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‘Goha’, ‘Gangha’, ‘Gwanha’, and ‘Yeolha’ are newly-developed Korean everbearing strawberry (Fragaria ananassa Duch.) cultivars. Bioactive phytochemicals play a crucial role in the prevention of cancer, cardiovascular, neurodegenerative, and metabolic diseases. We examined the free radical scavenging activity and α-glucosidase inhibitory activity in these four cultivars and a junebearing cultivar ‘Seolhyang’ for comparison. ‘Gwanha’ showed the strongest 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) free radical scavenging activities, and ‘Gwanha’ and ‘Goha’ had the most potent α-glucosidase inhibitory activity. Total anthocyanin content (TAC) was the highest in ‘Gwanha’. The major anthocyanin components of everbearing strawberry were determined to be pelargonidin-3-O-glucoside (Pg3G), pelargonidin-3-O-rutinoside, and cyanidin-3-O-glucoside (C3G). A correlation study between activity and components revealed that TAC was highly correlated with antioxidant and antihyperglycemic activities, and in principal component analysis, C3G is highly correlated with antioxidant activity and Pg3G is highly correlated with the antihyperglycemic effect of everbearing strawberries. Among the four everbearing strawberry cultivars, ‘Gwanha’ and ‘Goha’ are rich sources of pelargonidin showing strong α-glucosidase inhibitory activity and are promising dietary sources to prevent diabetes.

Background In malnourished patients, postoperative morbidity, hospitalization period, and medical expenses are reportedly to be high. We evaluated the clinical impact of a preoperative nutritional support program (PNSP) among malnourished cancer patients. Methods For this quasi-experimental study, we enrolled 90 patients who underwent major pancreatobiliary cancer surgery. Malnutrition was defined as at least one of the following: (1) Patient-Generated Subjective Global Assessment (PG-SGA) grade B or C; (2) > 10% weight loss within 6 months; (3) body mass index 2; and (4) serum albumin level < 3.0 g/dL. Forty-five malnourished patients allocated to the PNSP group received in-hospital PNSP for a median of 6 (4–35) days. In the PNSP group, the nutrition support team calculated the patients’ daily nutritional requirements based on their nutritional status and previous day’s intake. The supplementation targets were as follows: total calorie intake, 30–35 kcal/kg/day; protein intake, 1.2–1.5 g/kg/day; and lipid intake, 1–1.5 g/kg/day. Patients who did not meet the diagnostic criteria for malnutrition were allocated to the well-nourished group and underwent surgery without receiving the PNSP (n = 45). We compared the perioperative nutritional indices (as measured using PG-SGA), postoperative outcome, and quality of life (QOL) according to the European Organization for Research and Treatment of Cancer Quality of Life Questionnaire version 3.0. Results In the PNSP group, the proportion of patients with serum prealbumin p = 0.013). Moreover, patients with PG-SGA grade A had a statistically significant increase (2.2% vs. 50%, p < 0.001). The overall and major complication rates were higher in the PNSP group than in the well-nourished group without significance (51.1%, 33.3%; 42.2%, 26.7%, respectively). However, the overall and major complication rates were similar between the subgroup with PG-SGA improvement after PNSP and the well-nourished group (40.9% vs. 42.2%, p = 0.958; 27.3% vs. 26.7%, p = 0.525, respectively). QOL indicators in the PNSP group were comparable with those in the well-nourished group after PNSP. Conclusion PNSP may improve perioperative nutritional status and clinical outcomes among malnourished patients with pancreatobiliary cancer.

Agrimonia pilosa L. (AP) showed potent &alpha, glucosidase inhibitory (AGI) activity, but it is uncertain what phytochemicals play a key factor. The phytochemical study of AP based on AGI activity led to the isolation of four isocoumarins, agrimonolide (1), agrimonolide-6-O-&beta, d-glucopyranoside (2), desmethylagrimonolide (3), desmethylagrimonolide-6-O-&beta, d-glucopyranoside (4), and four flavonoids, luteolin (5), quercetin (6), vitexin (7), and isovitexin (8). The four isocoumarins were isolated as &alpha, glucosidase inhibitors for the first time. Isocoumarins, compound 1 (agrimonolide) and 3 (desmethylagrimonolide) showed strong &alpha, glucosidase inhibitory activities with IC50 values of 24.2 and 37.4 &micro, M, respectively. Meanwhile, isocoumarin and flavonoid glycosides showed weak AGI activity. In the kinetic analysis, isocoumarins, compounds 1 and 3 showed non-competitive inhibition, whereas flavonoid, compound 6 showed competitive inhibition.

To compare the antioxidant properties and flavonols in various parts; dry skin (DS) and edible portion (EP), of 8 red onions (Allium cepa L, ROs), total content of phenolics (TPC), flavonoids (TFC), and anthocyanins (TAC) and DPPH radical scavenging properties were estimated and the content of six flavonols were quantified by HPLC–PDA analysis. The major component of DS and EP of RO was quercetin and quercetin-4′-glucoside, respectively. Score plots of the PCA and PLS-DA were segregated by flavonols content and antioxidant properties according to the EP and DS of ROs. Loading plot of the PCA showed that the quercetin and sum of flavonol content were highly correlated with antioxidant activity of ROs. Therefore, flavonol content and antioxidant activity can be used as markers for distinct parts of ROs.

