Showing papers in "Archives of Pharmacal Research in 2001"
TL;DR: It is suggested that potent β-glucuronidase activity is a prime factor in the etiology of colon cancer.
Abstract: The fecal beta-glucuronidase activity of patients with colon cancer and healthy controls were measured to determine the relationship between the fluctuation of intestinal bacterial beta-glucuronidase and colon cancer. The fecal beta-glucuronidase activity of patients with colon cancer was 1.7 times higher than that of the healthy controls. However, when these fecal specimens were sonicated, the enzyme activity of patients with colon cancer was 12.1 times higher than that of the healthy controls. The fecal beta-glucuronidase activity of human intestinal bacteria was drastically induced by its substrate or the bile secreted after a subcutaneous injection of 1,2-dimethylhydrazine (DMH) and benzo[a]pyrene into rats. DMH- and benzo[a]pyrene-treated biles induced beta-glucuronidase activity in the human intestinal microflora by approximately 1.5- and 2.3-fold, respectively. They also induced beta-glucuronidase in E. coli HGU-3, which is a beta-glucuronidase-producing bacterium from the human intestine. D-saccharic acid 1,4-lactone similarly inhibited fecal beta-glucuronidase in several patients with colon cancer in addition to the healthy controls. This suggests that potent beta-glucuronidase activity is a prime factor in the etiology of colon cancer.
162 citations
TL;DR: The results strongly suggest that GRA can improve hyperglycemia in KKAy mice, possibly by blocking intestinal glucose absorption and inhibiting hepatic glucose-6-phosphatase, and GRP through the upregulation of adipocyte PPAR-γ protein expression as well as inhibiting intestine glucose absorption.
Abstract: The mechanisms responsible for the antidiabetic activity of both the white ginseng radix (Ginseng Radix Alba, GRA) and the rootlet (Ginseng Radix Palva, GRP) were investigated. After a four week oral administration, the fasting blood glucose levels in the GRA- and GRP-treated groups were lower when compared to the control group. To elucidate the hypoglycemic mechanism(s) of the ginseng radices, glucose absorption from the small intestine, hepatic hexokinase and glucose-6-phosphatase activities, in addition to PPAR-γ expression in adipose tissue were examined. The results strongly suggest that GRA can improve hyperglycemia in KKAy mice, possibly by blocking intestinal glucose absorption and inhibiting hepatic glucose-6-phosphatase, and GRP through the upregulation of adipocyte PPAR-γ protein expression as well as inhibiting intestinal glucose absorption.
115 citations
TL;DR: Six bioactive alkaloids were isolated by bioactivity-guided fractionation of a methanolic extract of the aerial part of Houttuynia cordata and several exhibited significant cytotoxicity against five human tumor cell lines in vitro.
Abstract: Six bioactive alkaloids, aristolactam B(1), piperolactam A(2), aristolactam A(3), norcepharadione B(4), cepharadione B(5) and splendidine(6) were isolated by bioactivity-guided fractionation of a methanolic extract of the aerial part ofHouttuynia cordata. Several of them exhibited significant cytotoxicity against five human tumor cell lines (A-549, SK-OV-3, SK-MEL-2, XF-498 and HCT-15)in vitro.
91 citations
TL;DR: It is demonstrated that curcumin inhibits invasion and induces apoptosis, proving the chemopreventive potential ofCurcumin, a dietary pigment in turmeric, in transformed breast cells.
Abstract: Curcumin, a dietary pigment in turmeric, posseses anti-carcinogenic and anti-metastatic properties. The present study was conducted to studyin vitro chemopreventive effects of curcumin in transformed breast cells. Here, we show that curcumin inhibits H-ras-induced invasive phenotype in MCF10A human breast epithelial cells (H-ras MCF10A) and downregulates matrix metalloproteinase (MMP)-2 dose-dependently. Curcumin exerted cytotoxic effect on H-ras MCF10A cells in a concentration-dependent manner. Curcumin-induced cell death was mainly due to apoptosis in which a prominent downregulation of Bcl-2 and upregulation of Bax were involved. We also suggest a possible involvement of caspase-3 in curcumin-induced apoptosis. Curcumin treatment resulted in the production of reactive oxygen species (ROS) in H-ras MCF10A cells. Apoptotic event by curcumin was significantly inhibited by pretreatment of an antioxidantN-acetyl-1-cysteine (NAC), suggesting redox signaling as a mechanism responsible for curcumin-induced apoptosis in H-ras MCF10A cells. Taken together, our results demonstrate that curcumin inhibits invasion and induces apoptosis, proving the chemopreventive potential of curcumin.
