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Anti-Helicobacter pylori Compounds from Polygonum cuspidatum.

Atif Ali Khan KHALIL ; Woo Sung PARK ; Hye Jin KIM ; Kazi Marjahan AKTER ; Mi Jeong AHN

Natural Product Sciences.2016;22(3):220-224. doi:10.20307/nps.2016.22.3.220

Anti-Helicobacter pylori activity guided fractionation led to the isolation of five anthraquinones, two stilbenes and one naphthoquinone from the EtOAc fraction of Polygonum cuspidatum, using silica gel column chromatography, Sephadex-LH20, MPLC and recrystallization. The chemical structures were identified to be physcion (1), emodin (2), anthraglycoside B (3), trans-resveratrol (4), anthraglycoside A (5), polydatin (6), 2-methoxy-6-acetyl-7-methyljuglone (7) and citreorosein (8) by UV, ¹H-NMR, ¹³C-NMR and mass spectrometry. Anti-Helicobacter pylori activity including MIC values of each compound was evaluated. All of the isolates exhibited anti-H. pylori activity of which MIC values were lower than that of a positive control, quercetin. Compounds 2 and 7 showed potent growth inhibitory activity. Especially, a naphthoquinone, compound 7 displayed most potent antibacterial activity with MIC₅₀ value of 0.30 µM and MIC₉₀ value of 0.39 µM. Although anti-H. pylori activity of this plant was previously reported, this is the first report on that of compounds isolated from this species. From these findings, P. cuspidatum roots or its isolates may be useful for H. pylori infection and further study is needed to elucidate mechanism of action.
Anthraquinones ; Chromatography ; Emodin ; Fallopia japonica* ; Mass Spectrometry ; Plants ; Polygonum* ; Quercetin ; Silica Gel ; Stilbenes

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New Production of Antibacterial Polycyclic Quinazoline Alkaloid, Thielaviazoline, from Anthranilic Acid by the Marine-Mudflat-Derived Fungus Thielavia sp..

Alain Simplice LEUTOU ; Keumja YUN ; Byeng Wha SON

Natural Product Sciences.2016;22(3):216-219. doi:10.20307/nps.2016.22.3.216

The microbial transformation of anthranilic acid (1) by the marine-mudflat-derived fungus Thielavia sp. produced an antibacterial polycyclic quinazoline alkaloid, thielaviazoline (2). The stereostructure of the metabolite was assigned based on detailed spectroscopic data analyses including comparison of the NMR (¹H and ¹³C) data with those of reported compound (2). Compound 2 displayed in vitro antimicrobial activity against methicillin-resistant and multidrug-resistant Staphylococcus aureus (MRSA and MDRSA), with minimum inhibitory concentrations (MICs) of 6.25 and 12.5 µg/mL, respectively. Compound 2 also showed potent radical-scavenging activity against 2,2-diphenyl-1-picrylhydrazyl (DPPH) with an IC₅₀ of 11 µM, which was more active than the positive control, L-ascorbic acid (IC₅₀, 20.0 µM).
Ascorbic Acid ; Fungi* ; In Vitro Techniques ; Methicillin Resistance ; Microbial Sensitivity Tests ; Staphylococcus aureus ; Statistics as Topic

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Induction of Apoptosis with Kigelia africana fruits in HCT116 Human Colon Cancer Cells via MAPKs Signaling Pathway.

Tae Eun GUON ; Ha Sook CHUNG

Natural Product Sciences.2016;22(3):209-215. doi:10.20307/nps.2016.22.3.209

Kigelia africana (Lam.) Benth. (Bignoniaceae) is a flowering plants in South, Central and West Africa and commonly known as the sausage tree (Eng.); worsboom (Afr.); umVunguta, umFongothi (Zulu); Modukguhlu (North Sotho); Muvevha (Venda). The dried, powdered fruits are used as dressing for wounds and ulcers, haemorrhoids, rheumatism, purgative, skin-firming, lactation in breast-feeding mothers. The aim of this study is to investigate the cytotoxic and apoptotic potentials of 70% ethanolic extracts of Kigelia africana fruits in HCT116 human colon cancer cells. Treatment of Kigelia africana fruits with various concentrations resulted in a sequence of characteristic of apoptosis, including loss of cell viability and morphological changes. Flow cytometry analysis showed Kigelia africana fruits increased the sub-G1 phase (apoptosis) population. Apoptosis confirmed by annexin V-fluorescein isothiocyanate and propidium iodide double staining in HCT116 human colon cancer cell lines. Moreover, analysis of the mechanism indicated that Kigelia africana fruits showed an increased Bax and Bcl-2 expressions in a dose-dependent manner, resulting in activation of hallmarks of apoptotic events, caspase-3, caspase-9 and cleaved poly-ADP-ribose polymerase. This is the first report to demonstrate the cytotoxicity of Kigelia africana fruits on HCT116 human colon cancer cells.
Africa, Western ; Apoptosis* ; Bandages ; Caspase 3 ; Caspase 9 ; Cell Line ; Cell Survival ; Colon* ; Colonic Neoplasms* ; Ethanol ; Female ; Flow Cytometry ; Flowers ; Fruit* ; Humans* ; Lactation ; Mothers ; Propidium ; Rheumatic Diseases ; Trees ; Ulcer ; Wounds and Injuries