Diabetes mellitus (DM) is prevalent in patients with pancreatic cancer and tends to improve after tumor resection. However, the glycemic response of non-pancreatic cancer patients after surgery has not been examined in detail. We aimed to investigate the changes in glucose metabolism in patients with pancreatic cancer or non-pancreatic cancer after pancreatoduodenectomy (PD). We prospectively enrolled 48 patients with pancreatic cancer and 56 patients with non-pancreatic cancer, who underwent PD. Glucose metabolism was assessed with fasting glucose, glycated hemoglobin (HbA1c), plasma C-peptide and insulin, quantitative insulin check index (QUICKI), and a homeostatic model assessment of insulin resistance (HOMA-IR) and β cell (HOMA-β) before surgery and 6 months after surgery. Patients were divided into 2 groups: “improved” and “worsened” postoperative glycemic response, according to the changes in HbA1c and anti-diabetic medication. New-onset DM was defined as diagnosis of DM ≤ 2 years before PD, and cases with DM diagnosis >2 years preceding PD were described as long-standing DM. After PD, insulin resistance (IR), as measured by insulin, HOMA-IR and QUICKI, improved significantly, although C-peptide and HOMA-β decreased. At 6 months after PD, new-onset DM patients showed improved glycemic control in both pancreatic cancer patients (75%) and non-pancreatic cancer patients (63%). Multivariate analysis showed that long-standing DM was a significant predictor for worsening glucose control (odds ratio = 4.01, P = .017). Favorable glycemic control was frequently observed in both pancreatic cancer and non-pancreatic cancer after PD. PD seems to contribute improved glucose control through the decreased IR. New-onset DM showed better glycemic control than long-standing DM.

The antioxidant potentials of the methanol extract and its various fractions from Agrimonia pilosa Ledeb were measured as 1,1-diphenyl-2-picrylhydrazyl (DPPH), and 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging abilities as well as the reducing power decreasing NO in vitro . The methanol extract of Agrimonia pilosa Ledeb showed significantly strong scavenging effects on free radicals of DPPH, ABTS, and NO. Hexane fraction (HF), ethyl acetate fraction (EF) and n-butyl alcohol fraction (BF) were prepared by solvent fractionation. By comparison of polyphenol contents among BF and HF, EF with high polyphenol contents showed the highest DPPH, ABTS, and NO scavenging effects with the value of 50.2%, 80.4%, and 65.7%, respectively, at the highest tested dose. HPLC analysis revealed the presence of various phenolic compounds in EF of Agrimonia pilosa Ledeb. These results suggest that EF could be considered as natural antioxidant sources and dietary nutritional supplements to prevent oxidation-related diseases.

The aim of this work is to evaluate the potential of oriental melon (Cucumis melo L. var. makuwa Makino) seeds for the management of type 2 diabetes by controlling glucose absorption. The α-glucosidase and α-amylase inhibitory effects of the hexane extracts from oriental melon seeds were investigated. A bioassay-guided fractionation technique was used to elucidate the principal active components. The results show that the hexane extract from oriental melon seeds exhibited high inhibitory activities against α-glucosidase and α-amylase. The hexane extract was further fractionated into four sub-fractions. Among them, the sub-fraction F-1 exhibited the most potent anti-diabetic effect. The active components were isolated and identified by gas chromatography/mass spectroscopy (GC-MS). Free fatty acids showed significant hypoglycemic activity (p < 0.001) and fatty acid composition influenced enzyme inhibitory activities. These results suggest that oriental melon seeds could be used to prevent type 2 diabetes.

Methanol extracts from 100 Korean varieties of red pepper (Capsicum annuum L) were obtained. Chromatic parameters (L*, a*, and b*) and total phenolic content were analyzed. By evaluation of total phenolic content and 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging based-antioxidant associated with surface color measurement, red pepper varieties were classified into four groups by hierarchical cluster analysis. Cultivars of ‘PR-Sangsaeng’, ‘PR-Jijon’, ‘PREowoolrim’, ‘PR-Chambut’, ‘PAK37’, and ‘Hojanggoonbigalim” had high quantity of pigments and high phenolic content. These six cultivars also with higher levels of antioxidant might give an advantage to local growers in Korea. For further cytostatic activity evaluation, extracts from various parts including pericarp, seed, and stalk of cultivar ‘PAK37’ and ‘Hojanggoonbigalim’ were prepared. Four human cancer cells (HepG2, AGS, MCF-7, and HT-29) were used. The tumor cell growth inhibitory effect was evaluated by in vitro MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. High capsaicin content and antioxidant activity-containing red pepper stalk extract showed the strongest cytostatic activity. Tumor cell growth inhibitory activity was positively correlated with the capsaicin content. The anticancer potentials of various red pepper parts were in the following order: stalk > seed > pericarp. The data suggest that red pepper parts might have a promising health benefit against liver cancer, colon cancer and gastric cancer more than breast cancer.