83 citations
TL;DR: Results suggest that CC-oil and CNA can regulate the triggering of hepatic drugmetabolizing enzymes by the formation of a glutathione-conjugate.
Abstract: GC-MS analysis on the essential oil (CC-oil) of Cinnamomum cassia stem bark led to the identification of cinnamaldehyde (CNA, 1), 2-hydroxycinnamaldehyde (2-CNA), coumarin (2), and cinnamyl acetate. The major volatile flavor in CC-oil was found to be 2-CNA. Coumarin was first isolated from this plant by phytochemical isolation and spectroscopic analysis. CNA and CC-oil showed potent cytotoxicity, which was effectively prevented by N-acetyl-L-cysteine (NAC) treatment. Intraperitoneal administration with CNA considerably decreased malondialdehyde (MDA) formation and glutathione S-transferase activity in rats. These results suggest that CC-oil and CNA can regulate the triggering of hepatic drug-metabolizing enzymes by the formation of a glutathione-conjugate.
78 citations
TL;DR: A survey of nonsteroidal antiinflammatory drugs in rheumatoid arthritis found that NSAIDs were slightly less active than FA and that the HPLC method was capable of distinguishing true antiaggregant agents like FA and NSAIDs from substances capable of inhibiting the precipitation of denatured protein aggregates.
Abstract: The activity of nonsteroidal antiinflammatory drugs (NSAIDs) in rheumatoid arthritis is not only due to the inhibition of the production of prostaglandins, which can even have beneficial immunosuppressive effects in chronic inflammatory processes. Since we speculated that these drugs could also act by protecting endogenous proteins against denaturation, we evaluated their effect on heat-induced denaturation human serum albumin (HSA) in comparison with several fatty acids which are known to be potent stabilizers of this protein. By the Mizushimas assay and a recently developed HPLC assay, we observed that NSAIDs were slightly less active [EC50 to approximately 10(-5)-10(-4) M] than FA and that the HPLC method was less sensitive but more selective than the turbidimetric assay, i.e. it was capable of distinguishing true antiaggregant agents like FA and NSAIDs from substances capable of inhibiting the precipitation of denatured protein aggregates. In conclusion, this survey could be useful for the development of more effective agents in protein condensation diseases like rheumatic disorders, cataract and Alzheimers disease.
61 citations
TL;DR: Four lignan xylosides and two neolignan glycosides were isolated from the stem and root barks of Ulmus davidiana var.japonica and their structures were identified by comparison of their spectral data with those reported in the literatures.
Abstract: Four lignan xylosides and two neolignan glycosides were isolated from the stem and root barks ofUlmus davidiana var.japonica. Their structures were identified as lyoniside, nudiposide, 5′-methoxyisolariciresinol-9′-O-β-D-xylopyranoside, isolariciresinol-9′-O-β-D-xylopyranoside, rel-trans-dihydrodehydroconiferyl alcohol 4′-O-α-L-rhamnopyranoside and icariside E3 by comparison of their spectral data with those reported in the literatures, respectively.
54 citations
TL;DR: Seven phenylpropanoid glycosides isolated from Clerodendron trichotomum showed potent inhibitory activities against HIV-1 integrase with IC50 values of 7.8 ± 3.6 and 13.7 ± 6.0 μM, respectively.
Abstract: Seven phenylpropanoid glycosides named acteoside (1), acteoside isomer (2), leucosceptoside A (3), plantainoside C (4), jionoside D (5), martynoside (6), and isomartynoside (7) were isolated fromClerodendron trichotomum. Compounds1 and2 showed potent inhibitory activities against HIV-1 integrase with IC50 values of 7.8 ± 3.6 and 13.7 ± 6.0 μM, respectively.
