• Asian Pacific Journal of Cancer Prevention
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• v.16 no.16
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• pp.7155-7159
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• 2015

Background: Oral cancer is a health problem in Thailand. Cratoxylum formosum subsp. pruniflorum Gogel (Teawdang), normally consumed in northeast Thailand, has proven cytotoxic to cervical cancer cell lines including HeLa, SiHa and C-33A. Recently, Asian oral cancer cell lines, ORL-48 and ORL-136, were established. Therefore, we aimed to study cytotoxicity of Teawdang in these. Total phenolic (TPC) and flavonoid content (TFC), and antioxidant activity of Teawdang were also determined. Materials and Methods: Teawdang was purchased from Khon Kaen market during June-October 2013. Hexane (CHE), ethyl acetate (CEE) and methanol (CME) extracts of its edible part were analyzed for TPC by the folin-ciocalteau method and for TFC by an aluminium colorimetric method. Antioxidant activity and cytotoxicity in normal Vero cells and oral cancer cells were investigated. Cell viability was assessed using 3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide (MTT) assays. Results: CME and CEE had higher TPC and TFC and antioxidant activity than CHE. Both CME and CEE, at $200{\mu}g$ dry wt/mL, were cytotoxic to the studied oral cancer cell lines. However, CME was cytotoxic to Vero cells whereas CEE was not. Compared to Vero cells, CEE significantly inhibited ORL-48 and ORL-136 growth (p=0.03 and p=0.02, respectively). Conclusions: CEE exhibited cytotoxic effects on the studied oral cancer cell lines but not normal Vero cells. The bioactive compounds in CEE should be further purified and elucidated for their mechanisms of action for development as anticancer agents.

• Korean Journal of Medicinal Crop Science
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• v.12 no.4
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• pp.289-294
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• 2004

Reactive oxygen species (ROS) are continuously produced at a high rate as a by-product of aerobic metabolism. Several lines of evidence provided that ROS appears to cause to develop aging and various diseases. High level of hyaluronic acid with decreased molecular weight has been detected in patients with inflammatory diseases including rheumatoid arthritis. In this study, we have conducted to investigate the antioxidant and hyaluronidase inhibitory activities of Prunus persica Batsch var. davidiana Maximowicz in order to screen the bioactive substances which can be developed as possible anti-inflammatory agents. Among the extracts of Prunus persica Batsch var. davidiana Maximowicz, EtOAc extract exhibited the strongest effect on antioxidant experiment such as DPPH, Ferric- Thiocyanate and Rancimat. Also, EtOAc extract showed a potent hyaluronidase inhibitory activity.

• Korean Journal of Pharmacognosy
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• v.34 no.1 s.132
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• pp.109-117
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• 2003

Arachidonic acid(AA), which is stored in membrane glycerophospholipids, is liberated by phospholipase $A_2(PLA_2)$ enzymes and is sequentially converted to cyclooxygenase (COX) and lipoxygenase (LOX) then to various bioactive prostaglandins (PGs,) and leukotrienes (LTs). In order to find the specific inhibitors of AA metabolism enzymes such as $PLA_2$, COX-2, 5-LO and lyso PAF acetyltransferase. 195 Korean indigenous plant extracts were evaluated for their inhibitory activity on $PGD_2,\;LTC_4$ production from cytokine-induced mouse bone marrow-derived mast cells (BMMC) and arachidonic acid released from phospholipid and PAF production from lyso PAF. From this screening procedure, methanol extract of eight plants such as Saururus chinensis, Aster tataricus, Chrysanthemum cinerariaefolium, Reynoutria japonica, Disocorea nipponica, Epimedium koreanum, impatiens textori, Veronica rotunda var. subintegra were found to inhibit production of inflammatory mediators in vitro assay system.

• CELLMED
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• v.5 no.1
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• pp.6.1-6.10
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• 2015

Fumaria indica Linn. (Syn: Fumaria parviflora, Fumariaceae) is a wildly grown weed, mentioned and recommended in classical Ayurvedic texts for treatments of variety of ailments including dermatological diseases, topical diseases, cardiovascular complaints, circulatory disease, fever and headache etc. The present pilot study was designed to experimentally verify the possibility that fumarates are the major bioactive principles of Fumaria indica extracts involved in their stress response modulating activities, and to estimate pharmacologicallyactive dose ranges of fumarates and standardized methanolic extract of Fumaria indica (MFI). Effect of single, 5 and 10 daily oral doses of pure fumaric acid (FA), monomethyl fumarate (MMF), dimethyl fumarate (DMF) and MFI was quantified in well validated rodent models viz. apomorphine induced cage climbing, stress induced hyperthermia, and elevated plus-maze tests. Obtained results reveal high efficacy of MFI and pure fumarates possess qualitatively analogous activity profiles in all the three tests. There were no significant difference in the potencies of pure FA, MMF and DMF in the three tests, whereas efficacy of MFI in the elevated plus maze test for anxiolytics was higher than in the other two tests. Efficacies of all the four test agents in all the three tests increased with increasing number of days of oral treatments. Results of these pilot experiments should be helpful for more rational selections of pharmacologically interesting dose ranges and treatment regimens of fumarates and Fumaria indica extracts for further more holistic explorations of their diverse therapeutic potentials.

