• Title/Summary/Keyword: active compound

Search Result 968, Processing Time 0.025 seconds

Development of Biologically Active Compound from Edible Plant Sources-XV. Isolation of Triterpene Glycosides from the Leaf of Petasites japonicus (식용식물자원으로부터 활성물질의 탐색-XV. 머위(Petasites japonicus)잎으로부터 Triterpene 배당체의 분리)

  • Bang, Myun-Ho;Park, Jin-Kyu;Song, Myoung-Chong;Yang, Hye-Joung;Yoo, Jong-Su;Ahn, Eun-Mi;Kim, Dae-Keun;Baek, Nam-In
    • Applied Biological Chemistry
    • /
    • v.48 no.4
    • /
    • pp.421-424
    • /
    • 2005
  • The leaf of Petasites japonicus was extracted with 80% aqueous MeOH and solvent fractionated with EtOAc, n-BuOH and water successively. From the EtOAc fractions, two triterpenoids were isolated through the repeated silica gel and ODS column chromatographies. The chemical structures of the isolated terpenoids were determined as rosamutin (1) and peduncloside (2) through the interpretation of several spectral data including 2D-NMR such as $^1H-{^1H}$ gCOSY, gHSQC and gHMBC.

Inhibitory Effects of Quinizarin Isolated from Cassia tora Seeds Against Human Intestinal Bacteria and Aflatoxin $B_1$ Biotransformation

  • Lee, Hoi-Seon
    • Journal of Microbiology and Biotechnology
    • /
    • v.13 no.4
    • /
    • pp.529-536
    • /
    • 2003
  • The growth-inhibitory activity of Cassia tora seed-derived materials against seven intestinal bacteria was examined in vitro, and compared with that of anthraquinone, anthraflavine, anthrarufin, and 1-hydroxyanthraquinone. The active constituent of C. tore seeds was characterized as quinizarin, using various spectroscopic analyses. The growth responses varied depending on the compound, dose, and bacterial strain tested. At 1 mg/disk, quinizarin exhibited a strong inhibition of Clostridium perfringens and moderate inhibition of Staphylococcus aureus without any adverse effects on the growth of Bifidobacterium adolescentis, B. bifidum, B. longum, and Lactobacillus casei. Furthermore, the isolate at 0.1 mg/disk showed moderate and no activity against C. perfringens and S. aureus. The structure-activity relationship revealed that anthrarufin, anthraflavine, and quinizarin moderately inhibited the growth of S. aureus. However. anthraquinone and 1-hydroxyanthraquinone did not inhibit the human intestinal bacteria tested. As for the morphological effect of 1 mg/disk quinizarin, most strains of C. perfringens were damaged and disappeared, indicating that the strong activity of quinizarin was morphologically exhibited against C. perfringens. The inhibitory effect on aflatoxin $B_1$ biotransformation by anthraquinones revealed that anthrarufin ($IC_50,\;11.49\mu\textrm{M}$) anthraflavine ($IC_50,\;26.94\mu\textrm{M}$), and quinizarin ($IC_50,\;4.12\mu\textrm{M}$), were potent inhibitors of aflatoxin ${B_1}-8,9-epoxide$ formation. However, anthraquinone and 1-hydroxyanthraquinone did not inhibit the mouse liver microsomal sample to convert aflatoxin $B_1$ to aflatoxin ${B_1}-8,9-epoxide$. These results indicate that the two hydroxyl groups on A ring of anthraquinones may be essential for inhibiting the formation of aflatoxin ${B_1}-8,9-epoxide$. Accordingly, as naturally occurring inhibitory agents, the C. tora seed-derived materials described could be useful as a preventive agent against diseases caused by harmful intestinal bacteria, such as clostridia, and as an inhibitory agent for the mouse liver microsomal conversion of aflatoxin $B_1$ to aflatoxin ${B_1}-8,9-epoxide$.

