The leave of Polygonum tinctorium (LPT) have been used for centuries as a traditional medicine and as a food ingredient and natural dye. The aim of the current study was to develop high-value added products using LPT. Hot water extract (HWE) and ethanol extract (EE) of LPT were prepared, respectively, and their bioactivity was evaluated. The extraction ratio for the HWE was 27.6%, which was two-fold higher than that of the EE. The contents of total polyphenol in the HWE and total sugar in the EE were 51.2 mg/g and 297.8 mg/g, respectively. The total flavonoid and reducing sugar contents were similar in the extracts, irrespective of the extraction solvent. The HWE did not show antimicrobial activity in a disc-diffusion assay, but the EE showed strong growth inhibition against gram-positive bacteria. The EE exhibited stronger DPPH and ABTS radical scavenging activities and reducing power than those of the HWE. The HWE was particularly effective as a scavenger of nitrite ($RC_{50}$ of $6.0{\mu}g/ml$). In an antithrombosis activity assay, the EE showed significant anticoagulation activity as determined by an extended blood coagulation time (thrombin time, prothrombin time, and activated partial thromboplastin time), in addition to platelet aggregation activity. The HWE also showed platelet aggregation inhibitory activity. This report provides the first evidence of antithrombosis activities of LPT. Our results suggest that LPT has potential as a new antioxidant and antithrombosis agent.
Purpose: Glabridin (GD) is a bio-available isoflavane isolated from the root extract of licorice (Glycyrrhiza glabra L.). It exhibits a variety of pharmacological activities such as anti-inflammatory and anti-oxidant activities. However, extracellular vesicles (EVs) secretion and the anti-cancer mechanism of action remains largely unknown. The present study investigates the anticancer effects of GD by determining the inhibition of EVs secretion in the human breast cancer cell line, MDA-MB-231. Methods: Cell viability, reactive oxygen species (ROS) production, migration, invasion rate, and vascular endothelial growth factor (VEGF) concentration were assessed in MDA-MB-231 cells treated with increasing concentrations of GD (0.1, 1, 5, 10, 20 µM). Subsequently, EV secretion and exosomal DEL-1 protein expression were evaluated to determine the anticancer effects of GD. Results: The results showed that GD significantly inhibited the cell proliferation of MDA-MB-231 cells in a dose- or time-dependent manner. Also, ROS production and apoptosis marker protein cleaved caspase-3 were significantly increased in GD-treated MDA-MB-231, compared to control. Furthermore, GD exposure resulted in significantly decreased not only migration and invasion rates but also the VEGF concentration, thereby contributing to a reduction in angiogenesis. Interestingly, the concentration and number of EVs as well as EV marker proteins, such as CD63 and TSG101, were decreased in GD-treated MDA-MB-231 cells. Markedly, extracellular matrix protein DEL-1 as angiogenesis factor was decreased in EVs from GD-treated MDA-MB-231 cells. Conclusion: This study identifies that the anti-cancer molecular mechanism of GD is exerted via inhibition of angiogenesis and EVs secretion, indicating the potential of GD as a chemotherapeutic agent for breast cancer.