53 citations
TL;DR: The results indicate that EPC has an antifibrotic effect on fibrotic rats induced by BDL/S, and the morphological characteristics and expression of alpha smooth muscle like actin in fib rotic liver were improved in EPC treated fib Rotic liver.
Abstract: The antifibrotic effects of hot water extract (WEC), intracellular biopolymer (IPC) and extracellular biopolymers (EPC) from myceiial liquid culture ofCordyceps militaris on liver fibrosis were studied. Liver fibrosis was induced by a bile duct ligation and scission (BDL/S) operation, duration of 4 weeks in rats. In BDL/S rats, the levels of aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), total bilirubin in serum and hydroxyproline content in liver were dramatically increased. The WEC or IPC treatment (30 mg/kg/day for 4 weeks, p.o.) in BDL/S rats reduced the serum AST, ALT and ALP levels significantly (p<0.01). The EPC treatment (30 mg/kg/day for 4 weeks, p.o.) reduced the serum ALT, AST and ALP levels significantly (p<0.01). Malondialdehyde contents in liver treated with WEC, IPC or EPC were significantly reduced (p<0.05). But Liver hydroxyproline content was decreased only in EPC treated BDL/S rats to 55% that of BDL/S control rats (p<0.01). The morphological characteristics and expression of alpha smooth muscle like actin in fibrotic liver, which appeared in BDL/S control group were improved in EPC treated fibrotic liver. These results indicate that EPC (30 mg/kg/day for 4 weeks, p.o.) has an antifibrotic effect on fibrotic rats induced by BDL/S.
52 citations
TL;DR: A coumestan derivative, psoralidin was found to be a cytotoxic principle of the seeds ofPsoralea corylifolia L. (Leguminosae) with the IC50 values of 0.3 and 0.4 μg/ml against the HT-29 (colon) and MCF-7 (breast) human cancer cell lines, respectively.
Abstract: A coumestan derivative, psoralidin (1) was found to be a cytotoxic principle of the seeds ofPsoralea corylifolia L. (Leguminosae) with the IC50 values of 0.3 and 0.4 μg/ml against the HT-29 (colon) and MCF-7 (breast) human cancer cell lines, respectively. A coumarin, angelicin (2) was also isolated as a marginally cytotoxic agent along with an inactive compound, psoralen (3) from the plant. The isolates1–3 were not active against the A541 (lung) and HepG2 (liver hepatoma) cancer cell lines.
49 citations
TL;DR: Reversed-phase high performance liquid chromatographic method was applied for the determination of eleutheroside B and E in the various Canthopanax species collected in Korea, and in general, the contents in stems were higher than those in roots.
Abstract: Reversed-phase high performance liquid chromatographic method was applied for the determination of eleutheroside B and E in the various Acanthopanax species collected in Korea. The stationary phase used was Zorbax 300 SB C18 and a mobile phase program was used, which started at 6% acetonitrile for 2 min, and then a linear gradient was operated for the next 18 min to 17% acetonitrile at a flow rate of 1.0 ml/min. The column effluent was monitored at UV 210 nm. Identification was carried out by comparing the retention time and the LC/MS spectrum of each peak corresponding to eleutheroside B and E from sample with those of standards. In general, the contents of eleutheroside B and E in stems were higher than those in roots. Acanthopanax species could be classified into two groups based upon the contents of eleutheroside B and E: one group contains no or very little eleutheroside B and another contains both eleutheroside B and E.
TL;DR: Results suggest that costunolide-induced cell death is mediated by reactive oxygen species and the N-acetyl-L-cysteine antioxidant effectively prevented costunolia-induced cytotoxicity.
