• The Korean Journal of Mycology
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• v.35 no.2
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• pp.85-95
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• 2007

This study was carried out to investigate the physiological activities of the ethanol extract from Gymnopilus spectabilis mycelium (EGM) and of the supernatant obtained from fermentation broth (SGB). The contents of polysaccharides, phenol compounds and total ${\beta}-glucans$ of EGM were found to be 80.14%, 3.5 mg/ml and 5.91%, respectively and those for SGB were 78.68%, 3.32 mg/ml and 3.28%, respectively. Both EGM and SGB exhibited dose-dependent nitrate-scavenging abilities at pH 1.2. In addition, both EGM and SGB on the autoxidation rate of the linoleic acid demonstrated powerful antioxidant activities at 1 mg/ml level. With respect to fibrolytic activity, EGM showed 1,180 unit/g, which was the same activity as streptokinase, while SGB was 1,011 unit/g. The angiotensin converting enzyme inhibition activity of EMG determined by both the normal and pretreatment methods were estimated to be 8.2% and 10.2%, respectively. However, SGB showed no corresponding activity. The growth inhibitory effects of EGM on AGS, A549, HeLa and NCTC cells were over 58.88%, respectively. And the growth inhibitory effects of the SGB on HeLa and NCTC cells were 44.92 and 76.76%, respectively. Also, EGM and SGB activated the components of the alternative complement pathway from 51 and 62% at the concentration of 100 mg/ml, The xanthine oxidase inhibition activities of EGM and SGB (1 mg/ml) were 9.53 and 16.92%, respectively.

• Asian Pacific Journal of Cancer Prevention
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• v.16 no.16
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• pp.7179-7188
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• 2015

Cancer is a major health obstacle around the world, with hepatocellular carcinoma (HCC) and colorectal cancer (CRC) as major causes of morbidity and mortality. Nowadays, there isgrowing interest in the therapeutic use of natural products for HCC and CRC, owing to the anticancer activity of their bioactive constituents. Boswellia serrata oleo gum resin has long been used in Ayurvedic and traditional Chinese medicine to alleviate a variety of health problems such as inflammatory and arthritic diseases. The current study aimed to identify and explore the in vitro anticancer effect of B. Serrata bioactive constituents on HepG2 and HCT 116 cell lines. Phytochemical analysis of volatile oils of B. Serrata oleo gum resin was carried out using gas chromatography-mass spectrometry (GC/MS). Oleo-gum-resin of B. Serrata was then successively extracted with petroleum ether (extract 1) and methanol (extract 2). Gas-liquid chromatography (GLC) analysis of the lipoidal matter was also performed. In addition, a methanol extract of B. Serrata oleo gum resin was phytochemically studied using column chromatography (CC) and thin layer chromatography (TLC) to obtain four fractions (I, II, III and IV). Sephadex columns were used to isolate ${\beta}$-boswellic acid and identification of the pure compound was done using UV, mass spectra, $^1H$ NMR and $^{13}C$ NMR analysis. Total extracts, fractions and volatile oils of B. Serrata oleo-gum resin were subsequently applied to HCC cells (HepG2 cell line) and CRC cells (HCT 116 cell line) to assess their cytotoxic effects. GLC analysis of the lipoidal matter resulted in identification of tricosane (75.32%) as a major compound with the presence of cholesterol, stigmasterol and ${\beta}$-sitosterol. Twenty two fatty acids were identified of which saturated fatty acids represented 25.6% and unsaturated fatty acids 74.4% of the total saponifiable fraction. GC/MS analysis of three chromatographic fractions (I,II and III) of B. Serrata oleo gum resin revealed the presence of pent-2-ene-1,4-dione, 2-methyl- levulinic acid methyl ester, 3,5- dimethyl- 1-hexane, methyl-1-methylpentadecanoate, 1,1- dimethoxy cyclohexane, 1-methoxy-4-(1-propenyl)benzene and 17a-hydroxy-17a-cyano, preg-4-en-3-one. GC/MS analysis of volatile oils of B. Serrata oleo gum resin revealed the presence of sabinene (19.11%), terpinen-4-ol (14.64%) and terpinyl acetate (13.01%) as major constituents. The anti-cancer effect of two extracts (1 and 2) and four fractions (I, II, III and IV) as well as volatile oils of B. Serrata oleo gum resin on HepG2 and HCT 116 cell lines was investigated using SRB assay. Regarding HepG2 cell line, extracts 1 and 2 elicited the most pronounced cytotoxic activity with $IC_{50}$ values equal 1.58 and $5.82{\mu}g/mL$ at 48 h, respectively which were comparable to doxorubicin with an $IC_{50}$ equal $4.68{\mu}g/mL$ at 48 h. With respect to HCT 116 cells, extracts 1 and 2 exhibited the most obvious cytotoxic effect; with $IC_{50}$ values equal 0.12 and $6.59{\mu}g/mL$ at 48 h, respectively which were comparable to 5-fluorouracil with an $IC_{50}$ equal $3.43{\mu}g/mL$ at 48 h. In conclusion, total extracts, fractions and volatile oils of B. Serrata oleo gum resin proved their usefulness as cytotoxic mediators against HepG2 and HCT 116 cell lines with different potentiality (extracts > fractions > volatile oil). In the two studied cell lines the cytotoxic acivity of each of extract 1 and 2 was comparable to doxorubicin and 5-fluorouracil, respectively. Extensive in vivo research is warranted to explore the precise molecular mechanisms of these bioactive natural products in cytotoxicity against HCC and CRC cells.