Kim, Soo Hyun;Lee, AhReum;Kim, SuJi;Kim, Kyeong Jo;Kwon, Ojun;Choi, Joon Young;Koo, Jin Suk;Roh, Seong-Soo
The Korea Journal of Herbology
/
v.32
no.4
/
pp.17-24
/
2017
Objectives : Advanced glycation end products (AGEs) is bind formation of glucose and protein. Acceleration of AGE formation during hyperglycemia is associated with the pathogenesis of diabetic complications and causes kidney and skin damage. The aim of this study was investigated the AGEs inhibitory activity and antioxidant activity of water extracts from young persimmon (YP) and heated young persimmon (HYP). Methods : Paeoniae Radix Alba (YP) is prepared by heating with 30% ethanol. AGEs formation inhibitory activities of YP and HYP measured using bovine serum albumin. To evaluate the protective effects of YP and HYP in diabetic rats induced with streptozotocin (STZ) and methyl glyoxal (MGO), SD rats were distributed into four groups; normal mice (Nor), AGEs-induced rats (Con), AGEs-induced rats treated with 100 mg/kg YP (YP), AGEs-induced rats treated with 100 mg/kg heated YP (HYP) for 3weeks. Heated young persimmon respectively decrease AGEs construction. Results : YP and HYP administration inhibited the biomarkers of AGEs in serum, kidney and skin tissues. AGE-induced rats revealed that the significant decreased collagen however, heat processing methods of young persimmon up regulated inhibits AGEs-induced collagen decrease. The expressions of AGEs were decreased in YP and HYP treated group compared with the control group in tissues. It specifies that HYP has potential to serve as a positive regulator of via AGEs path way. Conclusion : It has proposed that may have an improvement effect on diabetic complications, heated young persimmon has AGEs inhibitory excellent activities and antioxidant effect.
Journal of the Korean Applied Science and Technology
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v.38
no.6
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pp.1543-1552
/
2021
Atractylodes japonica has been widely used in a traditional Korean herbal medicine exerting various pharmacological activities such as diauretic action, asriction, anti-allergy, neuroprotective activity, anti-cancer, immunomodulation and gastrointestinal protective effect. This study was to investigate the antioxidant, nitric oxide and inflammatory cytokines production of A. japonica extract by water and 70% ethanol. DPPH and ABTS free radical scavenging activity were increased in a dose-dependent manners with both extracts and there was no difference with extract solvents. 70% ethanol extract of A. japonica showed a very strong inhibitory effect on NO production. Both extracts of A. japonica significantly reduce the expression of iNOS and COX-2 proteins involved in NO prodction. A. japonica extract by water and 70% ethanol inhibited LPS-induced proinflammatory cytokines such as IL-6 and IL-1b. In this study, 70% ethanol extract of A. japonica significantly suppresses LPS-induced NO and inflammatory cytokine production. Therefore it can be widely used to treat and improve inflammatory diseases.
Ji, Choi;Hae-Jin, Park;Il-ha, Jeong;Min Ju, Kim;Mi-Rae, Shin;Seong-Soo, Roh;Soon-Ae, Park;Mi-Lim, Kim
The Korea Journal of Herbology
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v.38
no.2
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pp.17-26
/
2023
Objectives : A persistent inflammatory response can cause diseases such as fibrosis, cancer, and allergies. This study aimed to investigate the anti-inflammatory activity of Curcumae longae Rhizoma and Cinnamomi Ramulus Mixture (CCM) in lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Methods : The total polyphenol and flavonoid contents of CCM were confirmed through an in vitro experiment. Also, radical scavenging activities of 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), and Hydroxyl were confirmed. Moreover, ferric reducing antioxidant power (FRAP) activity were confirmed. After, CCM (50, 100, and 200 ㎍/mL) were applied to 0.1 ㎍/mL LPS-stimulated RAW264.7 cells. The levels of nitric oxide (NO) and pro-inflammatory cytokines in the supernatant fraction were determined. Also, the expressions of mitogen-activated protein kinase (MAPK) and nuclear factor-κB (NF-κB) pathways were detected using Western blot. Results : As a result of in vitro experiments, there was an excellent antioxidant activity in CCM-treated cells. In addition, in RAW264.7 cells stimulated with LPS, the increased NO level was inhibited in a concentration-dependent manner by the treatment of CCM. In addition, inflammatory cytokines production were significantly inhibited in a concentration-dependent manner in CCM-treated group. CCM treatment significantly decreased the protein expressions of MAPKs. Moreover, the expressions of NF-κBp65 and cyclooxygenase-2 (COX-2) were significantly decreased when 200 mg/kg of CCM was applied, and phospho-inhibitor of nuclear factor kappa B-α (p-IκBα) and inducible nitric oxide synthase (iNOS) were significantly decreased at all concentrations treated with CCM. Conclusion : Our findings show that CCM exhibited excellent antioxidant activity and exhibited superior anti-inflammatory effect through the MAPKs and NF-κB pathways in LPS-stimulated RAW 264.7 macrophages.
