• Archives of Pharmacal Research
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• v.29 no.6
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• pp.459-463
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• 2006

Previous studies on the anticonvulsant activity of $N-Cbz-{\alpha}-aminoglutarmides$ have shown that the derivatives of $N-Cbz-{\alpha}-amino-N-alkoxy$ glutarimide have significant anticonvulsant activity. In addition, their anticonvulsant activities are dependent on the presence of N-alkoxy groups. Based on these results, a series of $N-Cbz-{\alpha}-amino-glutarimidooxy$ carboxylates derivatives (3a-e) were synthesized in moderate yield using a known synthetic procedure. Their anticonvulsant activities were evaluated using the maximal electroshock seizure (MES) test, the pentylene tetrazole induced seizure (PTZ) test, and the strychinine (Str) threshold test with the ultimate aim of developing more active anticonvulsants. None of the compounds (3a-e) tested showed anticonvulsant activity in the MES and PTZ test. However, all the compounds tested exhibited significant anticonvulsant activity in the Str. test. The most active compound in the Str. test was the methyl ester of $N-Cbz-{\alpha}-amino-glutarimidooxy$ acetic acid 3a $(ED_{50}\;=\;42.9\;mg/kg)$.

• Korean Journal of Microbiology
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• v.19 no.2
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• pp.52-62
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• 1981

In order to interpret the effect of IAA on the phosphate metabolism and biosynthesis of organic compounds, Saccharomyces uvarum were cultured in the media treated with various concnetration of IAA $(10^{-3}M,\;10^{-5}M,\;10^{-7}M)$. Sampling at the beginning and intervals of culture, yeast cells fractionated were traced the contents of inorganic phosphate and organic compounds of various fractions. 1. Growth of Saccharomyces uvarum were enhanced by IAA $(10^{-3}M,\;10^{-5}M)$ and phosphate contents in DNA and RNA fractions treated with IAA were accelerated 2.3 times and 2 times in comparison with those of control. 2. Amounts of poly-P"A" and poly-p"B" were increased but poly-P"C" decreased during the culture. Therefore, it is considered that poly-P"C" play on most important role as a phosphate pool. 3. It is suggested that because phosphate contents in DNA, protein and lipid fractions increased, inorganic phosphates required phosphates required RNA were transferred from phosphates in cytoplasm, because these increased slowly during the culture. 4. Alkali-labile protein were accelerated by IAA and alkali stable protein only were inhibiction were enhanced by IAA while, ethanol : ether soluble fraction was induced by $10^{-7}M$ IAA in comparison with those control.X> IAA in comparison with those control.

• Biomolecules & Therapeutics
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• v.6 no.2
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• pp.159-164
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• 1998

General pharmacological properties of recombinant human parathyroid hormone (hPTH) were examined. The administration of hPTH (7, 35 and 175 lU/kg sc) in mice had no effects in general behavior and central nervous system, and no influences on normal body temperature, writhing syndromes induced by 0.7% acetic acid solution and chemoshock produced by strychnine and pentetrazol solution. hPTH (9 and 44 lU/kg, sc) given to anesthetized rabbits showed no effect on blood pressure of carotid artery and respiration, and it did not influence the responses produced by injection of acetylcholine or epinephrine. It showed no direct effect at 4.4$\times$10$_{-2}$IU/ml in isolated stomach fundus and uterus of rats and ileum of guinea-pig, and it also showed no inhibition of contraction produced by acetylcholine, oxytocin, serotonin and histamine in the above-mentioned preparations. It did not influence intestinal propulsion at the doses of 7,35 and 175 lU/kg sc in mice. This drug exhibited no effect on urinary excretion at the doses of 7 and 35 lU/kg sc in rats. However, at a dose of 175 lU/kg sc, it showed a decreased urination along with decreased excretion of potassium, sodium and chloride ion. These results indicate that hPTH does not exert any of serious pharmacological effects except the inhibition of urination at a highest dose used.