The aim of this study was to assess the potential of oriental melon ( Cucumis melo L. var. makuwa Makino) seeds for the management of hyperglycemia linked to type 2 diabetes. The inhibitory effects of the hexane extracts of roasted melon seed on α-glucosidase and α-amylase were examined under different roasting temperatures, and compared with those of the unroasted seeds. The highest hypoglycemic activity was exerted by the seed roasted at 250 °C for 90 min with an inhibition value of 87.7% and 52.3% against α-amylase and α-glucosidase, respectively. The α-glucosidase and α-amylase inhibitory effects were strongly correlated with the levels of triacylglyceride esterified with linoleic acid (trilinolein). These results suggest that oriental melon seed extracts contain TAG and unsaturated fatty acids, which are potent inhibitors of α-glucosidase and α-amylase Hence it is clear that oriental melon seeds, which at present are considered as agricultural waste, may usefully be extracted and added to foods.

Red pepper stalks, an agricultural waste product, are casually discarded at landfills where they oxidize and harm the local ecology. To our knowledge, no feasible method has been designed to evaluate the bioavailability of red pepper stalks. Therefore, the present study focused on the stalk waste investigating its superoxide dismutase (SOD) activity and inhibitory effect on nitric oxide (NO) production in macrophages. Interestingly, by comparison with red pepper pericarp and placenta extracts, the stalks were found to have higher phenolic, flavonoid, and capsaicin contents. Chromatographic data showed differences in the amounts of phenolic compounds in various parts of red pepper. At a concentration of 100 μg/mL, the stalk, placenta, and pericarp had SOD activities of 52.3%, 7.4%, and 10.4%, respectively. A very high level of chlorogenic acid (3.82 mg/g d w) and p-coumaric acid (2.98 mg/g d w) gave the stalks of red peppers the most powerful antioxidant activity among the three tested parts. The high phenolic and SOD activity-containing stalks also had the most significant NO inhibitory effect (53.5%) in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. These results demonstrated that there is an opportunity to develop a new anti-inflammatory agent from agricultural wastes.

Extracts from the pericarp, placenta and stalk of red pepper (Capsicum annuum L) were investigated to determine their antioxidant and in vitro inhibitory potential against key enzymes relevant for hyperglycemia and hypertension. We examined the total phenolic and capsaicin content in red pepper extract. Anti-hyperglycemia relevant in vitro α-glucosidase inhibitory activity correlated strongly to the antioxidant activity measured by the 1, 1-diphenyl-2-picrylhydrazyl method. The high phenolic and capsaicin content-containing red pepper stalk was found to have strong α-amylase and strong α-glucosidase inhibitory effects. The pericarp and placenta had high angiotensin I-converting enzyme (ACE) inhibitory activity and also had good α-glucosidase inhibitory profiles. Inhibition of these enzymes provides a strong biochemical basis for the management of type 2 diabetes by controlling glucose absorption and reducing associated hypertension, respectively. Practical Applications The inhibitory effect on key enzymes relevant for hyperglycemia (α-glucosidase and α-amylase) and hypertension (ACE) of the red pepper pericarp, placenta and stalk was investigated in this study. The in vitro inhibitory activities of α-amylase, α-glucosidase and ACE provide a strong biochemical rationale for further in vivo studies for type 2 diabetes through the control of glucose absorption and for the reduction of the associated hypertension. Furthermore, red pepper stalk, which has always been considered as an agricultural waste product, was an effective inhibitor of α-glucosidase and α-amylase. This study shows the potential of this agricultural waste product as a food additive and therapeutic agent for clinical applications.

Glucosinolates, their hydrolysis product concentrations, and the quinone reductase (QR) inducing activity of extracts of leaf tissue were assayed from 39 arugula (Eruca sativa Mill.) accessions. Arugula accessions from Mediterranean countries (n = 16; Egypt, Greece, Italy, Libya, Spain, and Turkey) and Northern Europe (n = 2; Poland and United Kingdom) were higher in glucosinolates and their hydrolysis products, especially glucoraphanin and sulforaphane, compared to those from Asia (n = 13; China, India, and Pakistan) and Middle East Asia (n = 8; Afghanistan, Iran, and Israel). The QR inducing activity was also the highest in Mediterranean and Northern European arugula accessions, possibly due to a significant positive correlation between sulforaphane and QR inducing activity (r = 0.54). No nitrile hydrolysis products were found, suggesting very low or no epithiospecifier protein activity from these arugula accessions. Broad sense heritability (H(2)) was estimated to be 0.91-0.98 for glucoinolates, 0.55-0.83 for their hydrolysis products, and 0.90 for QR inducing activity.

The objective of this study was to investigate the anticancer effects of the extracts of oriental melon seeds. Various solvent extracts of oriental melon seeds were prepared and their anticancer effects were examined using in vitro MTT and CV assays. The anticancer effects of various extracts of oriental melon seeds were also examined in five human cancer cell lines including A549, AGS, HT-29, MCF-7 and HepG2. The ethanol extract of heated oriental melon seeds showed the potent cytotoxic effects especially against mouse hepatoma cell line(Hepa1c1c7), human hepatoma cell line(HepG2) and human breast cancer cell line(MCF-7). These data suggest that oriental melon seeds can be a promising anticancer agent against human liver and breast cancer.

