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| 2. |
- Dzhambazov, Balik, et al.
(author)
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In vitro screening for antitumour activity of Clinopodium vulgare L. (Lamiaceae) extracts.
- 2002
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In: Biological and Pharmaceutical Bulletin. - : Pharmaceutical Society of Japan. - 0918-6158 .- 1347-5215. ; 25:4, s. 499-504
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Journal article (peer-reviewed)abstract
- Aqueous extract of Clinopodium vulgare L. showed strong antitumour activity when tested in vitro on A2058 (human metastatic melanoma), HEp-2 (epidermoid carcinoma, larynx, human) and L5178Y (mouse lymphoma) cell lines-6 h after treatment disintegration of the nuclei and cell lysis started. Applied at a concentration of 80 microg/ml it reduced the cell survival to 1.0, 5.6 and 6.6%, respectively. The concentrations of aqueous extract inhibiting the growth of A2058, HEp-2 and L5178Y cells by 50% (IC50 values) were calculated to be 20, 10 and 17.8 microg/ml respectively. Two groups of active substances were detected: the first one, probably combining glycosides, influenced adhesion, while the second one caused massive cell vacuolisation. The chloroform extract, which contained ursolic acid and gentriacontan had also cytotoxic, however a little bit weaker effect. All changes observed were irreversible.
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| 3. |
- Hellgren, I, et al.
(author)
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Study of the beta1 adrenergic receptor expression in human tissues: immunological approach.
- 2000
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In: Biological & pharmaceutical bulletin. - : Pharmaceutical Society of Japan. - 0918-6158 .- 1347-5215. ; 23:6, s. 700-3
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Journal article (peer-reviewed)abstract
- Questions exist regarding tissue distribution of the beta1 adrenergic receptor (beta1-AR). The aim of this study was to investigate relative distribution patterns of the beta1-AR at the protein level in a variety of human tissues by Western blot analysis. The specificity of anti-peptide antibodies was confirmed both by Western blot with recombinant beta1-AR expressed as a membrane protein in E. coli and by immunoprecipitation of membranes from Sf9 cells infected with baculovirus to express the human recombinant beta1-AR. beta1-AR was found in all tissues examined. The relative amount of protein varied significantly between the tissues, from highest in lung and testis to very low in liver. beta1-ARs were rather abundant in heart, kidney, placenta, spleen and thyroid. These results reveal unique distribution of beta1-AR protein that suggests its tissue specific role. Moreover, our data demonstrate a high sensitivity of immunological detection that allows direct comparison of beta1-AR subtype expression and could be used for receptor study in biopsies available in limited amounts, such as human heart biopsy.
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| 4. |
- Miyake, Masateru, et al.
(author)
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Inhibitory Potency of Marketed Drugs for Ulcerative Colitis and Crohn's Disease on PEPT1
- 2017
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In: Biological and Pharmaceutical Bulletin. - : PHARMACEUTICAL SOC JAPAN. - 0918-6158 .- 1347-5215. ; 40:9, s. 1572-1575
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Journal article (peer-reviewed)abstract
- We investigate the inhibitory effect of marketed drugs for treatment of inflammatory bowel disease (IBD) such as ulcerative colitis (UC) and Crohn's disease (CD) on the uptake transporters of peptide transporter 1 (PEPT1), which are up-regulated under the inflamed condition. The uptake transport of glycylsarcosine, a typical substrate for PEPT1, was reduced to 60% only by 5-aminosalicylate at the clinically relevant concentration among tested marketed drugs in PEPT1 transfected HEK293 cell lines. These findings suggest that the inhibition of PEPT1, which were up-regulated in inflamed or non-inflamed site on UC and CD patients, contribute to the clinical effect of commercially available drugs for IBD patients through the inhibition of uptake of antigenic proinflammatory oligopeptides such as formyl-methionine (Met)-leucine (Leu)-phenylalanine (Phe) via PEPT1.
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| 6. |
- Pettersson, Jenny, et al.