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Moringa oleifera Prolongs Lifespan via DAF-16/FOXO Transcriptional Factor in Caenorhabditis elegans.

Jun Sang IM ; Ha Na LEE ; Jong Woo OH ; Young Jin YOON ; Jin Suck PARK ; Ji Won PARK ; Jung Hoon KIM ; Yong Sung KIM ; Dong Seok CHA ; Hoon JEON

Natural Product Sciences.2016;22(3):201-208. doi:10.20307/nps.2016.22.3.201

Here in this study, we investigated the lifespan-extending effect and underlying mechanism of methanolic extract of Moringa olelifa leaves (MML) using Caenorhabditis elegans (C. elegans) model system. To define the longevity properties of MML we conducted lifespan assay and MML showed significant increase in lifespan under normal culture condition. In addition, MML elevated stress tolerance of C. elegans to endure against thermal, oxidative and osmotic stress conditions. Our data also revealed that increased activities of antioxidant enzymes and expressions of stress resistance proteins were attributed to MML-mediated enhanced stress resistance. We further investigated the involvement of MML on the aging-related factors such as growth, food intake, fertility, and motility. Interestingly, MML significantly reduced growth and egg-laying, suggesting these factors were closely linked with MML-mediated longevity. We also observed the movement of aged worms to estimate the effects of MML on the health span. Herein, MML efficiently elevated motility of aged worms, indicating MML may affect health span as well as lifespan. Our genetic analysis using knockout mutants showed that lifespan-extension activity of MML was interconnected with several genes such as skn-1, sir-2.1, daf-2, age-1 and daf-16. Based on these results, we could conclude that MML prolongs the lifespan of worms via activation of SKN-1 and SIR-2.1 and inhibition of insulin/IGF pathway, followed by DAF-16 activation.
Caenorhabditis elegans* ; Caenorhabditis* ; Eating ; Fertility ; Longevity ; Methanol ; Moringa oleifera* ; Moringa* ; Osmotic Pressure

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Bioassay-Guided Isolation and Identification of Compounds from Arecae Pericarpium with Anti-inflammatory, Anti-oxidative, and Melanogenesis Inhibition Activities.

Amelia INDRIANA ; Kyoung Jin LEE ; Yeong Shik KIM

Natural Product Sciences.2016;22(3):193-200. doi:10.20307/nps.2016.22.3.193

This study describes the anti-inflammatory, anti-oxidant, and melanogenesis inhibition activities of methanol extract and various organic solvent fractions of Arecae Pericarpium. We examined the inhibition of lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW 264.7 cells, 1,1-diphenyl-2-picrylhydrazine (DPPH) scavenging activity, mushroom tyrosinase inhibition activity and melanin contents. The study showed that, among all tested fractions, methylene chloride fraction showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells (IC₅₀ value 8.89 µg/mL) and DPPH radical scavenging activity (EC₅₀ value 21.39 µg/mL). Methylene chloride and ethyl acetate fractions similarly inhibited mushroom tyrosinase activity. Methanol extract exhibited strongest reduction of melanin content in B16F10 melanoma cells. Based on the bioactivity assay results, methylene chloride and ethyl acetate fractions were further separated. Eight phenolic compounds were isolated, which are dimeric syringol (1), catechol (2), 4-hydroxybenzaldehyde (3), vanillin (4), 4-hydroxyacetophenone (5), apocynin (6), protocatechuic acid (7) and 4-hydroxybenzoic acid (8). Among the isolated compounds tested, catechol showed the strongest inhibition of LPS-induced NO production in RAW 264.7 cells. Catechol also showed the concentration-dependent NF-κB inhibition activity. Arecae Pericarpium might have potentials to be developed as anti-inflammatory agent or dermatological product for skin-whitening agent.
Agaricales ; Areca* ; Melanins ; Melanoma ; Methanol ; Methylene Chloride ; Monophenol Monooxygenase ; Nitric Oxide ; Phenol ; RAW 264.7 Cells

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Effects of Gypenosides on Dopaminergic Neuronal Cell Death in 6-Hydroxydopamine-lesioned Rat Model of Parkinson's Disease with Long-term L-DOPA Treatment.