Ginsenoside Rg3 was reported to have important biological activities. We demonstrate conjugation and quantification procedures of ginsenoside Rg3 to gold nanoparticles for future biological and medical applications. Ginsenoside Rg3 was conjugated to spherical gold nanoparticles using a bifunctional heptaethylene glycol linker. The sulfhydryl group of heptaethylene glycol was adsorbed onto gold nanoparticles, and carboxylic acid end of heptaethylene glycol was bonded through a hydroxyl group of Rg3 via ester bond formation. The conjugation of Rg3 was characterized with various spectroscopic techniques, high resolution-transmission electron microscopy, and using Rg3 monoclonal antibody. The Rg3- functionalized gold nanoparticles were 4.7 ± 1.0 nm in diameter with a surface charge of ‒4.12 mV. The total number of Rg3 molecules conjugated to a 3.6 mL solution of gold nanoparticle was determined to be 9.5 × 10 14 corresponding to ~6 molecules of Rg3/gold nanoparticle. These results suggest that ginsenoside Rg3 is successfully conjugated to gold nanoparticles via heptaethylene glycol linker. The quantification was performed by using Rg3 monoclonal antibody without interference of gold’s intrinsic color.

Although pepper leaves have been consumed as a traditional folk food in Korea, chemopreventive researches on pepper leaves are very rare. Thus, chemopreventive activity of pepper leaves was evaluated by isolating active compounds from pepper leaves. The methanol extract of pepper leaves showed significantly strong quinone reductase (QR) inductive activity compared to that of broccoli. Through partition and column chromatography, two major QR inducers were isolated from pepper leaves. Based on visible spectra, thin layer chromatography, solubility, chemical reactions, and DIP-MS, two major QR inducers from pepper leaves were identified as lutein and β-carotene. The concentration required to double the specific activity of QR (CD) values of lutein and β-carotene were 87.5 and 10.0 μM, respectively.

The study investigated the effect of shopping orientations of male and female consumers on the attitude toward sales clerk`s service and shopping environments. The subjects of the study were male and female consumers who were residents in Seoul. Among the 400 distributed questionnaires, 364 questionnaires were used for data analysis. Statistical analyses used for the study were cluster analysis, t-test, ANOVA, Duncan`s multiple range test, and . The results showed that shopping orientations of male and female consumers had 6 factors: pleasure, economic, store loyal, planned, convenience, and impulsive. These 6 factors were classified into 5 groups by cluster analysis: pleasure/impulsive group, planned group, economic/ convenient group, planned/store loyal group, and low interest group. In regard to the differences among the five shopping orientation groups, the result showed that the groups were significantly different concerning the attitude toward sales clerk`s service and shopping environments. In addition, male and female consumers were significantly different in shopping orientations, and the attitude toward sales clerk`s service and shopping environment. For example, female consumers sought more pleasurable shopping while male consumers sought more store loyal shopping. Based on the findings of this study, the marketing strategies can be developed fur the specific segmented groups.

Olive (Olea europaea) contains large quantity of triterpene acids including oleanolic acid (6) as a major one. Varieties of biological activities exhibited by triterpene acids attracted our attentions, especially from pharmaceutical viewpoints. Cell culture of olive plant was induced and its triterpene constituents were studied. From the cell suspension cultures, six ursane type triterpene acids; ursolic acid (9), pomolic acid (10), rotundic acid (11), tormentic acid (12), 2alpha-hydroxyursolic acid (13) and 19alpha-hydroxyasiatic acid (14), and two oleanane type acids; oleanolic acid and maslinic acid (7), have been isolated. Quantity of ursane type triterpene acids produced by cell cultures was larger than that of oleanane type. Further, a multifunctional oxidosqualene cyclase (OSC) named OEA was cloned by homology based PCRs from the same cultured cells. Major product of OEA is alpha-amyrin (ursane skeleton), showing good accordance to higher content of ursane-type triterpene acids in the cultured cells, and strongly suggesting OEA to be a major contributor OSC for their production.

Young barley leaves (YLB) have been no studies comparing the antioxidant activities of various cultivars, or differences the antioxidant activity at different harvest times. The objective of this study was to evaluate the differences in the antioxidant activities of YLB by different cultivars and growth stages. The 4 Korean YLB, Nakyoung, Dahyang, Saegang, and Boanchal, were sprouted, and their total polyphenols, total flavonoids, and ABTS radical cation (ABTS.+) scavenging activity were measured. The 4 cultivars exhibited high total polyphenol contents (TPC) and total flavonoid contents (TFC), with a range of 1047.8-1263.2 GAE mg.100 g-1 and 443.7-550.7 CE mg.100 g-1, DW, respectively. In addition, they exhibited high levels of ABTS.+ (RC50 value range of 41.8-80.8 ug.mL-1) scavenging activity. After sprouting, the antioxidant activity of the 4 cultivars increased. That is, in these YLB, the TPC, TFC and radical scavenging ability were enhanced by sprouting. Lutonarin (LN) and saponarin (SN) are the major compounds of YLB. LN exhibited stronger radical scavenging activity than SN. Over time, LN contents increased and SN contents decreased. As a result, the antioxidant ability of YLB was improved with increased growing time.

The sustainable synthesis of gold nanoparticles from gold ions was conducted with caffeic acid as a green reducing agent. The formation of gold nanoparticles was confirmed by spectroscopic and microscopic methods. Spherical nanoparticles with an average diameter of 29.99 ± 7.43 nm were observed in high- resolution transmission electron microscopy and atomic force microscopy images. The newly prepared gold nanoparticles exhibited catalytic activity toward the reduction of 4-nitrophenol to 4-aminophenol in the presence of sodium borohydride. This system enables the preparation of green catalysts using plant natural products as reducing agents, which fulfills the growing need for sustainability initiatives.