Abstract: In a course of obtaining more amount of bioactive costunolide and successive phytochemical isolation fromMagnolia sieboldii (Magnoliaceae), a novel acyclic monoterpene 1 named deoxygeraniol (2,6(E)-dimethyl-2, 6-octadiene) was isolated along with β-sitosterol 3-O-linoleate (2), trilinolein (3) and high amount of costunolide (4) in the pure state. The structure of compound1 was determined on the basis of spectroscopic data. Costunolide was found to induce apoptotic cell death in a dose-dependent manner by nucleosomal DNA ladder and flow cytometric analysis. Immunoblot analysis showed that the level of the anti-apoptotic protein, Bcl-2, was decreased, whereas the cleavage of poly-(ADP-ribose) polymerase was activated. Furthermore, the N-acetyl-L-cysteine antioxidant effectively prevented costunolide-induced cytotoxicity. These results suggest that costunolide-induced cell death is mediated by reactive oxygen species Received March 20, 2001
TL;DR: The proandrogenic effect of E. longifolia Jack supported the traditional use of this plant as an aphrodisiac in Malaysian men because it increases male virility and sexual prowess during sexual activities.
Abstract: It has been reported that Eurycoma longifolia Jack commonly known as Tongkat Ali has gained notoreity as a symbol of man's ego and strength by the Malaysian men because it increases male virility and sexual prowess during sexual activities. As such, the effects of 200, 400 and 800 mg/kg of butanol, methanol, water and chloroform fractions of E. longifolia Jack were studied on the laevator ani muscle in both uncastrated and testosterone-stimulated castrated intact male rats after dosing them for 12 consecutive weeks. Results showed that 800 mg/kg of butanol, methanol, water and chloroform fractions of E. longifolia Jack significantly increased (p<0.05) the leavator ani muscle to 58.56+/-1.22, 58.23+/-0.31, 60.21 +/-0.86 and 62.35 +/-0.98 mg/100 g body weight, respectively, when compared with the control (untreated) in the uncastrated intact male rats and 49.23+/-0.82, 52.23+/-0.36, 50.21+/-0.66 and 52.35+/-0.58 mg/100 g body weight, respectively, when compared to control (untreated) in the testosterone-stimulated castrated intact male rats. Hence, the pro-androgenic effect as shown by this study further supported the traditional use of this plant as an aphrodisiac.
TL;DR: Four prostane-type triterpenes were isolated from a methanol extract of Alismatis Rhizoma by bioassay-guided isolation usingin vitro cytotoxic assay and showed significant cytotoxicity against SK-OV3, B16-F10, and HT1080 cancer cell lines with ED50 values of 7.5, 7.9 μg/ml, respectively.
Abstract: Four prostane-type triterpenes were isolated from a methanol extract of Alismatis Rhizoma by bioassay-guided isolation usingin vitro cytotoxic assay. The compounds were identified as alisol B 23-acetate (1), alisol C 23-acetate (2), alisol B (3), alisol A 24-acetate (4) by spectroscopic methods. Amongst the compounds, alisol B (3) showed significant cytotoxicity against SK-OV3, B16-F10, and HT1080 cancer cell lines with ED50 values of 7.5, 7.5, 4.9 μg/ml, respectively.
TL;DR: Kojic acid is a potential inhibitor of NF-κB activation in human keratinocytes, and the hypothesis that NF-kB activation may be involved in kojic Acid induced anti-melanogenic effect is suggested.
Abstract: The activation of NF-kappaB induced by kojic acid, an inhibitor of tyrosinase for biosynthesis of melanin in melanocytes, was investigated in human transfectant HaCaT and SCC-13 cells. These two keratinocyte cell lines transfected with pNF-kappaB-SEAP-NPT plasmid were used to determine the activation of NF-kappaB. Transfectant cells release the secretory alkaline phosphatase (SEAP) as a transcription reporter in response to the NF-kappaB activity and contain the neomycin phosphotransferase (NPT) gene for the dominant selective marker of geneticin resistance. NF-kappaB activation was measured in the SEAP reporter gene assay using a fluorescence detection method. Kojic acid showed the inhibition of cellular NF-kappaB activity in both human keratinocyte transfectants. It could also downregulate the ultraviolet ray (UVR)-induced activation of NF-kappaB expression in transfectant HaCaT cells. Moreover, the inhibitory activity of kojic acid in transfectant HaCaT cells was found to be more potent than known antioxidants, e.g., vitamin C and N-acetyl-L-cysteine. These results indicate that kojic acid is a potential inhibitor of NF-kappaB activation in human keratinocytes, and suggest the hypothesis that NF-kappaB activation may be involved in kojic acid induced anti-melanogenic effect.
