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

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.45 no.1
• /
• pp.44-51
• /
• 2016

The aim of the study was to investigate the antioxidant content and activities of ethanol extract of the edible flower Dianthus chinensis L. (DCE) as well as its inhibitory activities against nitric oxide (NO) production in macrophages and growth and adhesion of human cancer cells. The total polyphenol, flavonoid, and carotenoid levels of DCE were 19.0 mg gallic acid equivalent/g, 65.7 mg quercetin equivalent/g, and $95.0{\mu}g/g$, respectively. The 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity and ferric reducing antioxidant power of DCE at a concentration of $1,000{\mu}g/mL$ were 44% and 51%, respectively. In lipopolysaccharide-treated RAW 264.7 macrophages, treatment with DCE at concentrations of 500 and $1,000{\mu}g/mL$ resulted in significantly reduced NO levels (to 7~23% of the control). In H1299 human lung carcinoma cells and HCT116 human colorectal carcinoma cells, treatment with DCE at concentrations of 250, 500, and $1,000{\mu}g/mL$ resulted in dose-dependent growth inhibition. DCE was also effective in inhibiting adhesion of both H1299 cells (to 55% of the control at concentration of $1,000{\mu}g/mL$) and HCT116 (to 26~40% of the control at concentrations of 250, 500, and $1,000{\mu}g/mL$). These results suggest that DCE exerts antioxidant, anti-inflammatory, and anti-cancer activities in vitro.

• Journal of Life Science
• /
• v.26 no.1
• /
• pp.109-116
• /
• 2016

Ulmi cortex is the elm bark or root bark of Ulmus macrocarpa Hance and has been used as an ingredient of traditional medicine for anti-inflammatory, analgesic, anti-cancer and wound healing on both the East and the West. This study investigated whether the Ulmus macrocarpa Hance Water extract (UMWE) has the in vivo and in vitro immune activating effect. Animals were orally administrated for 14 days as follows: no treat group with distilled water, cyclophosphamide (CY) group with 120 mg/kg of CY, UMWE 100+CY group with 100 mg/kg of UMWE and 120 mg/kg of CY, UMWE 200+CY group with 200 mg/kg of UMWE and 120 mg/kg of CY, UMWE 100 group with 100 mg/kg of UMWE and UMWE 200 group with 200 mg/kg of UMWE. The immunosuppressive drug CY was intraperitoneally injected to induce immune suppression. Spleen indices showed small changes in CY injected groups but splenocyte indices showed greater decrease in the same groups. However, UMWE appeared to relieve CY’s immunosuppression. UMWE also delayed in vitro splenocyte death increasing its longevity. These data obtained by MTT assay and 7-amino-actinomycin D which stains preferentially dead than live cells. UMWE alone did not show cytotoxicity based on its apoptototic effect on splenocytes in vitro and in vivo. Splenic NK cell activity was maintained by UMWE under the presence of CY in vitro. The data indicated that UMWE protects splenocytes from the immunosuppressive drug CY under in vitro and in vivo conditions.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.29 no.2 s.43
• /
• pp.205-232
• /
• 2003