Wild lowbush blueberry fruit extract was fractionated using vacuum chromatography and analyzed for chemopreventive potential using bioassays that test the ability of compounds to inhibit the initiation, promotion, and progression stages of carcinogenesis. A fraction containing phytosterols was active against the initiation stage (quinone reductase assay). However, more polar compounds were inhibitors of later stages of carcinogenesis; a fraction containing flavan-3-ols and fractions containing mainly anthocyanins, phenolic acids, flavan-3-ols, and some proanthocyanidin dimers demonstrated activity against the promotion stage (cyclooxygenase and ornithine decarboxylase assays, respectively), and a proanthocyanidin-rich fraction demonstrated antiproliferation activity (inhibition of cancerous murine hepatocyte proliferation is associated with the progression stage). These results indicate that lowbush blueberries contain a range of compounds that have bioactivity against multiple stages of carcinogenesis, and different types of phenolic compounds are active at different stages.

The female parts of hops (Humulus lupulus L.) show estrogenic effects as well as cancer chemopreventive potential. We analyzed the chemopreventive mechanism of hops by studying its antioxidative activities and its effect on the detoxification of a potentially toxic quinone (menadione). The detoxification enzyme quinone reductase [(NAD(P)H:quinone oxidoreductase, QR] protects against quinone-induced toxicity and has been used as a marker in cancer chemoprevention studies. Although the hop extract was only a weak quencher of free radicals formed from 1,1-diphenyl-2-picrylhydrazyl, it demonstrated strong QR induction in Hepa 1c1c7 cells. In addition, compounds isolated from hops including xanthohumol (XH) and 8-prenylnaringenin were tested for QR induction. Among these, XH was the most effective at inducing QR with a concentration required to double the specific activity of QR (CD value) of 1.7 +/- 0.7 microM. In addition, pretreatment of Hepa1c1c7 cells with XH significantly inhibited menadione-induced DNA single-strand breaks. The QR inhibitor dicumarol reversed the protective effect of XH against menadione-induced DNA damage. Because the expression of QR and other detoxifying enzymes is known to be upregulated by binding of the transcription factor Nrf2 to the antioxidant response element (ARE), the reporter activity mediated by ARE in HepG2-ARE-C8 cells was investigated after incubation with XH for 24 h. Under these conditions, XH increased ARE reporter activity in a dose-dependent manner. One mechanism by which XH might induce QR could be through interaction with Keap1, which sequesters Nrf2 in the cytoplasm, so that it cannot activate the ARE. Using LC-MS-MS, we demonstrated that XH alkylates human Keap1 protein, most likely on a subset of the 27 cysteines of Keap1. This suggests that XH induces QR by covalently modifying the Keap1 protein. Therefore, XH and hops dietary supplements might function as chemopreventive agents, through induction of detoxification enzymes such as QR.

Activity-guided fractionation of the EtOAc-soluble extract of the stems of Couepia ulei, using a bioassay based on the induction of quinone reductase (QR) in cultured Hepa 1c1c7 mouse hepatoma cells led to the isolation of two active compounds, a new natural product, erythro-2,3-bis(4-hydroxy-3-methoxyphenyl)-3-ethoxypropan-1-ol (1), and a known compound, evofolin-B (2), along with five inactive compounds all of known structure, viz., betulinic acid, oleanolic acid, pomolic acid, (+/-)-syringaresinol, and ursolic acid. These isolates were identified by analysis of physical and spectral data. Compounds 1 and 2 exhibited QR inducing activity, with observed CD (concentration required to double induction) values of 16.7 and 16.4 microM, respectively.

α-Tocopheryl succinate (TOS), a vitamin E analog, is a promising anticancer agent due to its abilities to inhibit proliferation and to induce apoptosis in a variety of human malignant cell lines, while being relatively less active toward normal cells. However, the molecular mechanisms underlying the apoptotic effects of TOS are not precisely understood. Reports that TOS can generate reactive oxygen species (ROS) prompted us to investigate the role of ROS in TOS-induced apoptosis in cancer cells. We found that the human lung cancer A549 and H460 cell lines were much more sensitive to TOS-induced apoptosis than the human glioblastoma T98G and U87MG cell lines. Our data suggested that the differential TOS sensitivity was not caused by differences in the uptake and retention of TOS between TOS-sensitive and –resistant cancer cells. The differential ability of cancer cells to generate ROS in response to TOS appears to be an important factor in determining the susceptibility of cells to TOS-induced apoptosis. Our results further suggest that TOS-induced generation of ROS is involved in caspase-independent apoptosis. Taken together, our findings suggest an important role of ROS generation in TOS-induced, caspase-independent apoptosis of cancer cells. © 2004 Wiley-Liss, Inc.

A new butenylflavanone, (2S)-5-hydroxy-7-methoxy-8-[(E)-3-oxo-1-butenyl]flavanone (1), and a new rotenoid, 4',5'-dihydro-11,5'-dihydroxy-4'-methoxytephrosin (2), as well as three active flavonoids of previously known structure, isoliquiritigenin (3), genistein (4), and chrysoeriol (5), along with nine known inactive compounds, alpha-toxicarol (6), sumatrol, 6a,12a-dehydro-alpha-toxicarol, 11-hydroxytephrosin, obovatin, marmesin, lupenone, benzyl benzoate, and benzyl trans-cinnamate, were isolated from an ethyl acetate-soluble extract of the stems of Tephrosia toxicaria, using a bioassay based on the induction of quinone reductase (QR) in cultured Hepa 1c1c7 mouse hepatoma cells to monitor chromatographic fractionation. The structures of compounds 1 and 2 were elucidated by spectroscopic data interpretation. All isolates were evaluated for their potential cancer chemopreventive properties utilizing an in vitro assay to determine quinone reductase induction. Selected compounds were tested in a mouse mammary organ culture assay to evaluate the inhibition of 7,12-dimethylbenz[a]anthracene (DMBA)-induced preneoplastic lesions.