TL;DR: It is found that culture broths from two unidentified fungal strains exerted potent inhibitory activities on capillary-like tube formation of human umbilical vein endothelial cells (HUVEC) in vitro, suggesting that gliotoxin could be a useful compound for further study as an anti-angiogenic agent.
Abstract: In the search for new naturally occurring angiogenic inhibitor, we found that culture broths from two unidentified fungal strains exerted potent inhibitory activities on capillary-like tube formation of human umbilical vein endothelial cells (HUVEC)in vitro. Two active compounds were isolated by bioassay-guided separation and their structures were identified as gliotoxin (1) and its derivative methylthiogliotoxin (2) by spectroscopic analyses. These compounds significantly inhibited the migration of HUVEC assessed byin vitro wounding migration assay and exhibited at least 10 times more potent inhibition of proliferation of HUVECs as compared with that of cancer cell lines such as HeLa, MCF-7, and KB 3-1 cells. Especially, gliotoxin having disulfide group exerted more potent activities than methylthiogliotoxin, suggesting that gliotoxin could be a useful compound for further study as an anti-angiogenic agent.
TL;DR: This study investigated the effect that some polyacetylenes and protopanaxatriol, which were isolated from heated ginseng, have on inhibitingHelicobacter pylori growth.
Abstract: This study investigated the effect that some polyacetylenes and protopanaxatriol, which were isolated from heated ginseng (family Araliaceae), have on inhibitingHelicobacter pylori (HP) growth. Among the compounds tested, panaxytriol was quite effective in inhibiting HP growth with an MIC of 50 μg/ml. Ginsenoside Rh1 and protopanaxatriol weakly inhibited H+/K+-ATPase from a rat stomach.
TL;DR: To search for cytotoxic components from Allium victorialis, MTT assays on each extract and an isolated component, gitogenin 3-O-lycotetroside, were performed, suggesting that disulfides produced secondarily are the antitumor principles.
Abstract: To search for cytotoxic components fromAllium victorialis, MTT assays on each extract and an isolated component, gitogenin 3-O-lycotetroside, were performed against cancer cell lines. Cytotoxicities of most extract were shown to be comparatively weak, though IC50 values of CHCl3 fraction was found to be <31.3–368.4 μg/ml. From the incubated methanol extract at 36°C, eleven kinds of organosulfuric flavours were predictable by GC-MS performance. The most abundant peak was revealed to be 2-vinyl-4H-1,3-dithiin (1) by its mass spectrum. Further, this extract showed significant cytotoxicities toward cancer cell lies. Silica gel column chromatography of the n-butanol fraction led to the isolation of gitogenin 3-O-lycotetroside (3) along with astragalin (4) and kaempferol 3, 4′-di-O-β-D-glucoside (5). This steroidal saponin exhibited significant cytotoxic activities (IC50, 6.51–36.5 μg/ml) over several cancer cell lines. When compound3 was incubated for 24 h with human intestinal bacteria, a major metabolite was produced and then isolated by silica gel column chromatography. By examining parent- and prominent ion peak in FAB-MS spectrum of the metabolite, the structure was speculated not to be any of prosapogenins of3, suggesting that spiroketal ring were labile to the bacterial reaction. These suggest that disulfides produced secondarily are the antitumor principles.
TL;DR: Three varieties of methyl citrate and 1-methyl malate were isolated from the fruits of Opuntia ficus-indica throughin vitro bioassay-guided isolation for the inhibition on monoamine oxidase (MAO) and showed only marginal activity on MAO-A.
Abstract: Three varieties of methyl citrate and 1-methyl malate were isolated from the fruits ofOpuntia ficus-indica var.saboten Makino throughin vitro bioassay-guided isolation for the inhibition on monoamine oxidase(MAO). The IC50 values for MAO-B of 1-monomethyl citrate, 1,3-dimethyl citrate, trimethyl citrate and 1-methyl malate were 0.19, 0.23, 0.61 and 0.25 mM, respectively. However, on MAO-A, their inhibitions showed only marginal activity.
