• Toxicological Research
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• v.29 no.3
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• pp.195-201
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• 2013

The anti-inflammatory effects of glycosaminoglycan (GAG) derived from Isaria sinclairii (IS) and of IS extracts were investigated in a complete Freund's adjuvant (CFA)-treated chronic arthritis rat model. Groups of rats were treated orally with 30 mg/kg one of the following: [1] saline control, extracts of [2] water-IS, [3] methanol-IS, [4] butanol-IS, [5] ethyl acetate-IS, or [6] Indomethacin(R) as the positive control for a period of two weeks. The anti-paw edema effects of the individual extracts were in the following order: water-IS ex. > methanol ex. > butanol ex. > ethyl acetate ex. The water/methanol extract from I. sinclairii remarkably inhibited UV-mediated upregulation of NF-${\kappa}B$ activity in transfected HaCaT cells. GAG as a water-soluble alcohol precipitated fraction also produced a noticeable anti-edema effect. This GAG also inhibited the pro-inflammatory cytokine levels of prostaglandin $E_2$-stimulated lipopolysaccharide in LAW 264.7 cells, cytokine TNF-${\alpha}$ production in splenocytes, and atherogenesis cytokine levels of vascular endothelial growth factor (VEGF) production in HUVEC cells in a dose-dependent manner. In the histological analysis, the LV dorsal root ganglion, including the articular cartilage, and linked to the paw-treated IS GAG, was repaired against CFA-induced cartilage destruction. Combined treatment with Indomethacin(R) (5 mg/kg) and IS GAG (10 mg/kg) also more effectively inhibited CFA-induced paw edema at 3 hr, 24 hr, and 48 hr to levels comparable to the anti-inflammatory drug, indomethacin. Thus, the IS GAG described here holds great promise as an anti-inflammatory drug in the future.

• Advances in Traditional Medicine
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• v.8 no.3
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• pp.302-310
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• 2008

Azadirachta indica A. Juss (N.O. Meliaceae), popularly known, as 'Neem' is an indigenous tree widely available in India. Almost every part of the tree has long been used in Unani system of medicine for the treatment of a variety of human ailments. The flowers have been mentioned as a remedy useful in controlling diabetes mellitus. The present study had been designed to investigate the hypoglycemic/anti-hyperglycemic effects of the methanolic extract of the flowers of A. indica (Gule-Neem) and its different fractions on normal, glucose fed hyperglycemic, adrenaline induced hyperglycemic and alloxan induced diabetic rats. The methanolic extract was resolved into water soluble and water insoluble fractions. Water soluble portion of the methanolic extract was found to possess significant blood sugar lowering effect in glucose-fed and adrenaline-induced hyperglycemic rats but it did not show such effect in normal and alloxan induced mild and severe diabetic rats. Water-soluble portion was fractionated by employing the polarity criterion with ethyl acetate and butanol. The ethyl acetate fraction was further fractionated into phenolic and non-phenolic fractions. Hypoglycemic effect of these fractions was also evaluated. The results suggest that the flowers of A. indica contain at least two different constituents, responsible for the said activity. These investigations validate the use of flowers of A. indica in diabetes by Unani physicians.

• Journal of Food Hygiene and Safety
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• v.14 no.4
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• pp.358-364
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• 1999

Propolis, a natural resinous compound collected from honey bees, contains many biochemical constituents and has been used in traditional medicines as early as 300 B.C. Recently, it has been reported to possess many biological activities such as antibacterial, antiviral, fungicidal, local anaesthetic, immunostimulating, antiinflammatory and free radical scavenging properties. This study was performed to investigate the pharmacological effects of the propolis extract and fractions on the gastric lesion and ulcer. The ethanol extract was fractionated with hexane, toluene and ethyl acetate. Followed by bioassay on antigastric and antiulcer activity. Propolis ethanol extracts(500, 750, 1,000, 1,500 and 2,000 mg/kg) showed the protective effect on HCl·ethanol-induced gastric lesion and the antisecretory effect against Shay’s gastric secretion in pylorus-ligated rats in a dose related manner. In the animal models of HCl·ethanol, aspirin-induced gastric lesion and Shay’s gastric secretion, the hexane and toluene fraction of propolis significantly reduced the length of gastric lesion and the acid secretion. These data showed that the gastric protective effects of propolis might result from reduction of acid secretion through the inactivation of H+/K+ATPase activity.