Introduction: A patient-derived xenograft (PDX) as a preclinical model can reflect the pathological and molecular features and drug responsibility of a patient’s tumor. PDXs have been generated by subcutaneously implanting surgically resected tumor fragments into immunodeficient mice. Unfortunately, 80 % of pancreatic cancer patients is unresectable and they show highly aggressive and metastatic tumors. In most cases, diagnoses are confirmed histologically and diagnosed through endoscopic ultrasonography-guided/fine-needle aspiration (EUS/FNA) or percutaneous liver biopsy. However, they are not suitable for subcutaneous implantation into mice due to their threadlike shape and very small size. Therefore, the lack of patient-derived model system in pancreatic cancer is in desperate need of new strategy to cover unresectable patients as well as resectable. Here, we pioneered the development of a unresectable patient-derived orthotopic xenograft (PDOX) model satisfied with short period and high success rate, and made the best use of them as the test model for drug response. Methods and Results: PDOX models were established with a technique of direct surgical orthotopic implantation into the pancreatic tail of Athymic nude mice. PDOX models using fine needle biopsy had a higher success rate of engraftment, nearly 40% (17 cases among 44 cases) in patients with a time to progression of Conclusion: Collectively, our PDOX models using needle biopsy specimens can reflect the characteristics of unresectable patients and give the expectation the drug responsibility. They furthermore might be valuable in a screening and development system for targeted therapeutics, which can be applied to a wide range of pancreatic cancer patients. Citation Format: A-Ra Jeon, Sun Il Choi, Sang-Jae Park, Sung-Sik Han, Eun Kyung Hong, Sun-Young Kong, Min Kyeong Kim, Kyong-Ah Yoon, Young-Hwan Koh, Ju Hee Lee, Woo Jin Lee, Young Hwa Kang, Sang Myung Woo, Yun-Hee Kim. Patient derived orthotopic xenograft (PDOX) model developed from needle biopsy specimen replicated clinical outcomes in advanced pancreatic cancer [abstract]. In: Proceedings of the American Association for Cancer Research Annual Meeting 2017; 2017 Apr 1-5; Washington, DC. Philadelphia (PA): AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 2815. doi:10.1158/1538-7445.AM2017-2815

Neuraminidase (NA) is one of the key enzymes responsible for bacterial infection and pathogenesis. This study aimed to gain deeper insights into the inhibitory effects of flavone-glucosides (1-9) isolated from barley sprouts (BS) on neuraminidase activity. The isolated compounds were identified as, lutonarin (1), saponarin (2), isoorientin (3), orientin (4), isovitexin (5), isoscoparin-7-O-[6-sinapoyl]-glucoside (6), isoscoparin-7-O-[6-feruloyl]-glucoside (7), isovitexin-7-O-[6-sinapoyl]-glucoside (8), and isovitexin-7-O-[6-feruloyl]-glucoside (9). Among them, compounds 1-5 exhibited neuraminidase-inhibitory activities in a dose-dependent manner, with IC50 values ranging from 20.1 to 32.7 μM, in a non-competitive inhibition mode according to kinetic studies. Moreover, the individual flavone-glucoside levels differed notably, in particular, lutonarin (1) and saponarin (2) were shown to be present in the greatest amounts, according to UPLC analysis. Consequently, our results suggest that BS may be utilized as an effective NA inhibitor in human health food, additives, and feed.

Objective : In order to report the process of treatment of Aplastic anemia by herbal acupuncture Methods: This case was diagnosed as deficiency of Yang of spleen and kidneys, deficiency of Ki and blood, and fevescence from the deficiency of Urn. Hominis Placenta herbal acupuncture and Bee-venom acupuncture were choosen as the method to treat the case. Results: 1. The nocturnal fevescence and indigestion was decreased during the times when Hominis Placenta herbal acupuncture was used once a day. 2. The mobility of the joints was improved and the inflamation on the joints was decreased during the times when Bee-venom acupuncture was used every other day. 3. The interval between the transfusion was extended during the times when Hominis Placenta herbal acupuncture and Bee-venom acupuncture were used by turns. Conclution : Hominis Placenta herbal acupuncture and Bee-venom acupuncture sucessfully imporved the symtoms of patient with Aplastic anemia