TL;DR: The result indicated that the resveratrol compound induced apoptosis of cancer cells, and may be a candidate for use in the development of potential cancer chemotherapeutic or cancer chemopreventive agents.
Abstract: Resveratrol, a trihydroxystilbene found in grapes and several plants, has been shown to be active in inhibiting multistage carcinogenic process. Using resveratrol as the prototype, we synthesized several analogs and evaluated their growth inhibitory effect using cultured human cancer cells. In the present report we show that one of the resveratrol analogs, 3, 5,2',4'-tetramethoxy-trans-stilbene, potentiated the inhibition of cancer cell growth. Prompted by the strong growth inhibitory activity of the compound (IC50; 0.8 microg/ml) compared to resveratrol (IC50; 18.7 microg/ml) in cultured human colon cancer cells (Col2), we performed an action mechanism study using the compound. The compound induced the accumulation of cellular DNA contents in the sub-G0 phase DNA contents of the cell cycle by in a time-dependent manner. The morphological changes were also consistent with an apoptotic process. This result indicated that the compound induced apoptosis of cancer cells, and may be a candidate for use in the development of potential cancer chemotherapeutic or cancer chemopreventive agents.
TL;DR: The phytochemical study of the aerial parts of Artemisia japonica ssp.
Abstract: The phytochemical study of the aerial parts of Artemisia japonica ssp. littoricola (Asteraceae) led to the isolation of two acetylenic compounds, (3R)-dehydrofalcarinol (2) and (3R)-dehydrofalcarindiol (6), two sesquiterpenes, 1β, 6α-dihydroxy-4(15)-eudesmene (5) and oplodiol (8), and four phenolic compounds, eugenol (1), vanillin (3), 3′-methoxy-4′-hydroxy-trans-cinnamaldehyde (4) andp-hydroxyacetophenone (7). Their structures were determined by chemical and spectroscopic methods.
TL;DR: The synthetic GMD, DMP, and GMD/DMP hydrogels were characterized by fourier transform infrared (FT-IR) spectroscopy and FITC-albumin loaded hydrogel release was affected by molecular weight of dextran and the presence ofdextranase in the release medium.
Abstract: Biodegradable hydrogels based on glycidyl methacrylate dextran (GMD) and dimethacrylate poly(ethylene glycol) (DMP) were proposed for colon-specific drug delivery. GMD was synthesized by coupling of glycidyl methacrylate with dextran in the presence of 4-(N,N-dimethyl-amino)pyridine (DMAP) using dimethylsulfoxide as a solvent. Methacrylate-terminated poly (ethylene glycol) (PEG) macromer was prepared by the reaction of PEG with methacryloyl chloride. GMD/DMP hydrogels were prepared by radical polymerization of phosphate buffer solution (0.1M, pH 7.4) of GMD and DMP, using ammonium peroxydisulfate (APS) and UV as initating system. The synthetic GMD, DMP, and GMD/DMP hydrogels were characterized by fourier transform infrared (FT-IR) spectroscopy. The FITC-albumin loaded hydrogels were prepared by adding FITC-albumin solution before UV irradiation. Swelling capacity of GMD/DMP hydrogels was controlled not only by molecular weight of dextran, but also by incorporation ratio of DMP. Degradation of the hydrogels has been studied in vitro with dextranase. FITC-albumin release from the GMD/DMP hydrogels was affected by molecular weight of dextran and the presence of dextranase in the release medium.
TL;DR: In this article, a new antioxidant monoterpene α-glycoside anomer was isolated from Paeonia suffruticosa along with known compounds, β-benzoyloxypaeoniflorin (2), paeonolide and mudanpioside H. Compound exhibited moderately potent radical scavenging activity on DPPH radical.
Abstract: α-Benzoyloxypaeoniflorin (1), a new antioxidant monoterpene α-glycoside anomer was isolated fromPaeonia suffruticosa along with known compounds, β-benzoyloxypaeoniflorin (2), paeonolide, paeoniflorin and mudanpioside H. The structure of1 has been determined by comparing spectral data with those of β-benzoyloxypaeoniflorin(2). Compound1 exhibited moderately potent radical scavenging activity on DPPH radical.