Identification of AMPK activator from twelve pure compounds isolated from Aralia Taibaiensis: implication in antihyperglycemic and hypolipidemic activities

  • Li, Yuwen;Park, Jongsun;Wu, Yin;Cui, Jia;Jia, Na;Xi, Miaomiao;Wen, Aidong
    • The Korean Journal of Physiology and Pharmacology
    • /
    • v.21 no.3
    • /
    • pp.279-286
    • /
    • 2017
  • The root bark extract of Aralia taibaiensis is used traditionally for the treatment of diabetes mellitus in China. The total saponin extracted from Aralia Taibaiensis (sAT) has effective combined antihyperglycemic and hypolipidemic activities in experimental type 2 diabetic rats. However, the active compounds have not yet been fully investigated. In the present study, we examined effects of twelve triterpenoid saponins on AMP-activated protein kinase (AMPK) activation, and found that compound 28-O-${\beta}$-D-glucopyranosyl ester (AT12) significantly increased phosphorylation of AMPK and Acetyl-CoA carboxylase (ACC). AT12 effectively decreased blood glucose, triglyceride (TG), free fatty acid (FFA) and low density lipoprotein-cholesterol (LDL-C) levels in the rat model of type 2 diabetes mellitus (T2DM). The mechanism by which AT12 activated AMPK was subsequently investigated. Intracellular ATP level and oxygen consumption were significantly reduced by AT12 treatment. The findings suggested AT12 was a novel AMPK activator, and could be useful for the treatment of metabolic diseases.

Pyrophen Produced by Endophytic Fungi Aspergillus sp Isolated from Piper crocatum Ruiz & Pav Exhibits Cytotoxic Activity and Induces S Phase Arrest in T47D Breast Cancer Cells

  • Astuti, Puji;Erden, Willy;Wahyono, Wahyono;Wahyuono, Subagus;Hertiani, Triana
    • Asian Pacific Journal of Cancer Prevention
    • /
    • v.17 no.2
    • /
    • pp.615-618
    • /
    • 2016
  • Ethyl acetate extracts obtained from culture of endophytic fungi Aspergillus sp isolated from Piper crocatum Ruiz & Pav, have been shown to possess cytotoxic activity against T47D breast cancer cells. Investigations were here conducted to determine bioactive compounds responsible for the activity. Bioassay guided fractionation was employed to obtain active compounds. Structure elucidation was performed based on analysis of LC-MS, $^1H$-NMR, $^{13}C$-NMR, COSY, DEPT, HMQC, HMBC data. Cytotoxity assays were conducted in 96 well plates against T47D and Vero cell lines. Bioassay guided isolation and chemical investigation led to the isolation of pyrophen, a 4-methoxy-6-(1'-acetamido-2'-phenylethyl)-2H-pyran-2-one. Further analysis of its activity against T47D and Vero cells showed an ability to inhibit the growth of T47D cells with IC50 values of $9.2{\mu}g/mL$ but less cytotoxicity to Vero cells with an $IC_{50}$ of $109{\mu}g/mL$. This compound at a concentration of 400 ng/mL induced S-phase arrest in T47D cells.

Evidence for the Participation of ATP-sensitive Potassium Channels in the Antinociceptive Effect of Curcumin

  • Paz-Campos, Marco Antonio De;Chavez-Pina, Aracely Evangelina;Ortiz, Mario I;Castaneda-Hernandez, Gilberto
    • The Korean Journal of Pain
    • /
    • v.25 no.4
    • /
    • pp.221-227
    • /
    • 2012
  • Background: It has been reported that curcumin, the main active compound of Curcuma longa, also known as turmeric, exhibits antinociceptive properties. The aim of this study was to examine the participation of ATP-sensitive potassium channels ($K_{ATP}$ channels) and, in particular, that of the L-arginine-nitric oxide-cyclic GMP-$K_{ATP}$ channel pathway, in the antinociceptive effect of curcumin. Methods: Pain was induced by the intraplantar injection of 1% formalin in the right hind paw of Wistar rats. Formalin-induced flinching behavior was interpreted as an expression of nociception. The antinociceptive effect of oral curcumin was explored in the presence and absence of local pretreatment with L-NAME, an inhibitor of nitric oxide synthase, ODQ, an inhibitor of soluble guanylyl cyclase, and glibenclamide, a blocker of $K_{ATP}$ channels. Results: Oral curcumin produced a dose-dependent antinociceptive effect in the 1% formalin test. Curcumin-induced antinociception was not altered by local L-NAME or ODQ, but was significantly impaired by glibenclamide. Conclusions: Our results confirm that curcumin is an effective antinociceptive agent. Curcumin-induced antinociception appears to involve the participation of $K_{ATP}$ channels at the peripheral level, as local injection of glibenclamide prevented its effect. Activation of $K_{ATP}$ channels, however, does not occur by activation of the L-arginine-nitric oxide-cGMP-$K_{ATP}$ channel pathway.

