• Journal of Life Science
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• v.33 no.4
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• pp.349-356
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• 2023

Gout, a chronic inflammatory arthritic disease, is characterized by hyperuricemia. Gout can be induced by an inflammatory response to monosodium urate (MSU) crystals mediated by pro-inflammatory cytokine release following activation of the NOD-like receptor protein 3 (NLRP3) inflammasome. Many sulfur-containing phytochemical compounds in garlic (Allium sativum L.) are considered active ingredients because of their potential pharmacological benefits for various diseases, but their efficacy in NLRP3 inflammasome activation-mediated gout has not been demonstrated. In this study, we investigated whether diallyl disulfide (DADS) and diallyl trisulfide (DATS), representative garlic-derived sulfur compounds, have an inhibitory effect on MSU-induced NLRP3 inflammasome activation. Our results showed that under non-cytotoxic conditions, DADS and DATS significantly blocked nitric oxide production and interleukin (IL)-1β release in response to MSU in lipopolysaccharide (LPS)-primed RAW 264.7 macrophages. DADS and DATS also attenuated enhanced expression of NLRP3 and its adapter protein, apoptosis-associated speck-like protein, which was associated with downregulation of and caspase-1 p20 and IL-1β expression, suggesting that MSU-induced LRP3 inflammasome activation was counteracted by DADS and DATS. Furthermore, DADS and DATS blocked oxidative stress, an upstream event for NLRP3 inflammasome activation, as evidenced by the fact that they scavenged reactive oxygen species (ROS) production. Taken together, our findings demonstrate that DADS and DATS suppressed NLRP3 inflammasome activation by inhibiting the ROS/NLRP3 pathway and that they have potential as treatments for NLRP3-dependent gouty arthritis.

• 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.

• Korean Journal of Environment and Ecology
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• v.28 no.5
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• pp.574-587
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• 2014

In this study, vertical distribution patterns of Quercus mongolica Fisch. ex Ledeb. and Q. serrata Murray in Korea were recognized and possibility of introgressive hybridization and gene flow between Q. mongolica and Q. serrata in Mt. Jiri was inferred by flavonoid analyses. The most critical factor on distribution patterns was the altitude in accordance with temperature condition. A zonal distribution was recognized: Quercus mongolica zone in the upper area and Q. serrata zone in the lower area. In Central Korea, the range of vertical distribution of Q. mongolica was above alt. 100m, almost everywhere, whereas that of Q. serrata was from alt. 0 m to alt. 500(-700) m, and the species is rare above that altitude. But in Southern Korea, Q. serrata is found up to above alt. 1,000 m, whereas frequency of Q. mongolica reduces as elevation in decline and the species is rare below alt. 300 m, even though pure stands being formed on higher mountain slope. Altitudinal distribution of the two species, however, overlaps, where the two species occur together. Thirty-seven individuals of Q. mongolica and Q. serrata in Mt. Jiri and other area were examined for leaf flavonoid constituents. Twenty-three flavonoid compounds were isolated and identified; they were glycosylated derivatives of the flavonols kaempferol, quercetin, isorhamnetin, myricetin, and four compounds among the flavonoid compounds were acylated. Kaempferol 3-O-glucoside, quercetin 3-O-glucoside, quercetin 3-O-galactoside and its acylated compounds were major constituents and present in all individuals. Quercus mongolica is distinguished from Q. serrata by the presence of quercetin 3-O-arabinosylglucoside and by high concentration of three acylated compounds, acylated kaempferol 3-O-glucoside, quercetin 3-O-glucoside, quercetin 3-O-galactoside, and by relatively low concentration or lacking of rhamnosyl flavonol compounds. There are intraspecific variations in flavonoid profiles for Q. mongolica and Q. serrata, the flavonoid profiles for individuals of two species in hybrid zone (sympatric zone) tend to be similar to each other, qualitatively and quantitatively. These findings strongly suggest that gene exchange or gene flow occurs through the introgressive hybridization between Q. mongolica and Q. serrata in Mt. Jiri. Therefore, Quercus crispula, occupying morphologically intermediate position between Q. mongolica and Q. serrata, is suspected of being a hybrid taxon of two putative parental species.