Ursolic acid (UA) and Oleanolic acid (ONA), known as urson, micromerol and malol, are pentacyclic triterpenoid compounds which naturally occur in a large number of vegetarian foods, medicinal herbs, and plants. They may occur in their free acid form or as aglycones for triterpenoid saponins, which are comprised of a triterpenoid aglycone, linked to one or more sugar moieties. Therefore UA and ONA are similar in pharmacological activity. Lately scientific research, which led to the identification of UA and ONA, revealed that several pharmacological effects, such as antitumor, hepato-protective, anti-inflammatory, anticarcinogenic, antimicrobial, and anti-hyperlipidemic could be attributed to UA and ONA. Here, we introduced the effect of UA and ONA on acutely barrier disrupted and normal hairless mouse skin. To evaluate the effects of UA and ONA on epidermal permeability barrier recovery, both flanks of 8-12 week-old hairless mice were topically treated with either 0.01-0.1 mg/ml UA or 0.1-1 mg/ml ONA after tape stripping, and TEWL (Transepidermal water loss) was measured . The recovery rate increased in those UA or ONA treated groups (0.1 mg/ml UA and 0.5 mg/ml ONA) at 6 h more than $20\%$ compared to vehicle treated group (p<0.05). Here, we introduced the effects of UA and ONA on acute barrier disruption and normal epidermal permeability barrier function. For verifying the effects of UA and ONA on normal epidermal barrier, hydration and TEWL were measured for 1 and 3 weeks after UA and ONA applications (2mg/ml per day). We also investigated the features of epidermis and dermis using electron microscopy (EM) and light microscopy (LM). Both samples increased hydration compared to vehicle group from f week without TEWL alteration (p<0.005). EM examination using RuO4 and OsO4 fixation revealed that secretion and numbers of lamellar bodies and complete formation of lipid bilayers were most prominent $(ONA{\geq}UA>Vehicle)$. LM finding showed that thickness of stratum corneum (SC) was slightly increased and especially epidermal thickening and flattening was observed (UA>ONA>Veh). We also observed that UA and ONA stimulate epidermal keratinocyte differentiation via $PPAR\;\alpha$. Protein expression of involucrin, loricrin, and filaggrin increased at least 2 and 3 fold in HaCaT cells treated with either $ONA\;(10{\mu}M)$ or UA $(10{\mu}M)$ for 24h respectively. This result suggested that the UA and ONA can improve epidermal permeability barrier function and induce the epidermal keratinocyte differentiation via $PPAR\;{\alpha}$. Using Masson-trichrome and elastic fiber staining, we observed collagen thickening and elastic fiber elongation by UA and ONA treatments. In vitro results of collagen and elastin synthesis and elastase inhibitory activity measurements were also confirmed in vivo findings. These data suggested that the effects of UA and ONA related to not only epidermal permeability barrier functions but also dermal collagen and elastic fiber synthesis. Taken together, UA and ONA can be relevant candidates to improve epidermal and dermal functions and pertinent agents for cosmeseutical applications.

• Journal of Physiology & Pathology in Korean Medicine
• /
• v.26 no.6
• /
• pp.908-914
• /
• 2012

To investigate the difference and change of ingredient and efficacy of Galgeun-tang (GGT) according to extraction solvent, water and 70% EtOH, the quantities of index components and the several in vitro activities of two kinds of GGT extract were compared. The contents of extracts were analyzed with HPLC. The biological activities such as anti-inflammatory and anti-obesity effects were measured through cell line-based in vitro assay. The cytotoxicity was measured by CCK-8 assay in RAW 264.7 cell, BEAS-2B cell, HaCaT cell and 3T3-L1 cell. We compared effects of two kinds of extract by measuring NO, PGE2, IL-6 and TNF-${\alpha}$ in RAW264.7 cell, RANTES in BEAS-2B cell, MDC and RANTES in HaCaT cell and GPDH activity and leptin level in differentiated 3T3-L1. 70% EtOH extract of GGT contained more compositions than water extract. The inhibitory effect of water extract of GGT on NO in RAW 264.7 cell and GPDH activity in 3T3-L1 was stronger than that of 70% EtOH. 70% EtOH has a stronger inhibitory effect on PGE2 in RAW264.7 cell, RANTES in BEAS-2B cell, MDC, RANTES in HaCaT cell, leptin in 3T3-L1 cell than water extraction. These results suggest that the ingredient and efficacy from 70% EtOH extract of GGT are more effective than water extract.