(author)
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NMR metabolomic analysis of fecal water from subjects on a vegetarian diet
- 2008
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In: Biological and Pharmaceutical Bulletin. - : Pharmaceutical Society of Japan. - 0918-6158 .- 1347-5215. ; 31:6, s. 1192-1198
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Journal article (peer-reviewed)abstract
- A vegetarian diet rich in phytochemicals may prevent colon carcinogenesis by affecting biochemical processes in the colonic mucosa. Compounds passing the digestive system reaching the colon could potentially be detected in fecal water. We previously reported that intact fecal water samples from human volunteers significantly decreased prostaglandin production and COX-2 protein expression in colonic cells. The aim with the present study was to further study the composition of the fecal waters, using NMR spectroscopy and multivariate data analysis, and to trace the COX-2 inhibiting activity. Intact fecal water samples and fractions thereof were analyzed for their ability to inhibit prostaglandin E2 production in the human colon cell line HT-29. The majority of the tested aqueous phases derived from intact fecal water showed ability to inhibit prostaglandin production in cells (13.8+/-1.34% inhibition, p=0.01). NMR analysis indicated the presence of significant quantities of amino acids and fatty acids. Major metabolites included; acetic acid, butanoic acid, propanoic acid, glutamic acid and alanine. Smaller amounts of glycine and fumaric acid, which are known to have anti-inflammatory and anti-tumorigenic properties, were also detected. This study describes for the first time NMR metabolomic analysis of fecal water from subjects on a vegetarian diet.
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| 7. |
- Pettersson, Jenny, et al.
(author)
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The flavouring phytochemical 2-pentanone reduces prostaglandin production and COX-2 expression in colon cancer cells
- 2008
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In: Biological and Pharmaceutical Bulletin. - : Pharmaceutical Society of Japan. - 0918-6158 .- 1347-5215. ; 31:3, s. 534-537
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Journal article (peer-reviewed)abstract
- Many phytochemicals found in the diet may prevent colon carcinogenesis by affecting biochemical processes in the colonic mucosa. Inflammation and subsequent elevation of the enzyme cyclooxygenase-2 (COX-2) are two such factors involved in the development of colon cancer, and inhibition of these processes could be important targets for chemoprevention. We have previously shown COX-2 inhibitory activity locally in the colon; e.g. in human fecal water from a group of vegetarians. In this study we focus on 2-pentanone, a frequently occurring compound in common foods such as banana and carrot. The aim was to study the inhibitory effects on prostaglandin production and COX-2 protein expression in tumour necrosis factor-alpha stimulated colon cancer cells (HT29) by radioimmunoassay and Western blotting. 2-Pentanone inhibited both prostaglandin production and COX-2 protein expression in human colon cancer cells. A concentration of 400 mumol/l 2-pentanone inhibited the prostaglandin production by 56.9+/-12.9% which is in the same range as the reference compound NS398 (59.8+/-7.6%). The two highest concentrations of 2-pentanone were further analyzed by Western blot, and 400 micromol/l and 200 micromol/l 2-pentanone resulted in a 53.3+/-9.6% and +/-27.1% reduction of the COX-2 protein levels respectively. Further studies on flavouring compounds, for example 2-pentanone, as colon cancer chemopreventives would be very valuable, and such results may contribute to future dietary recommendations.
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| 8. |
- Ruhaak, Lucia Renee, et al.
(author)
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Evaluation of the Cyclooxygenase Inhibiting Effects of Six Major Cannabinoids Isolated from Cannabis sativa
- 2011
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In: Biological and Pharmaceutical Bulletin. - : Pharmaceutical Society of Japan. - 0918-6158 .- 1347-5215. ; 34:5, s. 774-778
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Journal article (peer-reviewed)abstract
- Cyclooxygenase enzymes (COX-1 and COX-2) catalyse the production of prostaglandins from arachidonic acid. Prostaglandins are important mediators in the inflammatory process and their production can be reduced by COX-inhibitors. Endocannabinoids, endogenous analogues of the plant derived cannabinoids, occur normally in the human body. The Endocannabinoids are structurally similar to arachidonic acid and have been suggested to interfere with the inflammatory process. They have also been shown to inhibit cancer cell proliferation. Anti-inflammatory effects of cannabinoids and endocannabinoids have been observed, however the mode of action is not yet clarified. Anti-inflammatory activity (i.e., inhibition of COX-2) is proposed to play an important role in the development of colon cancer, which makes this subject interesting to study further. In the present work, the six cannabinoids tetrahydrocannabinol (Delta(9)-THC), tetrahydrocannabinolic acid (Delta(9)-THC-A), cannabidiol (CBD), cannabidiolic acid (CBDA), cannabigerol (CBG) and cannabigerolic acid (CBGA), isolated from Cannabis sativa, were evaluated for their effects on prostaglandin production. For this purpose an in vitro enzyme based COX-1/COX-2 inhibition assay and a cell based prostaglandin production radioimmunoassay were used. Cannabinoids inhibited cyclooxygenase enzyme activity with IC50 values ranging from 1.7.10(-3) to 2.0.10(-4) M.
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