β-Catenin serves not only as a structural component of the E-cadherin-mediated cell–cell adhesion system, but also as a signaling molecule of the Wnt/wingless pathway. Deregulated expression of β-catenin and mutations of the gene have been identified in a number of human malignancies. To determine the role of β-catenin defects in stomach cancer, we investigated β-catenin exon 3 mutations and altered protein expression in 77 primary gastric carcinomas and 11 cell lines. In addition, the immunohistochemical expression pattern of β-catenin in 303 consecutive gastric cancers was determined and their relationships with clinicopathologic features and patient outcome were investigated. This study revealed 5% (4 of 77) tumors and 27% (3 of 11) cell lines with β-catenin gene alteration, 6 missense mutations, and 1 interstitial deletion. These genetic changes were shown to correlate closely with nuclear localization of the protein (p = 0.001). In an immunohistochemical analysis, abnormal expressions of β-catenin, such as nuclear accumulation and loss of membranous distribution, were detected in 27% (81 of 303) of tumors overall. These altered β-catenin expressions were more commonly observed in 37% (58 of 158) diffuse type gastric carcinomas (p < 0.001). Loss of membranous β-catenin staining was associated with poor survival (p = 0.045). In conclusion, our results demonstrate that β-catenin mutations are common in gastric cancer cell lines but occur infrequently in gastric carcinoma tissues. These mutations are one of the causes of the nuclear accumulation of β-catenin. Frequent abnormalities of β-catenin expression in gastric carcinoma support the idea that both structural and signaling functions of the protein play a critical role in gastric carcinogenesis. © 2001 Wiley-Liss, Inc.

An antimetastatic and cytostatic substance, termed AC7-1, was isolated from Ardisia crispa and identified as a benzoquinonoid compound, 2-methoxy-6-tridecyl-1,4-benzoquinone. It was originally characterized as the potent PAF (platelet-activating factor) receptor-binding antagonist with nonspecific antiplatelet effects on platelet aggregation induced by various agonists including PAF, ADP, thrombin and collagen. The nonspecific antiaggregatory properties of AC7-1 drew our interest given its possible relationship in integrin receptor-binding antagonistic activity. The integrin receptor plays an important role in metastasis and thrombosis as the cell surface transmembrane protein. Based on the aforementioned facts, the antimetastatic activities of AC7-1 were examined using various in vitro and in vivo metastasis assays. AC7-1 strongly blocked B16-F10 melanoma cell adhesion to extracellular matrix (ECM) and B16-F10 melanoma cell invasion. AC7-1 also remarkably inhibited pulmonary metastasis and tumor growth in vivo. AC7-1 inhibited B16-F10 melanoma cell adhesion to only specific synthetic peptides including RGDS. These findings suggest that antimetastatic activities of AC7-1 can be caused by blocking integrin-mediated adherence. We found AC7-1 to be a potential candidate for the development of a new antimetastatic drug.

A new dibenzocyclooctadiene lignan named angustifolin D (1) together with four known lignans: kadsulignan L (2), kadsulignan N (3), schisantherin P (4) and meso-dihydroguaiaretic acid (5) were isolated from the stems of Kadsura angustifolia. Their structures and stereochemistries were elucidated by spectral studies. Compounds 2 and 5 showed moderate platelet-activating factor (PAF) antagonistic activities with IC50 values of 2.6 x 10(-5) and 4.1 x 10(-5) M, respectively.

Frangufoline, a sedative 14-membered frangulanine-type cyclopeptide alkaloid, was found to be rapidly converted, via enzymatic process, in vitro and in vivo in rodents to M1 ((S)-(N,N-dimethylphenylalanyl)-(2S,3S)-3-[(p-formylphenoxy) leucyl]-(S)-leucine); which is a substituted linear tripeptide. The reaction did not require low molecular weight cofactors, and mammalian serum failed to catalyze the reaction. Structure-reactivity study of cyclopeptide alkaloid analogs suggested that the enamide bond is the site being cleaved, and the reaction was inhibited by organophosphorus esters such as BPNP and by eserine at higher concentrations but not by eserine at lower concentrations or by EDTA and PCMB. On the basis of these results, a possible mechanism for metabolic conversion of frangufoline to M1 was proposed, in which oxidation of the vinyl group and enzyme-catalyzed hydrolysis of the adjacent amide bond, possibly by B-esterase-like enzyme, proceed in a concerted manner.

Substituted cinnamoyl-tyramine derivatives were synthesized by DCC-coupling of substituted cinnamic acid with tyramine or tyramine methyl-1-ether to evaluate PAF-receptor binding antagonistic activities and inhibitory activities on PAF-induced platelet aggregation with interest on structure-activity relations. The results show that 3,4-dimethoxy-cinnamoyl tyramine-amide or its methyl ether have significant PAF-receptor binding antagonistic activity and platelet anti-aggregatory activities.

We report the synthesis of biogenic silver nanoparticles using chlorogenic acid as a bioreducing agent. Chlorogenic acid is a polyphenol compound abundant in coffee. UV-Vis spectra showed the characteristic surface plasmon resonance band at 415 nm, indicating the successful synthesis of biogenic silver nanoparticles. Spherical and irregular shaped nanoparticles were observed with an average diameter of 19.29 +/- 8.23 nm. The reaction yield from silver ion to silver nanoparticles was observed as 95.43% by using inductively coupled plasma-mass spectrometry. Fourier transform infrared spectra revealed that the -C = O groups of chlorogenic acid may coordinate or complex into silver nanoparticles. Biogenic silver nanoparticles exerted higher antibacterial activity against Gram-negative bacteria than against Gram-positive bacteria. Interestingly, a comparable antibacterial activity to a standard antibiotic was observed against two strains of Pseudomonas aeruginosa (minimum inhibitory concentration of 0.66 microg/mL). The synergistic effect of a combination of silver nanoparticles and chlorogenic acid on antibacterial activity is obvious, leading to approximately 8-fold enhancement in the case of Pseudomonas aeruginosa when compared with chlorogenic acid alone. The present report suggests that a pure compound with a plant origin is capable of being a bioreducing agent for the synthesis of biogenic silver nanoparticles with superior antibacterial activity, opening up many applications in nanomedicine and nanobiotechnology.

