• Title/Summary/Keyword: $MgB_4$ addition

Search Result 529, Processing Time 0.026 seconds

The Promotive Effects of Antioxidative Apigenin on the Bioavailability of Paclitaxel for Oral Delivery in Rats

  • Choi, Sang-Joon;Choi, Jun-Shik
    • Biomolecules & Therapeutics
    • /
    • v.18 no.4
    • /
    • pp.469-476
    • /
    • 2010
  • This study was to investigate the effect of apigenin on the bioavailability of paclitaxel after oral and intravenous administration in rats. The effect of apigenin on P-glycoprotein (P-gp), cytochrome P450 (CYP)3A4 activity was evaluated. The pharmacokinetic parameters of paclitaxel were determined in rats after oral (40 mg/kg) or intravenous (5 mg/kg) administration of paclitaxel with apigenin (0.4, 2 and 8 mg/kg) to rats. Apigenin inhibited CYP3A4 activity with 50% inhibition concentration ($IC_{50}$) of 1.8 ${\mu}M$. In addition, apigenin significantly inhibited P-gp activity. Compared to the control group, apigenin significantly increased the area under the plasma concentration-time curve (AUC, p<0.05 by 2 mg/kg, 59.0% higher; p<0.01 by 8 mg/kg, 87% higher) of oral paclitaxel. Apigenin also significantly (p<0.05 by 2 mg/kg, 37.2% higher; p<0.01 by 8 mg/kg, 59.3% higher) increased the peak plasma concentration ($C_{max}$) of oral paclitaxel. Apigenin significantly increased the terminal half-life ($t_{1/2}$, p<0.05 by 8 mg/kg, 34.5%) of oral paclitaxel. Consequently, the absolute bioavailability (A.B.) of paclitaxel was significantly (p<0.05 by 2 mg/kg, p<0.01 by 8 mg/kg) increased by apigenin compared to that in the control group, and the relative bioavailability (R.B.) of oral paclitaxel was increased by 1.14- to 1.87-fold. The pharmacokinetics of intravenous paclitaxel were not affected by the concurrent use of apigenin in contrast to the oral administration of paclitaxel. Accordingly, the enhanced oral bioavailability by apigenin may be mainly due to increased intestinal absorption caused via P-gp inhibition by apigenin rather than to reduced renal and hepatic elimination of paclitaxel. The increase in the oral bioavailability might be mainly attributed to enhanced absorption in the gastrointestinal tract via the inhibition of P-gp and reduced first-pass metabolism of paclitaxel via the inhibition of the CYP3A subfamily in the small intestine and/or in the liver by apigenin. It appears that the development of oral paclitaxel preparations as a combination therapy is possible, which will be more convenient than the i.v. dosage form.

Immunostimulating Effect of Goamshimshinhwan on Methotrexate-induced Immunosuppressed SD Rats (고암심신환(古庵心腎丸)이 methotrexate로 유발된 SD Rat의 면역기능저하에 미치는 영향)

  • Kang, Dae-Sung;Kwon, Eun-Hee;Lee, Yeon-Kyeong;Shin, Hyeon-Cheol;Kang, Seok-Bong;Park, Song-Kee
    • Journal of Physiology & Pathology in Korean Medicine
    • /
    • v.20 no.6
    • /
    • pp.1576-1583
    • /
    • 2006
  • In order to investigate the effect of Goamshimshinhwan(GASSW) on SD rats with deteriorated immunity caused by methotrexate. Methotrexate was fed to the SD rats once a day for 4 days. After the immune responses of the at a dosage 1,000, 500 and 250mg/kg/10ml. and the changes on body weight and gains, spleen weight, total blood leukocyte numbers, total lymphocyte numbers, the percentage of B-cell, T-cell, CD3+CD+4 T-cell, CD3+CD8+ T-cell and CD4+/CD8+ T-cell ratios in the bolld and spleen were observed. In addition, the serum IL-2 levels and productivity of IL-2 of splenic cells were also demonstrated in this study. The changes on body weight were increased significantly in 100 and 500mg/kg of GASSW groups and the changes on body gain were increased significantly in 1000mg/kg of GASSW groups as compared with control group. The changes on the spleen weight (absolutely or relatively) were increased significantly in all GASSW groups as compared with control group. The total blood leukocyte numbers were increased significantly in 1000 and 500mg/kg of GASSW groups as compared with control group. The total lymphocyte numbers were increased significantly in all GASSW groups in the blood and increased significantly in 1000 and 500mg/kg of GASSW goups in spleen as compared with control group. The percentage of B-cell and T-cell were increased significantly in 1000mg/kg of GASSW groups in the blood and increased significantly in 1000 and 500mg/kg of GASSW groups in spleen as compared with control group. The percentage of CD3+CD4+ T-cell and the serum IL-2 levels and productivity of IL-2 of splenic cells were increased significantly in 100 and 500 mg/kg of GASSW groups in the blood and spleen as compared with control group. The percentage of CD3+CD8+ T-cell were increased significantly in 1000mg/kg of GASSW groups only in spleen as compared with control groups. The CD4+/CD8+ T-cell ratios were increased significantly in 1000 and 500mg/kg of GASSW groups only in the blood as compared with control group. Goamshimshinhwan(GASSW) has immuno-stimulating effect on SD rats with deteriorated immunity caused by methotrexate.