• Applied Chemistry for Engineering
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• v.26 no.1
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• pp.111-115
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• 2015

Two new analogs of bestatin were prepared from $\small{D}$-leucine and $\small{D}$-valine in a stereoselective and efficient way. An aminopeptidase inhibitor bestatin shows significant biological effects on immunomodulation and is marketed for the treatment of acute myelocytic leukemia. The key intermediates, trans-oxazolidine methyl esters 2a and 2b, were obtained with more than 20 to 1 stereoselectivity in a one-pot procedure by the three cascade reactions between N-hydroxymethyl protected ${\alpha}$-amino aldehydes (4a and 4b) and phenylsulfonylnitromethane ($PhSO_2CH_2NO_2$) and the following in-situ ozonolysis. Basic hydrolysis of 2a and 2b, and then the peptide coupling with $\small{L}$-Leu-OMe produced the protected derivatives of two new bestatin analogs, 3a and 3b, respectively. The new isobutyl and isopropyl analogs of bestatin (1a and 1b) were produced in overall 51% and 38% yields, respectively, with high stereoselectivity from the corresponding protected ${\alpha}$-amino aldehydes 4 in a six-step process.

• Journal of Nutrition and Health
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• v.37 no.8
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• pp.633-644
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• 2004

This study was performed to investigate effect of dried powders and ethanol extracts of garlic flesh and peel on antioxidative capacity in 16-month- old rats. Forty Sprague-Dawley male rats weighing 618.1$\pm$6.5g were blocked into five groups according to body weight and raised for 3 months with experimental diets containing 5% (w/w) of dried powders of garlic flesh or peel, or ethanol extracts from equal amount of each dried powder. Total polyphenols, flavonoids, /3 -carotene, vitamin C, vitamin E, and total antioxidant status (TAS) levels were determined in garlic preparations. Thiobarbituric acid reactive substances (TBARS) levels in plasma, liver and VLDL + LDL fraction, oxidative DNA damage (8-hydroxy-2' -deoxyguanosine, 80HdG) in kidney, xanthine oxidase (XO) activities in plasma and liver, superoxide dismutase (SOD) activities in erythrocyte and liver, and carotenoid concentration, and total antioxidant status (TAS) in plasma were measured. Total polyphenols and flavonoids contents in garlic preparations were highest in peel ethanol extract. Vitamin C content was not different significantly among preparations, but peel powder contains slightly more vitamin C. The content of $\beta$-carotene was highest in peel ethanol extract and vitmain E content was highest in flesh ethanol extract. The highest level of TAS was observed in peel ethanol extract. Plasma TBARS levels in all the experimental groups were found to be significantly lower than control group, and TBARS concentration in VLDL + LDL fraction was decreased in all the experimental groups in comparison to control group. Also levels of 80HdG in kidney in experimental groups were lower than that of control group. Plasma and liver XO activities were. decreased in all experimental groups, and erythrocyte and liver SOD activities were higher in experimental groups compared to control group. All experimental groups also showed higher plasma TAS levels than control group. Especially, garlic flesh powder group was significantly lower in plasma and liver XO activities, and significantly higher in erythrocyte and liver SOD activities than control group. Moreover, plasma TBARS level and kidney 8OHdG level were decreased in flesh powder group. In conclusion, garlic diets showed effect of improving antioxidative capacity in 16-month old rats, especially, garlic flesh powder was prominent in inhibiting XO activity, promoting SOD activity and decreasing kidney 8OHdG level among experimental groups.

• Korean Journal of Food Science and Technology
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• v.37 no.2
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• pp.233-240
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• 2005

To discover new functional materials using edible plants, antioxidant activities of methanol extracts from various parts of seven wild vegetables were investigated in vitro. Total polyphenol contents, determined by Folin-Denis method, varied from 16.74 to $130.22{\mu}g/mg$. Radical-scavenging activities of methanol extracts were examined using ${\alpha},\;{\alpha}-diphenyl-{\beta}-pirrylhydrazyl$ (DPPH) radicals and 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) assay. Inhibition effects on peroxidation of linoleic acid determined by ferric thiocyanate (FTC) method and on oxidative degradation of 2-deoxy-D-ribose in Fenton-type reaction system were dose-dependent. Athyrium acutipinulum Kodama (leaf and rood), Achyranthes japonica (Miq.) Nakai (seed), and Solidago virga-aurea var. gigantea Nakai (root) showed relatively high antioxidant activities in various systems.