Pinusolide, a potent platelet activating factor (PAF) receptor binding antagonist, inhibited PAF-induced aggregation of rabbit platelets with an IC50 value of 5 microM, whereas no inhibitory effects on the aggregation induced by ADP, thrombin, and collagen were observed. Pinusolide protected the mice from PAF-induced lethality with ED50 values of 1.1 mg/kg, i.v. and 69 mg/kg, p.o. Topically given pinusolide at 2 mg/ear effectively inhibited croton oil induced mouse ear edema. All the pinusolide treated ears recovered to normal healthy appearance in a sharp contrast to totally necrotized untreated ears. These results indicated that pinusolide is a potent and specific PAF antagonist in all experimental models as shown in vitro, in vivo, and in animal tests.

The bioassay-guided purification of ether extracts of Alpinia officinarum led to the isolation of two new compounds 6-hydroxy-1,7-diphenyl-4-en-3-heptanone ( 1 ) and 6-(2-hydroxy-phenyl)-4-methoxy-2-pyrone ( 4 ) as well as three known compounds 1,7-diphenyl-4-en-3-heptanone ( 2 ), 1,7-diphenyl-5-methoxy-3-heptanone ( 3 ), and apigenin ( 5 ). Their structures were established on the basis of spectral methods. All three diarylheptanoids 1 , 2 , and 3 exhibited potent PAF receptor binding inhibitory activities with an IC 50 of 1.3, 5.0, and 1.6 μM, respectively. These studies have identified diarylheptanoids as a novel class of potent PAF antagonists.

Cassiae Semen (seeds of Cassia tora) showed a remarkably different HPLC chromatogram after being treated with a crude enzyme extract from Aspergillus usamii. Increased and decreased compounds were identified as aurantio-obtusin and glucoaurantio-obtusin, respectively. The aurantio-obtusin content reached its maximum level (133.58 +/- 0.39 microg/mg extract) after being incubated for 50 min at 37 degrees C, whereas the inactivated crude enzyme-treated control remained unchanged (54.13 +/- 1.33 microg/mg). On the other hand, the glucoaurantio-obtusin content decreased by less than one-third (51.09 +/- 1.63 microg/ mg) of the untreated control (143.19 +/- 2.12 microg/mg), suggesting that an increase in aurantio-obtusin content originated from the enzymatic cleavage of its glucoside glucoaurantio-obtusin.

A C29-triterpene, beccaridiol (1), a dihydrochalcone natural product, 2',4'-dihydroxy-3-(4-methoxyphenyl)-propiophenone (2), as well as three known compounds, 4'-hydroxy-1',2'-dihydro-beta-ionone, 4'-O-methyldavidigenin (3), and ursolic acid, have been isolated from an EtOAc-soluble extract of the leaves of Diplectria beccariana. Beccaridiol (1) was characterized as an ursane-type 28-nortriterpene possessing an unusual aromatic E-ring by spectroscopic data interpretation. The relative configuration of this unusual isolate was established by analyzing the observed NOESY NMR correlations, and the absolute stereochemistry of 1 was then determined based on the circular dichroism (CD) spectrum of its 2,3-di-p-bromobenzoate (1b) derivative. All isolates were evaluated for their potential cancer chemopreventive properties utilizing a cell culture assay to determine quinone reductase induction.

European elderberry (Sambucus nigra), recognized in Europe for its health-promoting properties for many generations, is known to contain a range of anthocyanins, flavonoids, and other polyphenolics that contribute to the high antioxidant capacity of its berries. American elderberry (Sambucus canadensis), on the other hand, has not been cultivated, bred, and promoted as a medicinal plant like its better-characterized European counterpart. In this study, aqueous acetone extracts of the berries from these two species were fractionated and tested in a range of assays that gauge anticarcinogenic potential. Both cultivated S. nigra and wild S. canadensis fruits demonstrated significant chemopreventive potential through strong induction of quinone reductase and inhibition of cyclooxygenase-2, which is indicative of anti-initiation and antipromotion properties, respectively. In addition, fractions of S. canadensis extract showed inhibition of ornithine decarboxylase, an enzyme marker related to the promotion stage of carcinogenesis. Analysis of active fractions using mass spectrometry and liquid chromatography-mass spectrometry revealed, in addition to flavonoids, the presence of more lipophilic compounds such as sesquiterpenes, iridoid monoterpene glycosides, and phytosterols.

The sustainable synthesis of gold nanoparticles from gold ions was conducted with caffeic acid as a green reducing agent. The formation of gold nanoparticles was confirmed by spectroscopic and microscopic methods. Spherical nanoparticles with an average diameter of 29.99 ± 7.43 nm were observed in high-resolution transmission electron microscopy and atomic force microscopy images. The newly prepared gold nanoparticles exhibited catalytic activity toward the reduction of 4-nitrophenol to 4-aminophenol in the presence of sodium borohydride. This system enables the preparation of green catalysts using plant natural products as reducing agents, which fulfills the growing need for sustainability initiatives.