Studies on the Bacterial Production of L-Glutamate from Acetate Part II. Cultural Conditon (초산을 이용한 글루타민산의 발효생산에 관한 연구 (제2보) 글루타민산 생성을 위한 발효조건)

  • 하덕모;노완섭;서동하
    • Microbiology and Biotechnology Letters
    • /
    • v.2 no.3
    • /
    • pp.141-147
    • /
    • 1974
  • The cultural conditions for L-glutamate production were investigated using Brevibacterium flavum nov. sp. D2209B, the most productive strain among 5 strains reported in preceeding paper. A temperature of 3$0^{\circ}C$ and a medium volume of 30 ml per 500-flask were selected as standard culture conditions. And the following results were obtained. 1. When the concentration of acetate in the medium was below 30 g per litre, the maximum amount of L-glutamate was accumulated. 2. KH$_2$PO$_4$, MgSO$_4$, FeCI$_3$ and MnCI$_2$ were required for the L-glutamate poduction, but the concentration of those inorganic salts little effected. 3. Signifcant amount of L-glutamate was accutnulated in the limited biotin concentration less than 0.3 ug per litre. 4. The addition of malic acid or succinic acid enhanced the accumulation. 5. The L-glutamate accumulation was related to the incubation time of seed; the amount of L-glutamate accumulated was maximum by inoculating 16-20 hour incubated seed. 6. In the medium containing sufficient amount of biotin for growth, L-glutamate accumulation was stimulated by the addition of penicillin at appropreate time during incubation.

  • PDF

Effect of Milk Containing Streptococcus thermophilus KACC 91147 on Blood Glucose Levels (Streptococcus thermophilus KACC 91147 첨가우유 섭취가 혈당치에 미치는 영향)

  • Ham, Jun-Sang;Jeong, Seok-Geun;Noh, Young-Bae;Shin, Ji-Hye;Han, Gi-Sung;Chae, Hyun-Seok;Yoo, Young-Mo;Ahn, Jong-Nam;Cho, Yong-Min;Kim, Geun-Bae
    • Food Science of Animal Resources
    • /
    • v.27 no.4
    • /
    • pp.496-500
    • /
    • 2007
  • The lactase activities of nine species of lactic acid bacteria were compared using the chromogenic substrate, $o-nitrophenyl-{\beta}-D-galactopyranoside$. Streptococcus thermophilus KACC 91147 had the highest lactase activity among a total of thirty strains of Lactobacillus and S. thermophilus tested, including commercial strains. S. thermophilus KACC 91147 released $0.30{\pm}0.12\;mg/mL$ of galactose in treated milk A ($10^7\;CFU/mL$) and $6.49{\pm}0.38\;mg/mL$ in treated milk B ($10^9\;CFU/mL$ milk) over 2 hours. In milk tolerance tests, the blood glucose level (BGL) of 6 volunteers (2 males and 4 females) clinically diagnosed as lactose intolerant increased 3.0 mg/dl after drinking milk A, but a significant (p<0.05) additional increase of $11.2{\pm}4.18\;mg/dl$ was found after drinking milk B. This result suggests that the addition of S. thermophilus KACC 91147 cells into milk aids the digestion of lactose in milk and ameliorates the symptoms of lactose-intolerant individuals due to the activity of lactase from the lactic streptococci.

Effect of Water Extract of Carthamus tinctorious L. on In Vitro Activity of T and B Lymphocytes (시험관내에서 홍화의 물 추출물이 T 및 B 림프구의 활성에 미치는 영향)