TL;DR: Two triterpenoids, 24-methylene-3, 4-seco-cycloart-4(28)-en-3-oic acid and 3-oxo-9ß-lanosta-7, 22Z,24-trien-26, 23-olide were isolated from Abies koreana, together with ß-sitosterol (2), maltol (3), ß
Abstract: Two triterpenoids, 24-methylene-3, 4-seco-cycloart-4(28)-en-3-oic acid (1) and 3-oxo-9s-lanosta-7, 22Z, 24-trien-26, 23-olide (6) were isolated fromAbies koreana, together with s-sitosterol (2), maltol (3), s-sitosterol-O-s-D-glucoside (4), and hexacosylferulate (5). The structures of the compounds were established based on the spectroscopic data. The cytotoxic activities of triterpenoids have been evaluated using the sulforhodamine B (SRB) method. Compound 1 showed moderate cytotoxicities against human lung carcinoma (A549), ovarian carcinoma (SK-OV-3), malignant melanoma (SK-MEL-2), and colon carcinoma (HCT-15) cell lines.
TL;DR: The methanolic extract of the aerial parts ofLactuca scariola showed strong radical scavenging activity, and the EtOAc soluble fraction exhibited a stronger activity than the others, and was purified by silica gel and Sephadex LH-20 column chromatography.
Abstract: The antioxidant activity ofLactuca scariola (Compositae) was investigated by measuring the radical scavenging effect on DPPH (1,1-diphenyl-2-picrylhydrazyl) radical The methanolic extract of the aerial parts ofLactuca scariola showed strong radical scavenging activity The EtOAc soluble fraction exhibited a stronger activity than the others, and was purified by silica gel and Sephadex LH-20 column chromatography Quercetin-3-O-P-D-glucopyranoside, luteolin-7-O-β-D-glucopyranoside, luteolin, quercetin and kaempferol, together with 11β,13-dihydrolactucin were isolated from the EtOAc soluble fraction as active ingredients
TL;DR: In this paper, the synthesis of new salicylamidoacetyl sulfonamides was investigated, which were tested for their analgesic and anti-inflammatory activities as well as ulcerogenic effects.
Abstract: The present investigation deals with the synthesis of some new salicylamidoacetyl sulfonamides3a,b, salicylamido ethylacetate4, salicylamido acetic acid hydrazide5, which is considered as the key intermediate for the synthesis of several series of new compounds such as salicylamido pyrazol 6 and pyrazolone 7.N-imido-derivatives9, 10, 11, thiadiazole13, oxadiazole14, 15, Schiffs bases16a-f. Cyclocondensation of Schiffs bases with thioglycolic acid gave thiazolidinone18a-c while with acetylchloride afforded azitidinones19a-c and with acetic anhydride gave 1,4-benzoxazepine-3,5-dione. Some of the compounds were tested for their analgesic and antiinflammatory activities as well as ulcerogenic effects. Some derivatives were more effective than salicylamide and ulcerogenic activity was variably lowered.
TL;DR: In this paper, repeated column chromatographic separation of the CH2Cl2 extract of Artemisia stolonifera (Asteraceae) led to the isolation of a triterpene (I), a sesquiter pene (II), two aromatic compounds (III andIV) and a benzoquinone (V).
Abstract: Repeated column chromatographic separation of the CH2Cl2 extract ofArtemisia stolonifera (Asteraceae) led to the isolation of a triterpene (I), a sesquiterpene (II), two aromatic compounds (III andIV) and a benzoquinone (V). Their structures were determined by spectroscopic means to be simiarenol (I), (1S,7S)-1β-hydroxygermacra-4(15),5, 10(14)-triene (II), 3′-methoxy-4′-hydroxy-trans-cinnamaldehyde (III), vanillin (IV) and 2,6-dimethoxy-1,4-benzoquinone (V), respectively. Among these products, compoundV showed significant cytotoxicity against five human tumor cell linesin vitro, A549 (non small cell lung adenocarcinoma), SK-OV-3 (ovarian), SK-MEL-2 (skin melanoma), XF498 (CNS) and HCT15 (colon) with ED50 values ranging from 1.33~4.22 βg/ml.