• Biomolecules & Therapeutics
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• v.7 no.1
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• pp.89-96
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• 1999

CJ-50002 is an oral vaccine against V.vulnificus infection composed of whole cell lysate of V. vulnificus. The general pharmacological properties of CJ-50002 were evaluated in various animals and in vitro system. CJ-50002 at oral doses of 0.2, 2 and 20 mg/kg had no effect on general behavior in mice, chromo- and electro-convulsions in mice, writhing syndrome induced by acetic acid in mice, body temperature in rats, charcoal meal propulsion in mice and urine and electrolytes excretion in rats. However, oral administration of CJ-50002 at dose of 20 mg/kg prolonged the hexobarbital-inuced sleeping inducing time in mice. In anesthetized dogs, CJ-50002 showed no effect on blood pressure, heart rate and ECG but decreased the respiratory rate and femoral blood flow at dose of 20 mg/kg. p.o. CJ-50002 had no effect on the contractile response of the isolated guinea pig ileum to various spasmogen at concentrations of 0.2, 2 and 20 $\mu\textrm{g}$/ml, respectively. Since these pharmacological effects of CJ-500o2 were observed at dose much greater than those in clinical use (approximately 0.16 mg/kg, p.o.), it is likely that this vaccine may be relatively free of undesirable effects in clinical practice.

• Archives of Pharmacal Research
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• v.26 no.8
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• pp.659-665
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• 2003

We have studied the effect of rhEGF on the buccal mucosal ulcer healing. rhEGF was rapidly degraded upon incubation with the hamster buccal mucosal homogenates; The degradation of rhEGF was significantly inhibited by sodium lauryl sulfate (SLS). Eudispert hv hydrogel and Polycarbophil 974P hydrogel were prepared for rhEGF delivery and their mucoadhesiveness was measured by the $Instron^R$ method. The mucoadhesive force of Eudispert hv was significantly greater than that of Polycarbophil 974P. Moreover, rhEGF in Eudispert hv hydrogel remained stable for about 2 months. To evaluate the ulcer healing effect of rhEGF, the buccal mucosal ulcer was induced in golden hamsters using acetic acid. At 24 h after administration of rhEGF/Eudispert hv hydrogel, the ulcerous area was decreased compared with rhEGF solution and, as a result, the curative ratio was $36.8\pm5.68$%. By the addition of SLS (0.5%) to Eudispert hv hydrogel, the curative ratio increased 1.5 times. The mechanism of the action was probably due to a combination of protection of the drug against proteases present in mucosa and prolongation of the release of rhEGF from the formulation at the site of action.

• Journal of Microbiology and Biotechnology
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• v.34 no.3
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• pp.673-680
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• 2024

Kombucha, a fermented beverage, is gaining popularity due to its numerous beneficial health effects. Various substrates such as herbs, fruits, flowers, and vegetables, have been used for kombucha fermentation in order to enhance the flavor, aroma, and nutritional composition. This study aims to investigate the potential suitability of cascara as a novel ingredient for kombucha production. Our findings suggested that cascara is a suitable substrate for kombucha production. Fermentation elevated the total phenolic and flavonoid content in cascara, which enhanced the antioxidant, antibacterial, and prebiotic characteristics of the product. Furthermore, the accumulation of acetic acid-induced the pH lowering reached 2.7 after 14 days of fermentation, which achieved the microbiological safety of the product. Moreover, 14 days of fermentation resulted in a balanced amalgamation of acidity, sweetness, and fragrance according to sensory evaluation. Our findings not only highlight the potential of cascara kombucha as a novel substrate for kombucha production but also contribute to repurposing coffee by-products, promoting environmentally friendly and sustainable agricultural development.

• The Plant Pathology Journal
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• v.35 no.6
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• pp.662-673
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• 2019

Root-knot nematodes (RKNs) are among the most destructive plant-parasites worldwide, and RKN control has been attempted mainly using chemical nematicides. However, these chemical nematicides have negative effects on humans and the environment, thus necessitating the search for eco-friendly alternative RKN control methods. Here, we screened nematicidal lactic acid bacteria (LAB) isolated from kimchi and evaluated their efficacy as biocontrol agents against RKNs. Of 237 bacterial strains, Lactobacillus brevis WiKim0069 showed the strongest nematicidal activity against the second-stage juveniles (J2) of Meloidogyne incognita, M. arenaria, and M. hapla and inhibited the egg hatch of M. incognita. The culture filtrate of WiKim0069 had a pH of 4.2 and contained acetic acid (11,190 ㎍/ml), lactic acid (7,790 ㎍/ml), malic acid (470 ㎍/ml), and succinic acid (660 ㎍/ml). An artificial mixture of the four organic acids produced by WiKim0069 also induced 98% M. incognita J2 mortality at a concentration of 1.25%, indicating that its nematicidal activity was derived mainly from the four organic acids. Application of WiKim0069 culture filtrate suppressed the formation of galls and egg masses on tomato roots by M. incognita in a dose-dependent manner in a pot experiment. The fermentation broth of WiKim0069 also reduced gall formation on melon under field conditions, with a higher efficacy (62.8%) than that of fosthiazate (32.8%). This study is the first report to identify the effectiveness of kimchi LAB against RKNs and to demonstrate that the organic acids produced by LAB can be used for the RKN management.