Acaricidal Activity and Function of Mite Indicator Using Plumbagin and Its Derivatives Isolated from Diospyros kaki Thunb. Roots (Ebenaceae)

  • Lee, Chi-Hoon;Lee, Hoi-Seon
    • Journal of Microbiology and Biotechnology
    • /
    • v.18 no.2
    • /
    • pp.314-321
    • /
    • 2008
  • Acaricidal effects of materials derived from Diospyros kaki roots against Dermatophagoides farinae and D. pteronyssinus were assessed using impregnated fabric disk bioassay and compared with that of the commercial benzyl benzoate. The observed responses varied according to dosage and mite species. The $LD_{50}$ values of the chloroform extract of Diospyros kaki roots were 1.66 and $0.96{\mu}g/cm^2$ against D. farinae and D. pteronyssinus. The chloroform extract of Diospyros kaki roots was approximately 15.2 more toxic than benzyl benzoate against D. farinae, and 7.6 times more toxic against D. pteronyssinus. Purification of the biologically active constituent from D. kaki roots was done by using silica gel chromatography and high-performance liquid chromatography. The structure of the acaricidal component was analyzed by GC-MS, $^1H-NMR,\;^{13}C-NMR,\;^1H-^{13}C$ COSY-NMR, and DEPT-NMR spectra, and identified as plumbagin. The acaricidal activity of plumbagin and its derivatives (naphthazarin, dichlon, 2,3-dibromo-1,4-naphthoquinone, and 2-bromo-1,4-naphthoquinone) was examined. On the basis of $LD_{50}$ values, the most toxic compound against D. farinae was naphthazarin $(0.011{\mu}g/cm^2)$ followed by plumbagin $(0.019{\mu}g/cm^2),$ 2-bromo-1,4-naphthoquinone $(0.079{\mu}g/cm^2)$, dichlon $(0.422{\mu}g/cm^2)$, and benzyl benzoate $(9.14{\mu}g/cm^2)$. Additionally, the skin color of the dust mites was changed from colorless-transparent to dark brown-black by the treatment of plumbagin. Similar results have been exhibited in its derivatives (naphthazarin, dichlon, and 2-bromo-1,4-naphthoquinone). In contrast, little or no discoloration was observed for benzyl benzoate. From this point of view, plumbagin and its derivatives can be very useful for the potential control agents, lead compounds, and indicator of house dust mites.

Marine Algicolous Endophytic Fungi - A Promising Drug Resource of the Era

  • Sarasan, Manomi;Puthumana, Jayesh;Job, Neema;Han, Jeonghoon;Lee, Jae-Seong;Philip, Rosamma
    • Journal of Microbiology and Biotechnology
    • /
    • v.27 no.6
    • /
    • pp.1039-1052
    • /
    • 2017
  • Endophytic fungi have currently been acknowledged as the most promising source of bioactive compounds for drug discovery, and considerable progress has been made in exploring their diversity, species richness, and bioprospecting. Fungal endophytes from unique environmental settings offer a pool of potentially useful medicinal entities. Owing to the constant stresses imposed on macroalgae by marine environments, it is believed that algae and their associated endophytic symbionts represent a good source of structurally diverse bioactive secondary metabolites. Despite the proven significance of active metabolites of algal endophytes, little have been exploited. This review highlights the latest discoveries in algicolous endophytic research, with particular focus on the bioactive metabolites from algal endophytes. Compounds are classified according to their reported biological activities, like anticancer, antibacterial, antifungal, and antioxidant properties. Present experimental evidence suggests that a majority of the bioactive metabolites were reported from Phaeophyceae followed by Rhodophyceae and Chlorophyceae. An intensive search for newer and more effective bioactive metabolites has generated a treasure trove of publications, and this review partially covers the literature published up to 2016.