Keon Sung SHIN ; Ting Ting ZHAO ; Hyun Jin PARK ; Kyung Sook KIM ; Hyun Sook CHOI ; Myung Koo LEE

Natural Product Sciences.2016;22(3):187-192. doi:10.20307/nps.2016.22.3.187

The goal of this study was to determine whether gypenosides (GPS) exert protective effects against dopaminergic neuronal cell death in a 6-hydroxydopamine (OHDA)-lesioned rat model of Parkinson's disease (PD) with or without long-term 3,4-dihydroxyphenylalanine (L-DOPA) treatment. Rats were injected with 6-OHDA in the substantia nigra to induce PD-like symptoms; 14 days after injection, groups of 6-OHDA-lesioned animals were treated for 21 days with GPS (25 or 50 mg/kg) and/or L-DOPA (20 mg/kg). Dopaminergic neuronal cell death was assessed by counting tyrosine hydroxylase (TH)-immunopositive cells in the substantia nigra and measuring levels of dopamine, norepinephrine, 3,4-dihydroxyphenylacetic acid (DOPAC), and homovanillic acid (HVA) in the striatum. Dopaminergic neuronal cell death induced by 6-OHDA lesions was ameliorated by GPS treatment (50 mg/kg). L-DOPA treatment exacerbated 6-OHDA-induced dopaminergic neuronal cell death; however, these effects were partially reversed by GPS treatment (25 and 50 mg/kg). These results suggest that GPS treatment is protective against dopaminergic neuronal cell death in a 6-OHDA-lesioned rat model of PD with long-term L-DOPA treatment. Therefore, GPS may be useful as a phytotherapeutic agent for the treatment of PD.
3,4-Dihydroxyphenylacetic Acid ; Animals ; Cell Death* ; Dihydroxyphenylalanine ; Dopamine ; Dopaminergic Neurons* ; Homovanillic Acid ; Levodopa* ; Models, Animal* ; Norepinephrine ; Oxidopamine ; Parkinson Disease* ; Rats* ; Substantia Nigra ; Tyrosine 3-Monooxygenase

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Two-Week Repeated Dose Toxicity of Atractylodis Rhizoma Alba in F344 Rats.

Hyoung Yun HAN ; Young Su YANG ; Soo Nam KIM ; Su Cheol HAN ; Jong Hwa LEE ; Ja Young JEONG ; Hang sik ROH ; Ji Hyeon SEOK ; Joo Sang LEE ; Jeong Ah KIM ; Byung Sun MIN

Natural Product Sciences.2016;22(3):180-186. doi:10.20307/nps.2016.22.3.180

This research is to estimate the toxicity of Atractylodis Rhizoma Alba (ARA) in F344 rats and to find a dose level for the 13 weeks toxicity study. A hot water extract of ARA (ARWE) was administered orally to F344 rats at dose levels of 0 (vehicle control), 500, 1000, 2000, 3500, and 5000 mg/kg/day for 2 weeks. Each group was composed to five male and five female F344 rats. According to the result, there were no ARWE-related adverse changes in mortality, body weights, food consumption, urinalysis, hematology, clinical chemistry, gross finding at necropsy, and organ weight examination. Salivation was observed in 3500 and 5000 mg/kg/day in male and female rats but it could not have found any relationship with ARWE administration. Based on our findings, ARWE may not cause toxicity in rats under the experimental conditions. Therefore, dose level of 5000 mg/kg/day as a highest treatment group in 13-week exposure study is recommended for further toxicity assessment.
Animals ; Body Weight ; Chemistry, Clinical ; Female ; Hematology ; Humans ; Male ; Mortality ; Organ Size ; Rats ; Rats, Inbred F344* ; Salivation ; Toxicity Tests ; Urinalysis ; Water

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Beneficial Effect of Lespedeza cuneata (G. Don) Water Extract on Streptozotocin-induced Type 1 Diabetes and Cytokine-induced Beta-cell Damage.