Journal of the Korean Applied Science and Technology
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v.40
no.5
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pp.988-1000
/
2023
Hesperetin(HT) is a potent antioxidant flavonoid aglycone derived from hesperidin(HD). The antioxidant, anti-inflammatory, and antimicrobial activities of HT and its cyclodextrin(CD) inclusion complexes were compared in vitro. HT was prepared by enzymatic hydrolysis of HD, and HT/CD complexes were prepared using 𝛽-cyclodextrin(𝛽-CD) and hydroxypropyl-𝛽-cyclodextrin(HP-𝛽-CD) by solvent co-evaporation method. The solubility of the HT/HP-𝛽-CD inclusion complex increased 93.5-fold compared to HT, and the solubility of HT/𝛽-CD increased 22.5-fold. The HT/HP-𝛽-CD inclusion complex showed a similar effect as HT on radical scavenging activity in antioxidant assays, whereas the HT/𝛽-CD inclusion complex showed slightly lower activity than HT. Cytotoxicity was low in the following order; HT/HP-𝛽-CD, HT/𝛽-CD, and HT in murine macrophage RAW264.7 cells. Treatment with HT and HT/CD inclusion complexes reduced the levels of inflammatory mediators such as nitric oxide(NO), tumor necrosis factor-𝛼(TNF-𝛼) and interleukin-6(IL-6) in the cells. HT and HT/HP-𝛽-CD inclusion complex were more effective than HT/𝛽-CD inclusion complex at relatively low concentrations. Inhibitory effects were tested on skin-pathogenic bacteria, Staphylococcus aureus and Pseudomonas aeruginosa, and they showed an antimicrobial effect on S. aureus in the order of HT = HT/HP-𝛽-CD > HT/𝛽-CD, but they did not show any significant inhibitory effect on P. aeruginosa. In conclusion, HT, the aglycone form of HD, and its CD inclusion complexes showed various biological activities. HT/HP-𝛽-CD inclusion complex, which is the highly soluble form of HT, showed relatively higher activity compared to HT/𝛽-CD inclusion complex.
This study is to isolate bio-active compounds from Alnus firma and evaluate their antioxidant activity. Dried wood powder of A. firma was extracted by organic solvents and fractionated in the sequential extraction steps. The isolated compounds were characterized by EI-MS, $^{13}C-$ and $^1H-NMR$ including COSY, DEFT, HMQC, and HMBC. Antioxidant activities of the isolated compounds were evaluated by DPPH (1,1-diphenyl-2-picrylhydrazyl) free radical scavenging effect. From the wood of A. firma, three kinds of diarylheptanoids, alnusodiol (1), alnusonol (2) and alnusone (3), and gallic acid (4) were isolated. Among these four compounds, compound 1, 2, and 3 are isolated from A. firma for the first time. The antioxidant activity of gallic acid was 93.5% at the concentration of 100 ppm. This compound showed stronger antioxidant activity than those of other isolated compounds and the reference BHT (butylated hydroxytoluene).
Aspergillus niger has been used as a host to express many heterologous proteins. It has been known that the presence of an- abundant protease is a limiting factor to express a heterologous protein. The protease deficient mutant of A. niger was obtained using UV-irradiation. A total of $1{\times}10^5$ spores were irradiated with $10{\sim}20%$ survival dose of UV, 600 $J/m^2$ at 280 nm, and the resulting spores were screened on the casein-gelatin plates. Ten putative protease deficient mutants showing the reduced halo area around colonies were further analyzed to differentiate the protease deficient mutant from other mutant types. Among ten putative mutants, seven mutants showed significant growth defect on nutrient rich medium and two mutants appeared to be the secretory mutants, which resulted in the impaired secretion of extracellular proteins including proteases. A mutant $pro^--20$ showed reduced halo zone without any notable changes in growth rate. In addition, the starchdegrading and glucose oxidase activities in the culture filtrate of $pro^--20$ mutant showed the similar range as that of the parental strain, which suggested that the $pro^--20$ mutant ought to be the protease deficient mutant rather than a secretory mutant. The reduced proteolytic activity of the $pro^--20$ was demonstrated using SDS-fibrin zymography gel. The reduced extracellular proteolysis was quantified by casein degradation assay and, comparing with the parental strain, less than 30% residual extracellular protease activity was detected in the culture filtrate of the $pro^--20$ mutant. The bio-activity of an exogenously supplemented hGM-CSF(human Granulocyte-Macrophage Colony Stimulating Factor) in the culture filtrate of $pro^--20$ mutant was detected until eight times more diluted preparations than that of the parental strain.