• Horticultural Science & Technology
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• v.19 no.4
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• pp.459-464
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• 2001

Leaf disks from cultivar 'Kennebec' and one selection line (ND 860-2) were cultured on Murashige-Skoog medium with various combinations of indole acetic acid (IAA) and zeatin riboside. Shoots, roots and callus were induced at various combinations of plant growth regulator levels. The medium containing $3.5mg{\cdot}L^{-1}$ IAA and $4.0mg{\cdot}L^{-1}$ zeatin riboside produced the most plantlets. Rooted regenerants were grown in the greenhouse. The growth of regenerated plants obtained from the MS medium supplemented with $7.0mg{\cdot}L^{-1}$ IAA and $3.0mg{\cdot}L^{-1}$ zeatin riboside was significantly greater than those grown from nodal expalnts. In ND 860-2, a leaf chimera with chlorophyll deficient (light yellow) sectors was found in plants regenerated fiom leaf disks (grown on MS medium supplemented with $3.5mg{\cdot}L^{-1}$ IAA and $3.0mg{\cdot}L^{-1}$ zeatin riboside) but not in plants grown from nodal explants. The phenotypic variability was also observed in the tuber number, size and weight.

• The Korean Journal of Pharmacology
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• v.30 no.2
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• pp.227-242
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• 1994

The general pharmacological effects of a new anthracycline anticancer agent, DA-125 $[7-0-(2,\;6-dideoxy-2-fluoro-{\alpha}-L-talopyranosyl)-adriamycinone-14-{\beta}-alaninate{\cdot}HCI]$ were investigated in mice, rats, guinea pigs, rabbits and dogs. Intravenous administration of DA-125 presented no significant effects on the central and peripheral nervous systems of ICR mice except a decrease in the numbers of acetic acid-induced writhing response at a dose of 10 mg/kg. In anesthetized rats and dogs, DA-125 produced a transient depression of blood pressure and an increase in heart rate, but did not affect the peripheral blood flow in the isolated ear vessels of rabbits and the mechanical functions of the isolated hearts of guinea pigs. No significant effects were observed on the gastrointestinal functions and the contractilities of smooth muscle preparations obtained from guinea pig trachea, rabbit ileum, pregnant and non-pregnant uterus and vas deferens of rats. DA-125 Increased the contractility of the isolated ileum of guinea pigs in a dose range of $10^{-6}{\sim}10^{-9}g/ml$, and also increased, but weaker than adriamycin, the vascular permeability in rat skin. DA-125 had no effect on the kallikrein-induced increase in permeability and the permeability of the visceral organs. DA-125 did not adversely affect the liver function and the blood coagulation system, and did not induce hemolysis in vitro. It is concluded from the results that the general pharmachological effects of DA-125 are similar to or weaker than those of adriamycin, and that little adverse effects are anticipated with a therapeutic dose range.

• Korean Journal of Pharmacognosy
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• v.42 no.4
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• pp.317-322
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• 2011

Traditionally, the thorns of Gleditsia sinensis LAM. (GS) have been used for the treatment of various types of cancer and heart, skin, vascular and inflammatory diseases. However, there have been no reports on the antinociceptive or antiinflammatory properties of the thorn of GS. The present study was carried out to evaluate the anti-inflammatory and antinociceptive effects of the ethanolic extract of GS (EEGS) and its sub-fractions. The administration of EEGS (500 mg/kg) or its butanolic fraction (50 and 100 mg/kg) reduced the frequency of the acetic acid-induced writhing reflex in mice. In addition, the administration of the butanolic fraction of EEGS (50 and 100 mg/kg) prolonged the latency of reaction at the hot plate in mice. The butanolic fraction of EEGS also inhibited lipopolysaccharide-induced nitric oxide, prostaglandin $E_2$, and tumor necrosis factor-$\acute{a}$ production in the RAW 264.7 cell line. These results suggest that EEGS has anti-inflammatory and analgesic properties and is a potential therapeutic for inflammation and nociception.