• Preventive Nutrition and Food Science
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• v.20 no.3
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• pp.153-161
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• 2015

Matrix metalloproteinases (MMPs) are crucial extracellular matrices degrading enzymes that have important roles in metastasis of cancer progression as well as other significant conditions such as oxidative stress and hepatic fibrosis. Marine plants are on the rise for their potential to provide natural products that exhibit remarkable health benefits. In this context, brown algae species have been of much interest in the pharmaceutical field with reported instances of isolation of bioactive compounds against tumor growth and MMP activity. In this study, eight different brown algae species were harvested, and their extracts were compared in regard to their anti-MMP effects. According to gelatin zymography results, Ecklonia cava, Ecklonia bicyclis, and Ishige okamurae showed higher inhibitory effects than the other samples on MMP-2 and -9 activity at the concentrations of 10, 50, and $100{\mu}g/mL$. However, only I. okamurae was able to regulate the MMP activity through the expression of MMP and tissue inhibitor of MMP observed by mRNA levels. Overall, brown algae species showed to be good sources for anti-MMP agents, while I. okamurae needs to be further studied for its potential to yield pharmaceutical molecules that can regulate MMP-activity through cellular pathways as well as enzymatic inhibition.

• Preventive Nutrition and Food Science
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• v.17 no.2
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• pp.122-128
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• 2012

Gelidium (G.) elegans is a red alga inhabiting intertidal areas of North East Asia. We examined anti-oxidative and anti-inflammatory effects of G. elegans, depending on drying and extraction conditions, by determining reactive oxygen species (ROS) and nitric oxide (NO) in 3T3-L1 and RAW 264.7 cells. Extraction yields of samples using hot air drying (HD) and far-infrared ray drying (FID) were significantly higher than those using natural air drying (ND). The 70% ethanol extracts showed the highest total phenol and flavonoid contents compared to other extracts (0, 30, and 50% ethanol) under tested drying conditions. The scavenging activity on 2,2-diphenyl- 1-picrylhydrazyl (DPPH) and nitrite correlated with total phenol or flavonoid content in the extracts. The greatest DPPH scavenging effect was observed in 70% ethanol extract from FID and HD conditions. The production of ROS and NO in 3T3-L1 and macrophage cells greatly decreased with the 70% ethanol extraction derived from FID. This study suggests that 70% ethanol extraction of G. elegans dried by FID is the most optimal condition to obtain efficiently antioxidant compounds of G. elegans.

• ALGAE
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• v.29 no.1
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• pp.47-55
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• 2014

To develop effective and safe acne vulgaris therapies with a continuing demand for new solutions, we investigated unique efficacy of an antibacterial agent from marine brown alga Eisenia bicyclis in treating acne vulgaris. The methanolic extract of E. bicyclis exhibited potential antibacterial activity against acne-related bacteria. The ethyl acetate fraction showed the strongest antibacterial activity against the bacteria among solvent fractions. Six compounds (1-6), previously isolated from the ethyl acetate fraction of E. bicyclis, were evaluated for antibacterial activity against acne-related bacteria. Among them, compound 2 (fucofuroeckol-A [FF]) exhibited the highest antibacterial activity against acne-related bacteria with a minimum inhibitory concentration (MIC) ranging from 32 to $128{\mu}g\;mL^{-1}$. Furthermore, FF clearly reversed the high-level erythromycin and lincomycin resistance of Propionibacterium acnes. The MIC values of erythromycin against P. acnes were dramatically reduced from 2,048 to $1.0{\mu}g\;mL^{-1}$ in combination with MIC of FF ($64{\mu}g\;mL^{-1}$). The fractional inhibitory concentration indices of erythromycin and lincomycin were measured from 0.500 to 0.751 in combination with 32 or $64{\mu}g\;mL^{-1}$ of FF against all tested P. acnes strains, suggesting that FF-erythromycin and FF-lincomycin combinations exert a weak synergistic effect against P. acnes. The results of this study suggest that the compounds derived from E. bicyclis can be a potential source of natural antibacterial agents and a pharmaceutical component against acnerelated bacteria.

• Journal of Applied Biological Chemistry
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• v.51 no.6
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• pp.296-301
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• 2008

The extracts from Salvia officinalis were studied for antioxidative activities and inhibitory activities against angiotensin converting enzyme(ACE) and xanthine oxidase (XOase). Total phenolic compounds were found as 22.28, 26.3, 24.63, and 28.22 mg/g in the water, 60% ethanol, 60% methanol and 60% acetone extracts, respectively. The antioxidant activities of Salvia officinalis extracts were measured as $64.4{\pm}1.5%$ at $200\;{\mu}g/ml$ on EDA, inhibition rate on ABTS of $96.9{\pm}0.2%$, antioxidant protection factor of $2.30{\pm}0.16$ PF and TBARS was $0.6{\pm}0.05$ (${\times}100\;{\mu}M$) in the control and $0.28{\pm}0.02$ (${\times}100\;{\mu}M$) in 60% ethanol extracts. Inhibitory activities was the ACE of 75.50% and XOase 100% in 60% ethanol extracts. The 60% ethanol extracts from Salvia officinalis exhibited antimicrobial activities against Helicobacter pylori such as 13 mm of clear zone and inhibition rate of 63.4% with $200\;{\mu}g/ml$ of phenolics content. Rosemarinic acid was the most abundant phenolic compounds as analyzed by HPLC. The results suggest that the 60% ethanol extracts from Salvia officinalis L. will be useful as natural antioxidants and functional foods.