• Journal of the Korean Applied Science and Technology
• /
• v.35 no.1
• /
• pp.235-246
• /
• 2018

Paeony has pharmacological activities such as anti-inflammatory, anti-allergic, anti-bacterial, central inhibitory, gastric secretion inhibition, and antispasmodic activities. In addition, its antioxidant activity and whitening effect being reported, thus it is being explored as raw materials for cosmetics. We compared the changes in the contents of paeoniflorin and paeonol in Peony extracts, depending on the changes of extracting solvents, temperature and time. The HPLC method was set up for simultaneous analysis, the system suitabilities were confirmed by using the calibration curves and the QC samples for each assay batch. Paeonol was detected only in roots, and paeoniflorin was higher in leaf and flower than root. Higher concentrations of both ingredients were extracted when the root was used after grinding to a suitable size, and when 30% 1,3-butylene glycol was used as the extraction solvent. Also the concentrations tended to increase at higher temperature and longer time, but the increase was gradual at over $75^{\circ}C$ and 4 hours. The ratio of root, leaf and flower was determined to be 2+2+1g/0.5kg of batch, reaching the contents criteria of paeoniflorin and paeonol. Finally, we selected as the best extraction condition when the raw materials are mixed with 2+2+1g/0.5kg and extracted with 30% 1,3-butylene glycol as an extraction solvent at $75^{\circ}C$ for 4 hours, considering both the concentrations of two components and the cost of raw materials and manufacturing process, The extraction units were scaled up to 10 kg under this condition.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.42 no.7
• /
• pp.1015-1021
• /
• 2013

Glycyrrhiza inflata Batal, an important species of licorice, is one of the most widely used medicinal plants for over 4000 years. Glycyrrhiza plant species has been well known for its various therapeutic activities such as anti-inflammatory, anti-allergic, and anti-ulcer. The purpose of this study was to determine the effects of Glycyrrhiza inflata Batal ethanol extracts (GBE) on adipocyte and osteoblast differentiation. Mesenchymal C3H10T1/2 cells were treated with sub-cytotoxic doses of GBE, and its effects on adipocyte differentiation were assessed. We found that GBE dose-dependently increased lipid accumulation and also induced the expression of adipocyte markers, such as $PPAR{\gamma}$ and its target genes, aP2, and adiponectin, in C3H10T1/2 cells. Consistently, similar effects of GBE on lipid accumulation were also observed in preadipocyte 3T3-L1 cells that further supports the pro-adipogenic activities of GBE. We also investigated the effects of GBE on osteoblast differentiation of mesenchymal C3H10T1/2 cells. As a results, we found that GBE increased the activity of alkaline phosphatase in a dose-dependent manner and also promoted the expression of osteoblast markers, such as ALP and RUNX2, during osteoblast differentiation of C3H10T1/2 cells. Similar pro-osteogenic effects of GBE were also observed in preosteoblast MC3T3-E1 cells. Finally, our data show that a major bioactive compound found in Glycyrrhiza inflata Batal, licochalcone A (LA) but not glycyrrhizic acid (GA), can mediate the pro-adipogenic and pro-osteogenic effects of GBE. Taken together, this study provides data to show the possibility of GBE and its bioactive component LA as putative strategies for type 2 diabetes and bone diseases.

• Journal of the Korean Society of Food Science and Nutrition
• /
• v.43 no.2
• /
• pp.224-230
• /
• 2014

Marine algae have long been recognized as a health and beauty food, based on its anti-tumor, anti-inflammatory and anti-obesity activities. In this study, methanol extracts were prepared from 10 different phaeophyta, after which DPPH radical scavenging and cytoprotective activities of HT-22 cells against ${\beta}$-amyloid protein ($A{\beta}$), which has neurotoxic effects, were investigated. In DPPH experiments, Ecklonia cava and Ishige okamurai showed strong ROS scavenging activities, whereas eight other phaeophyta including Petalonia binghamiae (P. bin) showed weak ROS scavenging activities. To validate the cytoprotective effects of 10 different phaeophyta in $A{\beta}$-induced HT-22 cells, protein expression levels of APP, BACE1, iNOS, phosphorylated ERK1/2, phosphorylated p38 and phosphorylated JNK1/2 were determined along with MTT assay. In the MTT assay, P. bin showed the best effective cytoprotective activity at a concentrations of $25{\mu}g/mL$, whereas Sargassum confusum, Colpomenia sinuosa, Myelophycus simplex, and Sargassum hemiphyllum showed potential. Determination of protein expression levels related to $A{\beta}$-induced neurotoxicity in the five selected phaeophyta showed that P. bin inhibited BACE1 and iNOS expression in $A{\beta}$-induced HT-22 cells. These results indicate that the cytoprotective effects of P. bin are mediated by suppressing the pathways involving $A{\beta}$-induced ERK and p38 activation.