  • Choi, Youn-Hwa;Do, Jeong-Su;Nam, Sang-Yun
    • Korean Journal of Pharmacognosy
    • /
    • v.35 no.4 s.139
    • /
    • pp.330-337
    • /
    • 2004
  • Based on the traditional application of Carthamus tinctorious L. (CF) as a component of Korean medicinal decoctions, in the present study, we investigated in vitro an immunomodulatory activity of water extract of CF(WECF). Water extract of CF significantly increased the in vitro proliferative responses of spleen cells (SPC). However, addition of WECF during anti-CD3 activation resulted in a significant decrease in SPC proliferation. Flow cytometric analysis showed that WECF addition chanced T and B cell frequencies in anti-CD3-activated spleen cell populations. Using purified cells, it was revealed that WECF is mitogenic to B cells but rather inhibitory to T cell Proliferation. Upon anti-CD3 stimulation, high concentration (1 mg/ml) of WECF significantly inhibited T cell proliferation until day 2 of stimulation. At day 3, anti-CD3-activated cells exposed to WECF recovered their proliferation to the level comparable to control. Although B cell proliferation was also inhibited in proliferation at day 1, it recovered sooner and then was rather augmented by WECF at day 3. These data indicate that WECF down-regulates lymphocyte proliferation at early phase of activation but T cells are more vulnerable than B cells to WECF, However, CD4+ and CD8+ T cells did not differ in WECF-mediated immunotoxicity. Data of propidium iodide (PI) staining showed that WECF accelerates activated T cell, but not B cell, apoptosis and WECF concurrently inhibited cytokine production of activated T cells. Taken together, WECF exhibits B cell mitogenic activity and differential toxicity more pronounced to T cells, suggesting a possible in vivo application of WECF for specific control of T cells without alteration of B cell activity.

Effect of DA-6034, a Derivative of Flavonoid, on Experimental Animal Models of Inflammatory Bowel Disease

  • Kim, You-Sun;Son, Mi-Won;Ko, Jun-Il;Cho, Hyeon;Yoo, Moo-Hi;Kim, Won-Bae;Song, In-Sung;Kim, Chung-Yong
    • Archives of Pharmacal Research
    • /
    • v.22 no.4
    • /
    • pp.354-360
    • /
    • 1999
  • Inflammatory bowel disease (IBD) is a multifactorial disorder with unknown etiology and pathogenesis. DA-6034,$ 7-carboxymethyloxy-3^{l}, 4^{l},$ 5-trimethoxy flavone, is a synthetic flavonoid known to possess anti-inflammatory activity. This study was performed to evaluate the oral therapeutic effect of DA-6034 in three experimental animal models of IBD : two chemical-induced IBD models of rats and the human leukocyte antigen (HLA)-B27 transgenic rat model known to develop spontaneous colitis without the use of exogenous agents. Acute chemical colitis was induced by intracolonic instillation of 1.2 ml of 4% acetic acid solution. Prednisolone (1 mg/kg), sulfasalazine (100 mg/kg) and DA-6034 (0.3~3 mg/kg) were orally administered twice daily for 6 days in these rats. In addition, chronic chemical colitis was induced by intracolonic administration of trinitrobenzene sulfonic acid (TNBS) 30 mg in 50% ethanol and agents were orally administered for 6 or 20 days. In chemical-induced IBD models, all of these agents reduced the severity of colitis and specially, DA-6034 (3 mg/kg) showed more potent effect than other drugs in macroscopic lesion score. In HLA-B27 transgenic rats, DA-6034 (3 mg/kg) and prednisolone (0.5 gm/kg) were treated orally twice daily for 6 weeks. The HLA-B27 transgenic rats showed only mild colitis, compared with the chemical-induced colitis models. DA-6034 ameliorated the loose stool and decreased microscopic damage, which is the important indicator of this model. In conclusion, oral therapy of DA-6034 attenuated the macroscopic and histologic damages of the colon in all three experimental models of IBD, which suggest that DA-6034 could be a promising drug in the treatment of IBD.

  • PDF

Quality characteristics and antioxidant activity of roasted yakgwa according to the addition ratio of mealworm

  • Ji Eun Kim;Shin Youn Joo
    • Food Science and Preservation
    • /
    • v.31 no.2
    • /
    • pp.245-255
    • /
    • 2024
  • The proximate composition, quality characteristics, antioxidant activity, and sensory evaluation scores of yakgwa added with mealworm powder (MP) were examined. MP contained 5.83 wt% moisture, 55.70 wt% crude protein, 35.96 wt% crude fat, 3.70 wt% crude ash, and 2.43 wt% carbohydrate and feature total polyphenol and flavonoid contents of 406.52 mg GAE/100 g and 21.18 mg NE/100 g, respectively. The DPPH and ABTS•+ radical scavenging activities and the reducing power of MP were determined as 90.25%, 44.06%, and 1.74, respectively. Except for moisture and carbohydrate content, the proximate composition of mealworm yakgwa (MY) increased with the amount of MP increased. The pH of the dough increased with the addition of MP, whereas the expansion degree tended to decrease. Sugar content was highest at MP contents of 0 wt% and 12 wt% (FM4 group), and hardness was lowest in the FM4 group. With the increasing MP content, the L, b values and antioxidant activity increased, whereas a value decreased. The sensory evaluation scores for the overall preference, appearance, color, and taste were lowest in the FM4 group. These results suggested that MP contents of 6-9 wt% were optimal for mealworm-based yakgwa.