• Analytical Science and Technology
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• v.30 no.3
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• pp.113-121
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• 2017

Now a day's rise of new antibiotic resistant bacterial strains is a global threat. Ethnic people of India have been employing Aphanamixis polystachya (Wall.) R. Parker wood extract in healing cancerous wounds. The aim of this study was to evaluate the antimicrobial activity and to identify the medicinally potent chemicals in the essential oil extract of A. polystachya. The antibacterial properties of various organic extracts were evaluated against a range of bacteria (gram-positive and gram-negative bacteria) based on the disc diffusion method and GC-MS based analysis for finding active oil extract components. All extracts of A. polystachya leaves showed potential antibacterial activity, notably ethyl acetate, while petroleum ether extracts revealed highly sensitive activity against all tested bacteria (zones of inhibition ranging from 8.83 to 11.23 mm). In addition, the petroleum ether extract had the lowest MIC value (32 to $256{\mu}g/mL$) against E. coli, S. lutea, X. campestris, and B. subtilis bacteria. The major compounds detected in oil [${\beta}$-elemene (16.04 %), ${\beta}$-eudesmol (12.78 %), ${\beta}$-caryophyllene (19.37 %), ${\beta}$-selinene (11.32 %), elemol (5.76 %), and ${\alpha}$-humulene (5.68 %)] are expected to be responsible for the potent antimicrobial activity. The results of this study offer valuable insights into the potent role of A. polystachya essential oil extract in pharmaceutical and antibiotic research.

• Advances in Traditional Medicine
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• v.10 no.1
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• pp.21-28
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• 2010

The objective of the present investigation is to evaluate the antimicrobial potency of the terpenoid fractions isolated from Luffa cylindrica seeds against various pathogenic microbes. The seeds were powdered and extracted with methanol in soxhlet appratus based on phytochemical screening. Three terpenoid components were isolated by column chromatography and identified by thin layer chromatography and chemical analysis which were designated as ${LCSF_4}^*$, ${LCSF_6}^*$ & ${LCSF_8}^*$ respectively. Disc diffusion method was employed to determine the antimicrobial effectiveness of test compounds I, II and III $({LCSF_4}^*,\;{LCSF_6}^*\;&\;{LCSF_8}^*)$ against 6 microbial species viz., Staphylococcus (S.) aureus, Bacillus (B.) subtilis, Escherichia (E.) coli, Pseudomonas (P.) aeruginosa, Candida (C.) albicans and Aspergillus niger. The disc was saturated with $100{\mu}l$ of each compound, allowed to dry and introduced on the upper layer of seeded agar plate. The plates were incubated overnight at $37^{\circ}C$. Microbial growth was determined by measuring the zonal inhibition diameters. Compound I showed maximum potency against gram positive S. aureus (21 mm) in comparison with standard ciprofloxacin (38 mm), whereas the same compound was completely devoid of activity against both the fungi tested. Compound II was found to be highly sensitive against both the gram negative E. coli (20 mm) and P. aeruginosa (22 mm). Compound II was found to exhibit maximum potency against the fungi C. albicans (15 mm) and A. niger (20 mm). Compound III was found to be very effective against both the gram positive S. aureus (20 mm) and B. subtilis (15 mm) respectively.

• Natural Product Sciences
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• v.21 no.2
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• pp.104-110
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• 2015

The activities on the inhibition of NO on LPS-induced RAW 264.7 macrophages were investigated in this work. A simple and sensitive method has been developed and validated for fingerprinting analysis of leaves of Acanthopanax gracilistylus W.W. Smith (AGS). The cytotoxicity and inhibition of NO on LPS-induced RAW 264.7 cells of the extract and triterpenoids were determined. Optimal conditions of HPLC analysis were established as follows. The separation was performed with an ODS-C₁₈ column at $30^{\circ}C$, the detected wavelength was 210 nm, the flow rate was 1 mL/min, and the mobile phase consisted of acetonitrile (0.05% phosphoric acid)-0.05% phosphoric acid solution with gradient elution. Our results showed that impressic acid and acankoreaogenin was more effective on the inhibition of NO than the methanol extract and other compounds. There were seventeen peaks coexisted with similarities above 0.95 and nine lupane-triterpenoids including acankoreaogenin and impressic acid detected and identified. The result of anti-inflammatory activities provides a potential explanation for the use of AGS leaves as a herbal medicine in the treatment of inflammatory diseases. Our results also show that acankoreanogenin and impressic acid may be potentially useful in developing new anti-inflammatory agents. In addition, the fingerprint chromatography clearly illustrated and confirmed the material basis for the anti-inflammatory activities of this plant.