Min Suk KIM ; Bhesh Raj SHARMA ; Dong Young RHYU

Natural Product Sciences.2016;22(3):175-179. doi:10.20307/nps.2016.22.3.175

The aim of this study was to evaluate the anti-diabetic effects of the water extract of Lespedeza cuneata (LCW) using rat insulinoma (RIN) m5F cells and streptozotocin (STZ)-induced diabetic rats. The effect of LCW on the protection of pancreatic beta cells was assessed using MTT assay, and nitric oxide production was assessed using Griess reagent. STZ-induced diabetic rats were treated with 100 and 400 mg/kg body weight of LCW for 5 weeks. In results, LCW significantly protected cytokine-induced toxicity and NO production, and increased insulin secretion in RINm5F cells. LCW significantly decreased serum blood glucose, thiobarbituric acid reactive substances (TBARS), blood urea nitrogen (BUN) and advanced glycation end products (AGEs) levels, and renal fibronectin expression in STZ-induced diabetic rats. Also, LCW effectively improved BW loss in STZ-induced diabetic rats. Thus, our results suggest that LCW has a beneficial effect on cytokine-induced pancreatic beta cell damage and biomarkers of diabetic complication in hyperglycemic rats.
Animals ; Biomarkers ; Blood Glucose ; Blood Urea Nitrogen ; Body Weight ; Cytokines ; Diabetes Complications ; Fibronectins ; Glycosylation End Products, Advanced ; Insulin ; Insulin-Secreting Cells ; Insulinoma ; Lespedeza* ; Nitric Oxide ; Rats ; Streptozocin ; Thiobarbituric Acid Reactive Substances ; Water*

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Modulation of Melanin Synthesis by Amaranthus spp. L Seed Extract in Melan-a Cells.

Jae Ok SEO ; Moon Ho DO ; Jae Hak LEE ; Taek Hwan LEE ; Hussain Mustatab WAHEDI ; Yong Un PARK ; Sun Yeou KIM

Natural Product Sciences.2016;22(3):168-174. doi:10.20307/nps.2016.22.3.168

Anti-melanogenic effects of amaranth (AT), one of the key source of squalene, were investigated in melanocytes. Amaranth seed powder was extracted with water and melan-a cells were treated with various concentrations of AT. By using HPLC, content of myo-inositol, one of potential active components, was measured in the crude extract of AT.AT reduced the melanin content in melan-a melanocytes and down-regulated melanogenic enzyme activity such as tyrosinase, TRP-1 and TRP-2. By regulating melanogenic enzyme activity, AT may be a potential natural source for whitening agent. Myo-inositol was detected in AT by HPLC and may be one of the active compounds from AT involved in the regulation of anti-melanogenesis. In this study, we demonstrated that AT has anti-melanogenesis properties. This new function of amaranth may be useful in the development of new skin-whitening products and its value as food.
Amaranthus* ; Chromatography, High Pressure Liquid ; MART-1 Antigen* ; Melanins* ; Melanocytes ; Monophenol Monooxygenase ; Squalene ; Water

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Anti-obesity Effect of Steamed Soybean and Fermented Steamed Soybean in High-fat Diet-induced Obese ICR Mice.

Hye Rin SEO ; Ah Young LEE ; Kye Man CHO ; Eun Ju CHO ; Hyun Young KIM

Natural Product Sciences.2017;23(1):61-68. doi:10.20307/nps.2017.23.1.61

This study was performed to investigate the ameliorating effects of steamed soybeans (SS) and fermented SS (FSS) on lipid metabolism in high-fat diet-induced obese mice. ICR mice were divided into four groups and given the following different diets: normal diet (ND), high-fat diet (HFD), HFD with 1% SS (HFD + SS), and HFD with 1% FSS (HFD + FSS). After 14 weeks, the body weight gain was higher in the HFD group compared with the ND group but lower in the HFD + FSS group compared with the HFD group. Plasma levels of triglyceride (TG), total cholesterol (TC), low density lipoprotein-cholesterol, aspartate aminotransferase (AST), and alanine aminotransferase (ALT) were significantly higher in the HFD group compared to the ND group, but lower in the HFD + SS and HFD + FSS groups compared with the HFD group. In addition, leptin concentration in plasma was lower in the groups fed HFD + SS and HFD + FSS compared with the HFD group. The accumulation of hepatic TG and TC was significantly inhibited in the HFD + SS and HFD + FSS groups. Furthermore, SS and FSS attenuated lipid peroxidation and nitric oxide formation in the liver induced by the high-fat diet. These results suggest that soybeans, especially FSS, may be useful in preventing obesity-induced abnormalities in lipid metabolism.
Alanine Transaminase ; Animals ; Aspartate Aminotransferases ; Body Weight ; Cholesterol ; Diet ; Diet, High-Fat ; Leptin ; Lipid Metabolism ; Lipid Peroxidation ; Liver ; Mice ; Mice, Inbred ICR* ; Mice, Obese ; Nitric Oxide ; Obesity ; Oxidative Stress ; Plasma ; Soybeans* ; Steam* ; Triglycerides

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