• Journal of Microbiology and Biotechnology
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• v.30 no.4
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• pp.561-570
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• 2020

This study was designed to synthesize triglycerol monolaurate (TGML) with Lipozyme 435 as the catalyst, and explore its effects on the growth of Aspergillus parasiticus (A. parasiticus) and Aspergillus flavus (A. flavus) and the secretion of aflatoxin b1. The highest content of TGML (49.76%) was obtained at a molar ratio of triglycerol to lauric acid of 1.08, a reaction temperature of 84.93℃, a reaction time of 6 h and an enzyme dosage of 1.32%. After purification by molecular distillation combined with the washes with ethyl acetate and water, the purity of TGML reached 98.3%. Through characterization by electrospray-ionization mass spectrometry, infrared spectrum and nuclear magnetic resonance, the structure of TGML was identified as a linear triglycerol combined with lauroyl at the end. Finally, the inhibitory effects of TGML on the growths of A. parasiticus and A. flavus and the secretion of aflatoxin b1 were evaluated by measuring the colony diameter, the inhibition rate of mycelial growth and the content of mycotoxin in the media. The results indicated that TGML had a stronger inhibitory effects on colony growth and mycelial development of both toxic molds compared to sodium benzoate and potassium sorbate, and the secretions of toxins from A. parasiticus and A. flavus were completely suppressed when adding TGML at 10 and 5 mM, respectively. Based on the above results, TGML may be used as a substitute for traditional antifungal agents in the food industry.

• Korean Journal of Medicinal Crop Science
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• v.20 no.4
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• pp.222-230
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• 2012

We evaluated the inhibitory effects of extracts and components of Geranium thunbergii on aldose reductase (AR) and galactitol formation in rat lenses with high levels of galactose as a part of our ongoing search of natural sources for therapeutic and preventive agents for diabetic complications. The inhibitory effects of water, methanol and ethanol extracts of G. thunbergii on rat lens AR (RLAR) were determined. Comparing inhibitory effects of various solvent extracts, ethanol extract showed RLAR inhibitory activity ($IC_{50}$ values, 5.24 and $6.39{\mu}g/m{\ell}$, respectively). The ethanol extract was fractionated to chloroform, ethyl acetate and water. Of these, the ethyl acetate fraction from ethanol extract of G. thunbergii exhibited RLAR inhibitory activity ($IC_{50}$ value, $2.64{\mu}g/m{\ell}$). In order to identify the bioactive components of ethyl acetate soluble fraction of ethanol extract from G. thunbergii, eight compounds, namely gallic acid (1), protocatechuic acid (2), p-hydroxybenzoic acid (3), brevifolin carboxylic acid (4), geraniin (5), ellagic acid (6), kaempferol-3-O-arabinofuranosyl-7-O-rhamnopyranoside (7), kaempferitrin (8) were isolated. The isolates were subjected to in vitro bioassays to evaluate their inhibitory activity on RLAR and galactitol formation in rat lenses. The ellagic tannins (5, 6) and flavonoid (7) exhibited strong inhibitory effects on RLAR. Also, these three compounds (5, 6 and 7) suppressed galactitol accumulation in rat lens under high galactose conditions, demonstrating the potential to prevent galactitol accumulation exo vivo. These results suggest that the extracts and components of G. thunbergii are a promising agent in the prevention or treatment of diabetic complications.

