• Preventive Nutrition and Food Science
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• 제1권1호
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• pp.106-110
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• 1996

Bromelain(EC 3.4.22.4), the collective name for the proteolytic enzymes found in tissues of the plant family Bromeliaceae(pineapple), has been used as a tenderizing agent in food processing, and as an antiinflammatory agent in pharmaceuticals. In this paper, we describe the simple purification method of bromelain using Korean pineapple fruit. After removing contaminants at 30% saturation of ammonium sulfate, the supernatant obtained was treated again with ammonium sulfate to 80% saturation. Wit the above salt fractionation, partially purified bromelain could be obtained. To get highly purified bromelain, the previous 30% to 80% ammonium sulfate treated precipitate was dialyzed against 25mM sodium acetate buffer(pH 5.0) followed by passing through a CM- cellulose cation exchange column. Fruit bromelain was eluted as a major peak at 0.5~0.8M NaCI gradient. The present method is simpler with high wield than the traditional purification method-acetone treatment and several consecutive chromatographic processes.

• Biomolecules & Therapeutics
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• 제9권4호
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• pp.298-306
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• 2001

To develop a novel transdermal delivery system of loxoprofen (LP), a potent antiinflammatory and analgesic agent, the effects of vehicle composition and drug loading dose on the skin permeation property were investigated. And in vivo skin absorption property studied by analysing the $C_{max}$ and AUC was investigated after applying the developed plaster systems on rabbit back skin. Addition of isopropyl myristate (IPM) and IPM-diethylene glycol monoethyl ether (DGME) cosolvent in the plaster showed higher permeation rates than those from propylene glycol laurate-DGME cosolvent systems. As the concentration of LP in the plaster increased from 0.56 mg/$\textrm{cm}^2$ to 1.19 mg/$\textrm{cm}^2$, the drug release and skin permeation rates increased linearly. At loading dose of 1.19 mg/$\textrm{cm}^2$, the flux reached 35.6 $\mu$g/$\textrm{cm}^2$/hr. New LP plasters showed a good adhesive property onto skin, and showed no crystal formation. The AU $C_{0-24hr}$ and $C_{max}$ after dermal application of LP plaster (60 mg/70 $\textrm{cm}^2$) were found to be 6951$\pm$230 ng.hr/ml and 400$\pm$44 ng/ml, respectively. And the plasma concentration maintained above 300 ng/ml up to 24 hr period. In the carrageenan-induced rat paw edema test, LP plaster showed similar inhibition rate with marketed ketoprofen (Ketoto $p^{R}$) plaster.aster.r.

• Archives of Pharmacal Research
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• 제29권2호
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• pp.165-171
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• 2006

Osteoarthritis is thought to be induced by the ageing-related loss of homeostatic balance between degeneration and repair mechanism around cartilage tissue in which inflammatory mediators such as reactive oxygen species, cytokines and prostaglandins are prone to overproduction under undesirable physiological conditions. Phlorotannins are unique polyphenolic compounds bearing dibenzo-1,4-dioxin skeleton which are not found in terrestrial plants but found only in some brown algal species such as Ecklonia and Eisenia families. Phlorotanninrich extracts of Ecklonia cava including LAD103 showed significant antioxidant activities such as DPPH radical scavenging, ferric ion reduction, peroxynitrite scavenging, and inhibition of LDL oxidation, indicating their possible antioxidative interference both in onset and downstream consequences of osteoarthritis. LAD103 also showed significant down regulation of $PGE_2$ generation in LPS-treated RAW 246.7 cells, and significant inhibition of human recombinant interleukin-$1{\alpha}$-induced proteoglycan degradation, indicating its beneficial involvement in pathophysiological consequences of osteoarthritis, the mechanism of which needs further investigation. Since LAD103 showed strong therapeutic potentials in arthritic treatment through several in vitro experiments, it is highly encouraged to perform further mechanistic and efficacy studies.

• Journal of Pharmaceutical Investigation
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• 제13권2호
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• pp.66-72
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• 1983

Ketoprofen, 2-(3-benzoyl phenyl) propionic acid, has many advantages over the other antiinflammatory drugs, such as salicylates, phenytbutazone, and indomethacin. According to the reports, ketoprofen is well tolerated by patients and has very low incidence of side effects and toxic reactions. Although ketoprofen is widely used as an antiinflammatory agent, it shows poor solubility in water. In order to enhance water solubility, ketoprofen was made as lysine salt, such as acetylsalicylate lysine salt, ibuprofen lysine salt and amino acid salt of phenylbuatzone. The purpose of this study was to compare with ketoprofen lysinate in aspect of binding to human serum albumin (HSA) were made, and the association constant and the number of binding site were obtained using difference spectrophotometry. The number of binding site of HSA for ketoprofen and ketoprofen lysinate appears to be 3.3,3.2 respectively and association constants were found as follow; HSA-ketoprofen $2.23{\times}10^4\;M^{-1}$, HSA-ketoprofen lysinate $1.02{\times}10^4\;M^{-1}$.