Immunomodulating Effect of Edible Mushrooms in Mice (식용버섯의 면역조절에 미치는 영향)

  • Park, Hyun-Ji;Heo, Yong;Kim, Jong-Bong
    • Journal of Life Science
    • /
    • v.21 no.4
    • /
    • pp.515-520
    • /
    • 2011
  • This study was carried out to evaluate the immunomodulatory capacity of edible mushrooms, including Lepista nuda, Corprinis comatus, Letinus edodes, and Pleurotus eryngii, in mice. BALB/c mice were administered 1, 50, and 500 mg/kg body weight of various mushrooms five times a week over 4 weeks through gastric intubation. The control mice were administered distilled water. No significant changes in body weight were observed. IL-4 and IFN${\gamma}$ production was evaluated with splenic T lymphocytes stimulated in vitro with phytohemagglutinins for 48 hr. The mice group administered L. edodes showed significantly higher ratio of IFN${\gamma}$ versus IL-4 than the other groups. In addition, the ratio of plasma IgG2a versus IgG1 was also significantly elevated in mice treated with L. edodes. However, no significant change was observed in ratio of IgG2a versus IgG1 in splenic B lymphocytes stimulated in vitro with lipopolysaccharides for 7 days. These results indicate that L. edodes can enhance type-1 helper T cell-mediated cellular immunity.

Studies on the Processing of Yeast Extract by Waste Brewery Yeast (맥주효모박을 이용한 효모추출물의 제조에 관한 연구)

  • 최형택;이성갑;손종연
    • The Korean Journal of Food And Nutrition
    • /
    • v.14 no.2
    • /
    • pp.161-166
    • /
    • 2001
  • The optimum condition for production of yeast extract by autolysis and enzymatic method were studied with waste brewers\` yeast. The major components of brewer\`s yeast in proximate compositions were carbohydrate(46.0%) and protein(41.7%). There was a little appreciable difference in the promaximate composition of waste brewers\` and bakery yeast. The major minerals were identified as K, P, Mg and Ca, and their contents were about 1,659.7%, 1,197.4mg%, 210.4mg% and 105.6mg%, respectively. The major vitamins were identified as vitamin C and vitamin B group, and their contents were about 7.9IU/100g and 4.2IU/100g, respectively. The optimum yeast concentration in the reaction suspension was 10% (w/v) waste brewer\`s yeast slurry. The protein content in brewer\`s yeast extract was increased with addition of NaCl as plasmolyzers. However, the plasmolyzer effect of ethanol a little showed as the concentration increasd from 3% ∼7%. The 5\`-nucleotides(5\`-GMP and 5\`-IMP) content in brewer\`s yeast extract was increased with addition of glucanase. The total content of 5\`-nucleotides (5\`-GMP and 5\`-IMP) increased by 160% than those by the autolysis of waste brewer\`s and bakery yeast.

  • PDF

Effect of Jehotang Extract on the Growth of Intestinal Bacteria and Immunostimulation (제호탕의 장내 세균 및 면역 활성에 미치는 연구)

  • Ji, Myoung-Soon;Park, Min-Jung;Lee, Mi-Young;Kim, Jong-Goon;Ko, Byoung-Seob
    • Korean Journal of Food Science and Technology
    • /
    • v.38 no.1
    • /
    • pp.104-108
    • /
    • 2006
  • Water extracts of Jehotang were evaluated for their growth-promoting effects on Bifidobacterium longum, Lactobacillus sp., L. acidophilus, and Clostridium perfringens. Addition of Jehotang water extract to modified EG media at 0.1 mg/mL increased growths of B. longum, Lactobacillus sp., and L. acidophilus, with 1.8-fold increase in growth of L. acidophilus compared to that of control. Studies on these strains by agar diffusion method showed Lactobacillus sp. and L. acidophilus were activated by addition of Jehotang extract at 10 mg/disc. Proliferation responses of mice splenocytes and Peyer's patch cells to ConA by LPS-stimulation at 500 mg/kg B.W./day Jehotang extract were investigated in vitro. Upon treatment of 1 mg/mL Jehotang water extract to mice, proliferations of splenocytes and Peyer's patch cells increased 1.4- and 1.6-fold compared to control, respectively. In mice administered Jehotang extract, production of intestinal secretory IgA (sIgA) increased 2.4-fold compared to control. These results indicate water extract of Jehotang stimulated intestinal immune system of mice. In mice treated with Jehotang extract, production of lymphocytes was 4% lower, whereas those of granulocytes and platelets were 4% and slightly higher than control, respectively.