Ryu, Chang Seon;Oh, Soo Jin;Oh, Jung Min;Lee, Ji-Yoon;Lee, Sang Yoon;Chae, Jung-woo;Kwon, Kwang-il;Kim, Sang Kyum
Toxicological Research
/
v.32
no.3
/
pp.207-213
/
2016
Although propolis is one of the most popular functional foods for human health, there have been no comprehensive studies of herb-drug interactions through cytochrome P450 (CYP) inhibition. The purpose of this study was to determine the inhibitory effects of propolis on the activities of CYP1A2, 2A6, 2B6, 2C9, 2C19, 2D6, 2E1 and 3A4 using pooled human liver microsomes (HLMs). Propolis inhibited CYP1A2, CYP2E1 and CYP2C19 with an $IC_{50}$ value of 6.9, 16.8, and $43.1{\mu}g/mL$, respectively, whereas CYP2A6, 2B6, 2C9, 2D6, and 3A4 were unaffected. Based on half-maximal inhibitory concentration shifts between microsomes incubated with and without nicotinamide adenine dinucleotide phosphate, propolis-induced CYP1A2, CYP2C19, and CYP2E1 inhibition was metabolism-independent. To evaluate the interaction potential between propolis and therapeutic drugs, the effects of propolis on metabolism of duloxetine, a serotonin-norepinephrine reuptake inhibitor, were determined in HLMs. CYP1A2 and CYP2D6 are involved in hydroxylation of duloxetine to 4-hydroxy duloxetine, the major metabolite, which was decreased following propolis addition in HLMs. These results raise the possibility of interactions between propolis and therapeutic drugs metabolized by CYP1A2.
Park, Yong-Soo;Jeon, Min-Hee;Hwang, Hyun-Jung;Park, Mi-Ra;Lee, Sang-Hyeon;Kim, Sung-Gu;Kim, Mi-Hyang
Nutrition Research and Practice
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v.5
no.4
/
pp.281-287
/
2011
In this study, we evaluated the antioxidant activity of pine needle extracts prepared with hot water, ethanol, hexane, hot water-hexane (HWH), and hot water-ethanol (HWE), using the DPPH (1,1-diphenyl-2-picrylhydrazyl) radical method. The hot water extract possessed superior antioxidant activity than the other extracts. We also compared the antioxidant activity of pine needle extracts through ROS inhibition activity in a cellular system using MC3T3 E-1 cells. The hot water extract exhibited the lowest ROS production. The pattern of HPLC analysis of each extract indicated that the hot water extract contained the highest proanthocyanidin level. The pine needle hot-water extract was then isolated and fractionated with Sephadex LH-20 column chromatography to determine the major contributor to its antioxidant activity. The No.7 and 12 fractions had high antioxidant activities, that is, the highest contents of proanthocyanidins and catechins, respectively. These results indicate that the antioxidant activity of procyanidins from the hot water extract of pine needles is positively related to not only polymeric proanthocyanidins but also to monomeric catechins. Moreover, the antioxidant activity of the pine needle hot water extract was similar to well-known antioxidants, such as vitamin C. This suggests that pine needle proanthocyanidins and catechins might be of interest for use as alternative antioxidants.
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