• Korean Journal of Pharmacognosy
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• v.39 no.4
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• pp.357-364
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• 2008

The roots of Saposhnikovia divaricata Schischk. (Umbelliferae) have been known to possess analgesic, anti-inflammatory, anti-parasitic and anti-bacterial activities, and used for curing headaches, fever and arthralgia. In this study, we aimed to isolate active constituents to provide phytochemical data for the quality control of this plant. Nine coumarins, eight chromones, three sterols and a coumarolignan were isolated from EtOAc-soluble fraction of the roots of S. divaricata through repetive column chromatography method using silica gel, ODS gel, Sephadex-LH 20, MPLC and HPLC. By analyses of spectroscopic data and comparison of their data with those of published values, the compounds were identified as 3'-O-angeloylhamaudol (1), ${\beta}$-sitosterol (2), marmesin (3), phellopterin (4), anomalin (5), imperatorin (6), xanthotoxin (7), deltoin (8), bergapten (9), stigmasterol (10), ledebouriellol (11), hamaudol (12), 8'-epicleomiscosin A (13), xanthoarnol (14), cimifugin (15), 5-O-methylvisamminol (16), daucosterol (17), 4'-O-${\beta}$-D-glucosyl-5-O-methylvisamminol (18), nodakenin (19), sec-O-glucosylhamaudol (20), prim-O-glucosylcimifugin (21). Among them, 8'-epicleomiscosin (13) was firstly reported from Umbelliferae family and xanthoarnol (14) and nodakenin (19) were isolated from this plant for the first time.

• Journal of Microbiology and Biotechnology
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• v.30 no.2
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• pp.163-171
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• 2020

Brugmansia arborea L. (Solanaceae), commonly known as "angel's trumpet," is widely grown in North America, Africa, Australia, and Asia. It has been mainly used for ornamental purposes as well as analgesic, anti-rheumatic, vulnerary, decongestant, and anti-spasmodic materials. B. arborea is also reported to show anti-cholinergic activity, for which many alkaloids were reported to be principally responsible. However, to the best of our knowledge, a phytochemical study of B. arborea flowers has not yet been performed. Four flavonol glycosides (1-4) and one dihydroflavanol (5) were for the first time isolated from B. arborea flowers in this study. The flavonoids showed significant antioxidant capacities, suppressed nitric oxide production in lipopolysaccharide (LPS)-treated RAW 264.7 cells, and reduced inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX-2) protein production increased by LPS treatment. The contents of compounds 1-4 in n-BuOH fraction were determined to be 3.8 ± 0.9%, 2.2 ± 0.5%, 20.3 ± 1.1%, and 2.3 ± 0.4%, respectively, and that of compound 5 in EtOAc fraction was determined to be 12.7 ± 0.7%, by HPLC experiment. These results suggest that flavonol glycosides (1-4) and dihydroflavanol (5) can serve as index components of B. arborea flowers in standardizing anti-inflammatory materials.

• Journal of Applied Biological Chemistry
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• v.56 no.4
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• pp.213-217
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• 2013

Phytochemical studies on the leaves of Ailanthus altissima (Simaroubaceae) have not been reported previously. Thus, the authors isolated and identified secondary metabolites from A. altissima. Dried and powdered leaves were extracted with 80% aqueous methanol, and the concentrated extract was successively partitioned with ethyl acetate, n-butanol, and water. Four flavonoids were isolated from the ethyl acetate fraction through repeated silica gel and octadecyl silica gel column chromatography. Spectroscopic data including NMR, MS, and IR allowed for identification of the chemical structures as quercetin (1), afzelin (2), quercitrin (3), and isoquercitrin (4). This is the first report of the isolation of these compounds from A. altissima. The four isolated flavonoids 1-4 as well as solvent fractions (ethyl acetate, n-butanol, and water), were evaluated for DPPH radical scavenging activity.

• Preventive Nutrition and Food Science
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• v.14 no.3
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• pp.188-194
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• 2009

In this study, we evaluated the phytochemical compositions of the fruits of the pear cactus, mulberry, and Korean black raspberry to determine how they related to antioxidant capacity. Specifically, the total soluble polyphenol, flavonoid and anthocyanin contents were determined, and the phenolic compounds were evaluated by HPLC. In addition, the antioxidant capacity was evaluated by electron paramagnetic resonance (EPR), SOD-like activity and nitrate scavenging activity. Korean black raspberry was found to have the highest level of phytochemicals, followed by mulberry and pear cactus (p<0.05). Furthermore, EPR revealed that Korean black raspberry extract (100 ${\mu}g$/mL) removed 78.6% of the superoxide radicals in a xanthin-xanthin oxidase. Additionally, when the removal of hydroxyl radicals was evaluated, the extract of pear cactus showed 50% scavenging activity at 1000 ${\mu}g$/mL. Korean black raspberry extract showed the highest SOD-like activity, which was 44% (p<0.05). Finally, the nitrate scavenging activity of both extracts of mulberry and Korean black raspberry were found to be 93%, while that of the pear cactus was 63% at pH 1.2 (p<0.05).