• Journal of Life Science
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• v.31 no.11
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• pp.980-986
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• 2021

Natural products have always been an attractive source in terms of novel anti-metastatic compounds which can hinder MMP expression and activity. Corydalis heterocarpa is a salt marsh plant found in the seashores throughout Korea. Its yellow flowers and spikes have been an ingredient in folk medicine to treat spasm and contractions. The present study assessed the potential of different solvent-based fractions from the crude extract of Corydalis heterocarpa (CHE), a halophyte with reported bioactivities, to suppress the PMA-induced MMP expression in human fibrosarcoma HT-1080 cells. The solvent fractions which were named after the solvent used for fractionation (n-hexane, 85% aqueous (aq.) methanol (MeOH), n-butanol (BuOH), and H₂O were shown to inhibit the both elevated mRNA and protein expression levels of MMP-2 and MMP-9 and simultaneously relieved the suppression on the expression of the endogenous MMP inhibitors TIMP-1 and TIMP-2. Results indicated that the CHE fractions might intervene with the PMA-induced activation of the MAPK signaling which is the upstream activator of MMP overexpression. Among tested samples, 85% aq. MeOH and n-hexane fractions of CHE was determined to be the most active and future studies to isolate the bioactive substances responsible for the regulation of the MMP expression are, therefore, urged. In conclusion, C. heterocarpa was shown to be a potential source of anti-metastatic compounds and n-Hexane and MeOH fractions might yield lead molecules to develop novel MMP inhibitors.

• Journal of Life Science
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• v.32 no.1
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• pp.51-55
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• 2022

Matrix metalloproteinase (MMP) enzymes are responsible for the degradation and formation of the extracellular matrix (ECM), and overproduction of MMPs is observed in several diseases, such as cancer and asthma, that progress with metastatic characteristics. Natural products, especially phytochemicals, have been an important source of MMP inhibitors with reduced side effects. Although the majority of phytochemicals inhibit the enzymatic activity of MMPs, some suppress MMP production. In this context, the current study evaluated the potential of Corydalis heterocarpa, a halophyte with reported bioactivities, to inhibit MMP expression in PMA-stimulated HT-1080 cells. A crude C. heterocarpa extract was shown to decrease the mRNA and protein expression of MMP-2 and MMP-9 while increasing the endogenous MMP inhibitors TIMP-1 and TIMP-2 which regulate MMP expression in healthy tissues. In addition, our results show that the inhibitory effects of C. heterocarpa might occur through suppression of the phosphorylation of MAPK signaling, the upstream activator of MMP overexpression. In conclusion, C. heterocarpa is a potential source of antimetastatic compounds that might serve as lead molecules to develop novel MMP inhibitors.

• Journal of Life Science
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• v.28 no.9
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• pp.999-1006
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• 2018

Obesity is epidemic worldwide and has reportedly been linked to the progression of several metabolic and cardiovascular diseases. The natural products are decreasing the side effects of medicines used for obesity and also have health benefits dut to their numerous bioactive compounds. In this context, Artemisia scoparia is a widespread plant that has been suggested as possessing various types of bioactivity. In this study, the crude extract from A. scoparia (ASE) was tested for its ability to suppress adipogenesis in mouse 3T3-L1 pre-adipocytes. The molecular pathway by which ASE affects differentiation of 3T3-L1 cells was also investigated. The introduction of ASE to differentiating 3T3-L1 pre-adipocytes resulted in suppressed adipogenesis, as confirmed by decreased intracellular lipid accumulation. The differentiating cells treated with 10 and $100{\mu}g/ml$ of ASE showed 21.9 and 29.0% less lipid accumulation, respectively, than untreated adipocytes. In addition, the results indicated that ASE treatment lowered the expression of the adipogenesis-related factors $PPAR{\gamma}$, $C/EBP{\alpha}$, and SREBP-1c. Furthermore, treating with ASE notably decreased levels of phosphorylated p38, ERK, and JNK in 3T3-L1 adipocytes. These results indicate that ASE exhibits significant anti-adipogenesis activity by downregulating the MAPK and $PPAR{\gamma}$ pathways during the differentiation of 3T3-L1 pre-adipocytes. Therefore, A. scoparia may be a potential source of natural products against obesity.