• Biomolecules & Therapeutics
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• 제9권3호
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• pp.188-193
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• 2001

Free radical scavengers or quenching agents for reactive oxygen species (ROS) present in consumable fruits, vegetables, and beverages have received considerable attention as potential antioxidants, and thus uses for treatment of several human diseases. In this study, grapevine shoot extract (GSE) containing high concentration of resveratrol and viniferine was evaluated for antioxidant potential and inhibition of pro-inflam-matory mediator production. Utilizing 1,1-diphenyl-2-picrylhydrazyl (DPPH) scavenging activity and xanthine oxidase (XOD) inhibition assay the GSE showed inhibitory effects of DPPH radical scavenging and XOD activity with the $IC_{50}$/ values of 34.5 and 155 $\mu\textrm{g}$/ml, respectively. In addition, GSE also exhibited the inhibition of prostaglandin E$_2$ (PGE$_2$) and nitric oxide (NO) production in lipopolysaccharide (LPS)-induced mouse macrophage RAW264.7 cells with the $IC_{50}$/ value of 6.4 and 14.5 $\mu\textrm{g}$/ml, respectively. This result suggests that grapevine shoot extract has the potential activity as a natural antioxidant or antiinflammatory agent.

• Toxicological Research
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• 제2권1호
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• pp.9-21
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• 1986

Teratological study on pranoprofen, as antiinflammatory agent, was conducted by oral intubation in Sprague-Dawley rats. Pranoprofen was administered doses of 1.0, 2.5 and 5.0mg/kg/day and doze of 0.5mg/kg/day of Indomethacin was used as positive control. The rats were dosed from day 7 to 17 of gestation. At necropsy on day 20 of gestation, pathologically changes of gastroin-testinal system, liver and adrenal gland were examined at the high dose administered group. There were no differences between control and treated group on the number of implantations, the number of alive and dead fetuses, tail length, and external visceral and skeletal malformations.

• Archives of Pharmacal Research
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• 제16권2호
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• pp.134-139
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• 1993

The molecular structure of acemetacin, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid carboxymethyl ester, was determined by single cystal X-ray diffraction analysis. The compound was recrystallized from a mixture of acetone and water in triclinic, space group P1, with a=7.796(1), b=10.245(2), c=13.542(3)$\AA,\;\alpha=97.35(1),\;\beta=96.34(1),\;\gamma=107.06(1)^\circ$, and Z=2. The calculated density is 1.422; the observed value is $1.42\;g/cm^3$. The structure was solved by the direct method and refined by full matrix least-squares procedure to the final R value of 0,037 for 2960 independent reflections. There are water molecules, which are thought to be co-crystallized during the evaporation procedure, with the ratio of one water per compound molecule in the crystal. The conformation of the compound is found to be very similar to that of indomethacin. The molecules are stabilized by three O-H.....O type intermolecular hydrogen bonds between the oxygen of water molecule and those of the compound.

• Archives of Pharmacal Research
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• 제3권1호
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• pp.17-21
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• 1980

A sensitive spectrophotofluorometric method was developed for the analysis of 2[[3-(trifluoromethyl)phenyl]amino]-3-phridine carboxylic acid (I) in urine. The method is based on the fluoroscence behavior of the I-aluminum complex in absolute ethanol. This fluorophore has activation and emission wavelengths of 355 and 450 nm, respectively. Optimum conditions for the reaction were investigated. The fluorescence was linear in the range of 0.25 3.0 ug of I/ml. Replicate studies of spiked urine samples, each containing 2.5 ug of I/ml showed good precision with a relative standard deviation of 0.019. Overall recovery percent from five spiked urine samples was 99.4 $\pm$1.32%.

• 약학회지
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• 제23권1호
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• pp.11-16
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• 1979

Benorylate and ethoxybenzamide have been used alone or in combination as an analgesic, antipyretic and antiinflammatory agent. We investigated the significance of the differences of analgesic activities between single and concurrent administration of benorylate and ethoxybenzamide and lorazepam in mice and also antipyretic activity between single and concurrent administration of benorylate and ethoxybenzamide in rats. 1). Concurrent administration of each half dose of benorylate and ethoxybenamide showed much inhibiting effect on the acetic acid-induced writhing syndrome of mice than the above drug alone, and the some increased analgesic response by hot plate method. 2). The synergistic and analgesic effect of combined administration of benorylate and lorazepam was found to be significant. 3). Antipyretic effect of half-dose combined administration of benorylate and ethoxybenzamide on the rat pyrexia induced by yeast(s.c.) and T.T.G. (i.v.) was shown to be similar to the effect of each drug.

• Environmental Analysis Health and Toxicology
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• 제17권3호
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• pp.253-259
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• 2002

The phototoxicity inhibitory activity of 15 natural products having antiinflammatory effect was screened by three in vitro methods: yeast growth inhibition test with Candida albicans, RBC photohemolysis and MTT assay. We induced phototoxic reaction by irradiating UVA (365 nm) on chlorpromazine (CPZ) that has been widely documented as phototoxic agent in clinical and experimental studies and then observed the effects of the natural products after treating them with CPZ. In yeast growth inhibition test, X. stramonium showed the inhibitory effect on the UVA phototoxicity and E. officinalis, Yeast, P. suffruticosa showed phototoxicity inhibitory effect in that their ％ hemolysis compared with control were 36.14${\pm}$ 2.69, 42.82${\pm}$1.35, 36.41${\pm}$0.48 on UVA. In MTT assay, all tested natural products increased cell viability compared with the control.