Antibacterial Activity of Rhus javanica against the Fish Pathogens Vibrio ichthyoenteri and Streptococcus iniae (오배자(Rhus javanica) 추출물의 어병세균 Vibrio ichthyoenteri와 Streptococcus iniae에 대한 항균활성)

  • Kim, Kyoung-Hoon;Kim, Ah Ra;Cho, Eun-Ji;Joo, Seong-Je;Park, Jong-Hoon;Moon, Ji-Young;Yum, Jong-Hwa;Kim, Tae Hoon;Kwon, Hyun-Ju;Lee, Hyun-Tai;Kim, Young-Man;Lee, Eun-Woo
    • Korean Journal of Fisheries and Aquatic Sciences
    • /
    • v.47 no.1
    • /
    • pp.18-22
    • /
    • 2014
  • The antibacterial activities of methanol extracts of 19 commercial herbal medicines were measured against the fish pathogens Vibrio ichthyoenteri and Streptococcus iniae, which cause several fish diseases. Rhus javanica showed the strongest antibacterial activity against V. ichthyoenteri and S. iniae. The methanol extract of R. javanica was extracted further using several organic solvents with different polarities. The extract from the ethyl acetate fraction showed strong activity against both fish pathogens. The minimum inhibitory concentration (MIC) of the R. javanica extract was $32{\mu}g/mL$ for V. ichthyoenteri and $128{\mu}g/mL$ for S. iniae. Further purification and isolation of the active compound (s) responsible for these activities and further study of the synergistic effect using combinations of antibiotics against pathogenic bacteria are needed.

Antimicrobial Activity of N-Acetyl-Phenylalanine Produced from Streptomyces sp. G91353 (Streptomyces sp. G91353이 생산하는 N-Acetyl-Phenylalanine의 항균활성)

  • Kwon, Oh-Sung;Park, Hae-Ryong;Yun, Bong-Sik;Hwang, Ji-Hwan;Lee, Jae-Chan;Park, Dong-Jin;Kim, Chang-Jin
    • Microbiology and Biotechnology Letters
    • /
    • v.34 no.4
    • /
    • pp.306-310
    • /
    • 2006
  • For screening of the compounds exhibiting antimicrobial activities against the D-alanyl-D-alanine of Gram positive bacteria, approximately 2,500 actinomycetes isolated from soil were examined far antimicrobial activity. In consequence, we recently isolated the Streptomyces sp. G91353 strain produced an active compound, A91353, that inhibits the growth of Gram positive bacteria. A91353 was identified as N-acetyl-phenylalanine by various spectroscopic methods. The minimum inhibitory concentration (MIC) values of N-acetyl-phenylalanine on Gram positive bacteria such as Streptococcus pyogenes 308A, Streptococcus pyogenes 77A were determined as $50{\mu}g/ml$, respectively, but did not effect on Gram negative strains. These results indicate that N-acetyl-phenylalanine have an antimicrobial activity, which may be caused by the disturbance of D-alanyl-D-alanine synthesis.

Inhibitory Effects of Licochalcone A and Isoliquiritigenin on Monocyte Adhesion to TNF-$\alpha$-activated Endothelium

  • Kwon Hyang-Mi;Lim Soon Sung;Choi Yean-Jung;Jeong Yu-Jin;Kang Sang-Wook;Bae Ji-Young;Kang Young-Hee
    • Nutritional Sciences
    • /
    • v.8 no.3
    • /
    • pp.153-158
    • /
    • 2005
  • Numerous natural herbal compounds have been reported to inhibit adhesion and migration of leukocytes to the site of inflammation Licorice extracts, which have been widely used in traditional Chinese medicinal preparation, possess various pharmacological effects. Isoliquiritigenin, a biogenetic precursor of flavonoids with various pharmacological effects, is a natural pigment present in licorice. We attempted to explore whether licorice extracts and isoliquiritigenin mitigate monocyte adhesion to tumor necrosis factor-$\alpha$ (TNF-$\alpha$)-activated human umbilical vein endothelial cells (HUVEC). In addition, it was tested whether the inhibition of monocyte adhesion to the activated HUVEC accompanied a reduction in vascular cell adhesion molecule-l expression(VCAM-l). Dry-roasted licorice extracts in methylene chloride but not in ethanol markedly interfered with THP-l monocyte adhesion to INF-$\alpha$-activated endothelial cells. licochalcone A compound isolated from licorice extract in methylene chloride appeared to modestly inhibit the interaction of THP-l monocytes and activated endothelium. In addition, isoliquiritigenin abolished the monocyte adhesion with attenuating VCAM-l protein expression on HUVEC induced by INF-$\alpha$. These results demonstrated that non-polar components from dry-roasted licorice extracts containing licochalcone A as well as isoliquiritigenin were active in blocking monocyte adhesion to cytokine-activated endothelimn, which appeared to be mediated most likely through the inhibition of VCAM-l expression on HUVEC. Therefore, licorice may hamper initial inflammatory events on the vascular endothelium involving induction of endothelial cell adhesion molecules.