• The Korea Journal of Herbology
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• v.31 no.3
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• pp.49-57
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• 2016

Objectives： Polygonati Rhizoma (PR) has containing the bioactive compounds such as poly sccharide A,B,C, oligosaccharide, amino acid, it has reported to anti-diabetes and hypertension, atherosclerosis. In this study, we were evaluates antioxidant and anti-physical fatigue effects of PR and steamed PR.Methods : The sample was divided into 5 groups-PR0 (PR without steaming process), PR1 (PR with once steaming process), PR3 (PR with third steaming process), PR6 (PR with sixth steaming process), PR9 (PR with ninth steaming process). We measured anti-oxidant activity through contents of polyphenol, flavonoid and DPPH, ABTS free radical scavenging capacity. And, anti-physical fatigue effect was evaluated using the swimming test, and the AMPK protein expressions in soleus muscle.Results ： As a result, polyphenol, flavonoid, DPPH, ABTS free radical scavenging capacity of PR were increased as steaming times. Anti-physical fatigue effects by swimming test, PR0 have significantly increased, but steamed PR groups were decreased. The AMPK protein expressions of PR0 and PR1 groups were increased comparing with PR3, PR6 and PR9. All groups had effects on decreasing TG, creatine in blood serum, but had no effects on TC in blood serum.Conclusions ： In conclusion, PR with 9 steaming process was more excellent than not-processed PR in anti-oxidant effect such as DPPH, ABTS radical scavenging activity and contents of polyphenol, flavonoid, but, not-processed PR increased swimming times than processed PR. These results suggest that processed PR has anti-oxidant effect as steaming times, and not-processed PR may be a novel potential anti-physical fatigue agents than processed PR.

• Journal of the Korean Society of Food Science and Nutrition
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• v.46 no.1
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• pp.83-91
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• 2017

This study made jelly by adding Sansuyu (Corni Fructus) puree and examined the types and contents of gelling agents as well as the physicochemical characteristics of jelly depending on heating time. Water content of Sansuyu puree was 89.39%, pH was 2.92, sugar content was $10.28^{\circ}Brix$, and total polyphenol content was 1,791.71 mg GAE/100 g. As the added amount of Sansuyu puree increased, pH decreased slightly from 3.04 to 2.97, and yield stress decreased greatly. As heating time increased, red color was unstable and changed to yellow. When heated more than 5 min, jelly was not formed. The level of preference for jelly consisting of 10% Sansuyu puree, 1.5% agar, and 1.0% carrageenan was the highest at 5.15. Using pulp of Sansuyu, it will be possible to make jelly consisting of various bioactive substances.

• Food Science of Animal Resources
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• v.35 no.3
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• pp.293-298
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• 2015

Porcine placenta extract (PPE) is known to possess anti-inflammatory properties owing to its high concentration of bioactive substances. However, the need to eliminate blood-borne infectious agents while maintaining biological efficacy raises concerns about the optimal method for sterilizing PPE. Therefore, the objective of this study was to compare the effects of the standard pressurized heat (autoclaving) method of sterilization with γ-irradiation on the anti-inflammatory effects of PPE. The anti-inflammatory actions of these two preparations of PPE were evaluated by measuring their inhibitory effects on the production of NO, the expression of iNOS protein, and the expression of iNOS, COX2, TNF-α, IL-1β, and IL-6 mRNA in lipopolysaccharide-stimulated RAW 264.7 cells. Compared with autoclaved PPE, γ-irradiated PPE showed significantly greater inhibition of NO production and iNOS protein expression, and produced a greater reduction in the expression of iNOS, COX2, TNF-α, IL-1β, and IL-6 mRNA. These results provide evidence that the sterilization process is crucial in determining the biological activity of PPE, especially its anti-inflammatory activity. Collectively, our data suggest that γ-irradiated PPE acts at the transcriptional level to effectively and potently suppresses the production of NO and the expression of pro-inflammatory cytokines.

• Asian Pacific Journal of Cancer Prevention
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• v.17 no.4
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• pp.2291-2295
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• 2016

Small molecule tyrosine kinase inhibitors targeting HER 2 receptors have emerged as an important therapeutic approach in inhibition of downstream proliferation and survival signals for the treatment of breast cancers. Recent drug discovery efforts have demonstrated that naturally occurring polyphenolic compounds like delphinidin have potential to inhibit proliferation and promote apoptosis of breast cancer cells by targeting HER2 receptors. While delphinidin may thus reduce tumour size, it is associated with serious side effects like dysphonia. Owing to the narrow therapeutic window of delphinidin, the present study aimed to identify high affinity compounds targeting HER2 with safer pharmacological profiles than delphinidin through virtual screening approaches. Delphinidin served as the query parent for identification of structurally similar compounds by Tanimoto-based similarity searching with a threshold of 95% against the PubChem database. The compounds retrieved were further subjected to Lipinski and Verber's filters to obtain drug like agents, then further filtered by diversity based screens with a cut off of 0.6. The compound with Pubchem ID: 91596862 was identified to have higher affinity than its parent. In addition it also proved to be non-toxic with a better ADMET profile and higher kinase activity. The compound identified in the study can be put to further in vitro drug testing to complement the present study.