• Journal of the Society of Cosmetic Scientists of Korea
• /
• v.30 no.2
• /
• pp.211-219
• /
• 2004

Yew (Taxus cuspidata Sieb.) chose that grow as medicine, food, decorative plant in Korea's Kyong-Gi province surroundings. Extracts of yew extracted leaf of 250g and stems of 300g with 1,3-butylene glycol (l,3-BG), propylene glycol (PG) and water. As results, external appearance of leaf extract of yew was slightly brown clear extract. The pH was 5.3${\pm}$0.5, and specific gravity was 1.012${\pm}$0.05, and refractive index was l.375${\pm}$0.05. Also, appearance of stem's extract was slightly brown clear extract, and the pH was 5.4${\pm}$0.5, and specific gravity was 1.016${\pm}$0.05, and refractive index was 1.358${\pm}$0.05. Oil of yew separated from seeds, and extracted polysaccharide high purity from fruits. As a result, specific gravity of oil was 0.987, and obtained 40.0% of yield. Total polyphenols amount of yew extract is detected 0.563% in leaves, 0.325% in stems, whereas total tannins amount contained 0.054% and 0.037% each in leaves and stems. As effect in cosmetics, the anti-oxidative effect by DPPH method is 75.0% in leaves, and stems was 64.0%. Collagen synthesis rate was shown high activity by 54.16% in stem's extract, 33.18% in leaves' extract. Also, PPE-inhibitory activities were 13.7% and 23.5% each in leaves and stems. Anti-inflammatory effect of yew seed oil displayed superior effect of 41% than control. Polysaccharide's molecular weight that is gotten from fruits was 5${\times}$10$^4$-3${\times}$10$\^$5/ dalton, and got 20.0${\pm}$5% of yield.

• Journal of Life Science
• /
• v.19 no.11
• /
• pp.1629-1636
• /
• 2009

Pine trees (Pinus densiflora Sieb. et Zacc.) have been used as a traditional health-promoting medicinal food in Korea. This research was performed to determine the antioxidative and antibacterial activities, tyrosinase, nitric oxide synthesis, angiotensin converting enzyme (ACE), and xanthine oxidase inhibition effects of the pine bud ethanol extract (PBE). Antioxidative activities of PBE were measured by using 2,2-diphenyl-1-picryl-hydrazyl (DPPH) free radical scavenging activity and superoxide dismutase-like activity (SODA). DPPH radical scavenging and SOD-like activities of PBE were remarkably increased in a dose-dependent manner, and were about 88.9% and 47.9% at 1 mg/ml and 10 mg/ml, respectively. The xanthine oxidase and angiotensin converting enzyme activities were inhibited about 71.9% and 60.8% at 1 mg/ml and $100{\mu}g/ml$ of PBE, respectively. The tyrosinase inhibitory activities of PBE were slightly increased in a dose-dependent manner. The PBE showed strong antimicrobial activities on Escherichia coli (E. coli) and Vibrio paraheamolyticus. Stimulation of the macrophages RAW264.7 cells with lipopolysaccharide (LPS) resulted in increased production of nitric oxide (NO) in the medium. However, NO synthesis was reduced up to 54% by addition of PBE at $200{\mu}g/ml$. These results revealed that pine buds have a strong antioxidative and anti-inflammatory activity, and exhibit angiotensin converting enzyme and xanthine oxidase inhibitory activities. This suggests that pine buds have the greatest property as a source for natural health products.