• Journal of the Korea Academia-Industrial cooperation Society
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• v.14 no.8
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• pp.3907-3915
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• 2013

Cudrania tricuspidata has been used for a long time as a traditional herb medicine in Korea nad China. This paper has shown the experimental results about the physiological activities of water-, ethanol-, ethyl acetate-soluble fractions from ethanolic extracts of leaves, stems and roots of Cudrania tricuspidata. The effects of these fractions on the growth of various cells have exhibited that the ethyl acetate fractions from leaves, stems and roots inhibited significantly the growths of macrophage(RAW 264.7 cell), melanoma cell(B16-F10 cell), fibroblast cell(CCD-986sk cell), and lung carcinoma cell(A549 cell). The water and ethanol fractions of leaves and ethanol fraction of stems demonstrated better antioxidant activities scavenging radicals than other fractions when compared with the concentrations of different fractions for scavenging free radical DPPH (di(phenyl)-(2,4,6-trinitrophenyl) iminoazanium).

• Preventive Nutrition and Food Science
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• v.18 no.1
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• pp.76-79
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• 2013

We evaluated antioxidant activities of heated pear juice (HPJ) exposed to 120, 130, and $140^{\circ}C$ for 2 hr. HPJ was partitioned using n-hexane, chloroform, ethyl acetate, n-butanol, and water. The ethyl acetate fraction treated at $130^{\circ}C$ for 2 hr showed strong antioxidant activity; thus, this extract was isolated and purified using silica gel column chromatography and preparative high performance liquid chromatography. The structure of the purified compound was determined using ultraviolet and mass spectrometry, $^1H$-nucelar magnetic resonance (NMR), and $^{13}C$-NMR. Antioxidant activities of the isolated compound were evaluated and compared with ${\alpha}$-tocopherol, ascorbic acid, and butylated hydroxytoluene (BHT) using DPPH and ABTS assays. The isolated compound was identified as 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one (DDMP). The DPPH radical-scavenging activity ($IC_{50}$) of DDMP occurred in the following order: ascorbic acid ($45.3{\mu}g/mL$) > ${\alpha}$-tocopherol ($69.2{\mu}g/mL$) > DDMP ($241.6{\mu}g/mL$) > BHT ($268.0{\mu}g/mL$). Furthermore, DDMP showed strong ABTS radical-scavenging activity (569.0 mg AA eq/g).

• Natural Product Sciences
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• v.3 no.1
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• pp.19-28
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• 1997

Constitutive cyclooxygenase (COX-I) is present in cells under physiological conditions, whereas inducible cyclooxygenase (COX-II) is induced by some cytokines, mitogens, and endotoxin presumably in pathological conditions such as inflammation. We have evaluated the inhibitory effects of solvent fractionated extracts of natural products on the activities of COX-I and COX-II. Oxygen uptake COX assay was performed, as a primary screening from the tissue extracts of bovine seminal vesicles (BSV), by monitoring the initial rate of oxygen uptake using an oxygen electrode. Additionally, we evaluated plant extracts for the inhibitory effects of COX-I (in HEL cells) and COX-II (in lipopolysaccharide activated J774A.1 macrophages) using thin layer chromatography of prostanoids produced from $^{14}C-labelled$ arachidonic acid (AA). The use of such models of COX-I and COX-II assay will lead to the identification of specific inhibitors of cyclooxygenases with presumably less side effects than present therapies. Inhibitory effects of 50 kinds of plant extracts on the COX-I and COX-II activities were determined and the active fractions were found in the ethyl acetate fractions of Dryopteris crassirhizoma (roots), Amomum cardamomum (roots), Triticum aestivum (seeds), Perilla sikokiana (leaves), Anemarrhena asphodeloides (roots). Especially, the ethyl acetate fraction of Dryopteris crassirhizoma (roots), which exhibited the strong inhibition against BSV COX $(IC_{50},\;65.4\;{\mu}g/ml)$, COX-I $(IC_{50},\;8.5\;{\mu}g/ml)$, and COX-II $(IC_{50},\;17.2\;{\mu}g/ml)$, is under investigation to isolate active principles using activity-guided fractionation method.

• Natural Product Sciences
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• v.3 no.1
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• pp.29-37
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• 1997

Protein Kinase C (PKC) is generally believed to play a central role in signal transduction, cellular growth control, gene expression, and tumor promotion. And it has been suggested that inhibitors of PKC might play important roles for the prevention and treatment of cancer. In order to investigate the possible inhibitors of PKC from natural products, PKC receptor binding assay was performed using bovine brain particulate as a source of PKC and the amount of $[^3H]Phorbol$ 12,13-dibutyrate (PDBu) bound to PKC was measured in the presence of test materials. Total methanol extracts from 100 kinds of natural products were partitioned into 3 fractions (n-hexane, ethyl acetate and aqueous layer) and their binding ability to the regulatory domain of PKC was evaluated. The ethyl acetate fractions of Morus alba $(roots,\;IC_{50}:\;156.6\;{\mu}g/ml)$, Rehmannia glutinosa $(roots,\;IC_{50}:\;134.3\;{\mu}g/ml)$, Lysimachia foenum-graecum $(roots,\;IC_{50}:\;167.8\;{\mu}g/ml)$, Polygonum cuspidata $(roots,\;IC_{50}:\;157.3\;{\mu}g/ml)$, Cnidium officinale $(aerial\;parts,\;IC_{50}:\;145.2\;{\mu}g/ml)$, and the hexane $(IC_{50}:\;179.3\;{\mu}g/ml)$ and the EtOAc fraction of Symplocarpus nipponicus $(roots,\;IC_{50}:\;155.9\;{\mu}g/ml)$ showed inhibitory activity of $[^3H]PDBu$ binding to PKC.

