of LP, but the permeation rate did not decrease when the concentration of DGME in the cosolvent was increased upto 40%. The addition of linoleic acid (3%) in the cosolvent slightly increased the permeation rate, but others such as lauroyl sarcosine, fatty alcohols and fatty acids tested did not show enhancing effect. In conclusion, the DGME-IPM or DGME-PGL cosolvent system proved to be a good vehicle to enhance the skin permeation of LP.

• Proceedings of the Korean Society of Food Science and Nutrition Conference
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• 2001.12a
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• pp.69-73
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• 2001

Two opioid peptides, YPLDL and YPLDLF, were isolated from enzymatic digests of spinach ribulose-1, 5-bisphosphate carboxylase/oxygenase (RuBisCO) and named rubiscolin-5 and -6, respectively. These peptides were selective for delta-receptor and the latter was about 3 times more potent than the former. After oral administration in mice at the dose of 100 mg/kg, rubiscolin-6 showed analgesic activity in tail pinch test. It also stimutated learning performance at the same dose in passive avoidance experiment using step-through apparatus. An immunostimulating peptide, MITLAIPVNKPGR, was isolated from a trypsin digest of soybean protein and named soymetide. Immunostimulating activy of soymetide was mediated by fMLP receptor. Interestingly, after oral administration in rats at a dose of 300 mg/kg (po.), soymetide-4 (MITL) protected alopecia (hair-loss) induced by etoposide, a cancer chemotherapy agent. Stimulation of IL-1 release by the peptide was involved in the mechanism. Ovokinin(2-7), RADHPF, is a vasorelaxing peptide released from ovalbumin by the action of chymotrypsin. It lowered blood pressure of spontaneously hypersensive rats (SHR) after oral administration at a dose of 10 mg/kg. RPLKPW, which was designed by replacing 4 amino acid residues in ovokinin(2-7), exhibited hypotensive activity at a dose of 0.1 mg/kg (po.). This peptides was introduced into 3 homologous sites in soybean beta-conglycinin alpha' subunit by site-directed mutagenesis of the cDNA and expressed in E. coli. The minimum effective dose for hypotensive activity of the genetically modified beta-conglycinin alpha' subunit was 10 mg/kg (po.), which is about 1/200 that of ovalbumin.

• International Journal of Oral Biology
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• v.35 no.4
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• pp.215-220
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• 2010

Angelica decursiva has been used in Korean traditional medicine as an antitussive, an analgesic, an antipyretic and a cough remedy. However, its anti-cancer properties have not yet been well defined. In our current study, we report the cytotoxic activity and the mechanism of cell death induced by ethanol extracts of Angelica decursiva (EEAD) against the human oral cancer cell line, KB. Treatment of KB cells with EEAD induced apoptotic cell death in both a dose- and time-dependent manner as determined by MTT assay and DNA fragmentation. However, no cytotoxic effects of EEAD against human normal oral keratinocytes (HNOK) were evident. By western blot analysis, we found that apoptosis in KB cells is associated with a decrease in procaspase-7 and -9. In addition, the activation of caspase-7 was detectable in living KB cells by fluorescence microscopy. These results suggest that EEAD exhibits anti-cancer activity in KB cells via apoptosis and thus has potential as an anticancer agent in future drug development strategies.

• The Korean Journal of Pain
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• v.6 no.1
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• pp.32-39
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• 1993

Despite their sometimes fatal complications such as respiratory depression when used for postoperative pain control, intravenous and epidural narcotics remain the mainstay of treatment regimens. Because of the problems, anesthesiologists are seeking alternatives. We compared the analgesic effect and complications of continuous intravenous morphine with ketorolac. Ketorolac is a non-steroidal agent with potent analgesics and moderate anti-inflammatory activity. Forty ASA physical status I or II patients were given morphine(20 patients) or ketorolac(20 patients):In the morphine group, an initial bolus dose of 2 mg i.v. was given followed by continuous infusion at a rate of 1 mg/hr for 48 hours. The ketorolac group was given initial bolus of 30 mg i.v. This was followed by continuous infusion at a rate of 3.75 mg/hr for 48 hours using a Baxter Daymate Infuser. We checked systolic, diastolic and mean arterial pressure, heart rate, visual analogue scale(VAS) and the Prince Henry Score(PHS). This was done before the initial bolus, at 5, 15, 30 and 60 min, at 2, 6, 12, 24 and 48 hours after administration. We observed the side effects nausea and vomiting, pruritus, hypotension, somnolence, urinary retention and respiratory depression. From our study we believe ketorolac in selected patients, is as effective as morphine in alleviating postoperative pain without side effects of morphine.

• Biomolecules & Therapeutics
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• v.22 no.6
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• pp.558-562
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• 2014

Tramadol is an opioid analgesic agent that has been the subject of a series of case reports suggesting potential for misuse or abuse. However, it is not a controlled substance and is not generally considered addictive in Korea. In this study, we examined the dependence potential and abuse liability of tramadol as well as its effect on the dopaminergic and serotonergic systems in rodents. In animal behavioral tests, tramadol did not show any positive effects on the experimental animals in climbing, jumping, and head twitch tests. However, in the conditioned place preference and self-administration tests, the experimental animals showed significant positive responses. Taken together, tramadol affected the neurological systems related to abuse liability and has the potential to lead psychological dependence.