• Journal of Life Science
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• v.24 no.5
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• pp.491-497
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• 2014

Nowadays, starfish is one of problems about interruption of marine ecosystem, so many researchers are focusing on application of the starfish (Asterias amurensis). In this study, we investigated the contractile and relaxant activity of the smooth muscles and the antimicrobial and antioxidant activity of six different tissues (muscle, gut, liver, tube feet, gonads, and body) of A. amurensis. Frozen samples were extracted with distilled water containing 1% acetic acid. Extracts from all the tissues, except the body tissue, showed potent antimicrobial activity against Escherichia coli D31. The dorsal retractor muscles (DRM) of muscle and gut extracts showed strong contraction responses. On the other hand, contractile activity on esophagus of squid Todarodes pacificus could be detected in all tissues tested. The contractile activity of the liver extract was higher than that of the other tissues. The body, tube feet, and liver extracts showed the contractile activity on the intestine of the panther puffer fish (Takifugu pardalis). Relaxation response on the DRM of starfish (A. pectinifera) was observed in all tissues tested. Increased antioxidant activity was observed in the gut, liver, and body extracts. The results suggest that the starfish (A. amurensis) is a potential source of novel bioactive compounds.

• Journal of Life Science
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• v.17 no.10
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• pp.1447-1451
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• 2007

Through the screening of marine natural compounds that inhibit cancer cell proliferation, we previously reported that pectenotoxin-2 (PTX-2) isolated from marine sponges exhibits selective cytotoxicity against several cell lines in p53-deficient tumor cells compared to those with functional p53. However, the molecular mechanisms of its anti-proliferative action on malignant cell growth are not completely known. To further explore the mechanisms of its anti-cancer activity and to test whether the status of p53 in liver cancer cells correlates with their chemo-sensitivities to PTX-2, we used two well-known hepatocarcinoma cell lines, p53-deficient Hep3B and p53-wild type HepG2. We have demonstrated that PTX-2 markedly inhibits Hep3B cell growth and induces apoptosis whereas HepG2 cells are much more resistant to PTX-2 suggesting that PTX-2 seems to act by p53-independent cytotoxic mechanism. The apoptosis induced by PTX-2 in Hep3B cells was associated with the modulation of DNA fragmentation factor (DFF) family proteins, up-regulation of pro-apoptotic Bcl-2 family members such as Bax and Bcl-xS and activation of caspases (caspase-3, -8 and -9). Blockade of the caspase-3 activity by caspase-3 inhibitor, z-DEVD-fmk, prevented the PTX-2-induced growth inhibition in Hep3B cells. Moreover, treatment with PTX-2 also induced phosphorylation of AKT and extracellular-signal regulating kinase (ERK), but not c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase (MARK). Specific inhibitors of PI3K inhibitor (LY294002) and ERK1/2 inhibitor (PD98059) significantly blocks PTX-2-induced-anti-proliferative effects, whereas a JNK inhibitor (SP600125) and a p38 MAPK inhibitor (SB203580) have no significant effects demonstrating that the pro-apoptotic effect of PTX-2 mediated through activation of AKT and ERK signal pathway in Hep3B cells.

• Journal of Microbiology and Biotechnology
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• v.30 no.4
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• pp.571-582
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• 2020

Quorum sensing (QS)-mediated infections cause severe diseases in human beings. The control of infectious diseases by inhibiting QS using antipathogenic drugs is a promising approach as antibiotics are proving inefficient in treating these diseases. Marine fungal (Pestalotiopsis sydowiana PPR) extract was found to possess effective antipathogenic characteristics. The minimum inhibitory concentration (MIC) of the fungal extract against test pathogen Pseudomonas aeruginosa PAO1 was 1,000 ㎍/ml. Sub-MIC concentrations (250 and 500 ㎍/ml) of fungal extract reduced QS-regulated virulence phenotypes such as the production of pyocyanin, chitinase, protease, elastase, and staphylolytic activity in P. aeruginosa PAO1 by 84.15%, 73.15%, 67.37%, 62.37%, and 33.65%, respectively. Moreover, it also reduced the production of exopolysaccharides (74.99%), rhamnolipids (68.01%), and alginate (54.98%), and inhibited the biofilm formation of the bacteria by 90.54%. In silico analysis revealed that the metabolite of P. sydowiana PPR binds to the bacterial QS receptor proteins (LasR and RhlR) similar to their respective natural signaling molecules. Cyclo(-Leu-Pro) (CLP) and 4-Hydroxyphenylacetamide (4-HPA) were identified as potent bioactive compounds among the metabolites of P. sydowiana PPR using in silico approaches. The MIC values of CLP and 4-HPA against P. aeruginosa PAO1 were determined as 250 and 125 ㎍/ml, respectively. All the antivirulence assays were conducted at sub-MIC concentrations of CLP (125 ㎍/ml) and 4-HPA (62.5 ㎍/ml), which resulted in marked reduction in all the investigated virulence factors. This was further supported by gene expression studies. The findings suggest that the metabolites of P. sydowiana PPR can be employed as promising QS inhibitors that target pathogenic bacteria.