• Microbiology and Biotechnology Letters
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• v.24 no.1
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• pp.105-110
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• 1996

Mugwort has been known as a traditional substitutive foodstuff and as showing a physiologically beneficial function to a human being. Therefore, effect of mugwort extract in terms of mutagenicity and desmutagenicity was investigated to berify its function. Ethanol extract from mugwort did not exhibit any mutagenicity. On the contrary, inhibitory effects of the ethanol extract were observed on mutagenicity induced by aflatoxin $B_{1}(AFB_1)$, 3-amino-1,4-dimethyl-5H-pyrido[4,3-b]indole(Trp-P-1), 3-amino-1-methyl-5H-pyrido[4,3-b]indole(Trp-P-2) and 2-nitroflourene(2NF) using Salmonella typhimurium reversion assay. On direct-acting mutagen(2NF, 3${\mu}$g/plate), ethanol extract showed a slight inhibitory effect of 19.7~22.9%, however on indirect-acting mutagen such as AFB1(2${\mu}$g/plate), Trp-P-1(1${\mu}$g/plate) and Trp-P-2(1${\mu}$g/plate), we observed higher inhibitory effect of 47.9~61.2%, 64.1~70.7%, 67.4~78.7%, respectively. Step-wise fractionation of the ethanol extract was done by using hexane, chloroform, ethyl acetate and water to obtain effective fraction. Among them, hexane, chloroform, and ethyl acetate fractions showed high inhibition of 63.0~80.0%, 77.5~82.1%, and 68.5~83.1%, respectively on the mutagenicity of $AFB_1$ in Sal. typhimurium TA98. Consequently, these results indicated that mugwort extract contains some compound(s) which may show desmutagenicity.

• Korean Journal of Microbiology
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• v.50 no.1
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• pp.15-21
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• 2014

The promoting effect of Pseudomonas sp. P7014 on the mycelia growth of Pleurotus eryngii was investigated. An ethyl acetate fraction (F5) from the culture supernatant of the bacteria was confirmed to contain the growth promoting compound (GPC). The GPC was identified to be indole acetic acid (IAA) by TLC, HPLC, MS/MS, and NMR analyses. P. eryngii mycelia grew rapidly both on PDA and in PDB after the treatment of GPC. The promoting concentration of GPC was as low as 1.0 nM. Tryptophan, the aminated form of IAA, was confirmed to be the precursor of IAA. These results suggested that bacterial secreted compound was IAA and plays an important role in promoting growth of mushroom mycelia.

• Advances in Traditional Medicine
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• v.7 no.5
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• pp.477-484
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• 2008

The present study was aimed at investigating the hypouricemic and xanthine oxidase inhibitory activities of the various fractions of the hydromethanolic extract of the leaves of Coccinia grandis L. Voigt (Cucurbitaceae). The leaves of this species was used in traditional medicinal system for the treatment of gout, rheumatism, jaundice, bronchitis, fever, skin eruptions, wounds, etc. The degree of xanthine oxidase inhibition was determined in vitro by measuring the increase in absorbance at 295 nm associated with uric acid formation. Among the fractions tested, the chloroform fraction exhibited highest potency ($IC_{50}$ $17.8\;{\mu}g/ml$). This was followed by the pet-ether ($IC_{50}$ $29.7\;{\mu}g/ml$), ethyl acetate ($IC_{50}$ $41.2\;{\mu}g/ml$) and residual ($IC_{50}$ $47\;{\mu}g/ml$) fractions. The $IC_{50}$ value of allopurinol was $6.1\;{\mu}g/ml$. In addition, the hypouricemic and hepatic xanthine oxidase (XO)/xanthine dehydrogenase (XDH) inhibitory activities of the fractions were examined in vivo using oxonate (280 mg/kg, i.p.) induced hyperuricemic mice. At a dose of 200 mg/kg orally for 7 days, the pet-ether, chloroform and ethyl acetate fractions produced a significant (P < 0.01) reduction in serum urate level and also inhibited hepatic XO/XDH activities when compared to hyperuricemic mice. These inhibitory effects were weaker than that observed for the standard drug, allopurinol (10 mg/kg, p.o.). Lineweaver-Burk analysis of the enzyme kinetics indicated that the mode of inhibition was of a mixed type. These results suggest that the use of Coccinia grandis leaves for the treatment of gout could be attributed to its XO inhibitory activity.