TL;DR: The elevated endogenous sphinganine acts as a contributing factor to the fumonisin-induced cell death in Chinese hamster ovary cells.
Abstract: Fumonisins are specific inhibitors of ceramide synthase in sphingolipid metabolism. An alteration in sphingolipid metabolism as a result of fumonisin exposure is related to cell death (Yooet al., 1992). The objective of this study was to investigate whether elevated free sphinganine levels are related to the sensitivity of cultured cells to fumonisin exposure. Fumonisin B1 elevated the intracellular free sphinganine concentrations in both LLC-PK1 and Chinese hamster ovary (CHO) cells. However, CHO cells are resistant to fumonisin cytotoxicity at 50 μM, while LLC-PK1 cells are sensitive at concentrations greater than 35 μM. The intracellular concentration of free sphinganine in LLC-PK1 cells treated at 50 μM fumonisin B1 for 72 h was approximately 1450 pmol/mg protein relative to the 37 pmol observed in the control culture. Under the same conditions, the population of apoptotic cells in the 50 μM fumonisin B1-treated culture was approximately 37% of the total compared to 12% in the control. The caspase III-like activity after 72 h in the 50 μM fumonisin B1-exposed culture increased to approximately 50 pmol/mg protein/hr compared to 6 pmol/mg protein/hr in the control. L-cycloserine, a serine palmitoyltransferase inhibitor, reduced the fumonisin B1-stimulated caspase III-like activity down to the control level. Under the same culture conditions, the intracellular concentration of free sphinganine after L-cycloserine plus fumonisin B1 treatment was 140 pmol/mg protein compared to 1450 pmol/mg protein in fumonisin B1 alone. The intracellular concentration of free sphinganine in CHO cells treated with 50 μM fumonisin B1 for 72 h was approximately 460 pmol/mg protein, indicating that the mass amount of elevated free sphinganine in the CHO cells was about 32% of that in LLC-PK1 cells. Adding exogenous sphinganine to the CHO cells along with 50 μM fumonisin B1 treatment for 72 h caused both necrosis and apoptosis. In conclusion, the elevated endogenous sphinganine acts as a contributing factor to the fumonisin-induced cell death.
TL;DR: Two sesquiterpenoids were isolated from the rhizome of Curcuma zedoaria and their structures were identified as ar-turmerone and β-Turmerone.
Abstract: In the course of searching for biologically active sesquiterpenoids fromCurcuma genus, two sesquiterpenoids were isolated from the rhizome ofCurcuma zedoaria (Zingiberaceae) Their structures were identified as ar-turmerone (1) and β-turmerone (2) The structure elucidation of compounds1 and2 was carried out by comparison of their physical and spectral data with previously reported values
TL;DR: Results indicate that MOAE inhibits immediate hypersensitivity reaction in vivo and in vitro, and has a significant inhibitory effect on anti-DNP lgE-induced tumor necrosis factor-α production from RPMC.
Abstract: We studied the effect of aqueous extract ofMagnolia officinalis bark (Magnoliaceae) (MOAE) on the immediate hypersensitivity reaction. MOAE (0.01 to 1 g/kg) dose-depen-dently inhibited compound 48/80 induced systemic anaphylaxis in rats. MOAE (0.1 and 1 g/kg) also significantly inhibited local immunoglobulin E (IgE)-mediated passive cutaneous anaphylactic reaction. When MOAE was pretreated at concentrations ranging from 0.01 to 1 g/kg, the levels of plasma histamine were reduced in a dose-dependent manner. MOAE (0.001 to 1 mg/ml) dose-dependently inhibited the histamine release from rat peritoneal mast cells (RPMC) activated by compound 48/80 or anti-dinitrophenyl (DNP) lgE. The level of cyclic AMP (cAMP) in RPMC, when MOAE was added, significantly increased compared with that of the normal control. Moreover, MOAE (0.01 to 1 mg/ml) had a significant inhibitory effect on anti-DNP lgE-induced tumor necrosis factor-α production from RPMC. These results indicate that MOAE inhibits immediate hypersensitivity reactionin vivo andin vitro.