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Min-Tsang Hsieh, Li-Jiau Huang, Tian-Shung Wu, Hui-Yi Lin, Susan L Morris-Natschke, Kuo-Hsiung Lee, Sheng-Chu Kuo
The aim of this study was to develop a new drug substance with low toxicity and effective inhibitory activity against cisplatin-resistant oral cancer. The naturally produced pterostilbene was selected as the lead compound for design and synthesis of a series of bis(hydroxymethyl)propionate-based prodrugs. All derivatives were screened for antiproliferative effects against the cisplatin-resistant oral squamous (CAR) cell line and the results indicated that several compounds demonstrated superior inhibitory activity compared with pterostilbene and resveratrol...
June 8, 2018: Bioorganic & Medicinal Chemistry
Bora Tastekin, Aykut Pelit, Sait Polat, Abdullah Tuli, Leman Sencar, Mustafa Muhlis Alparslan, Yusuf Kenan Daglioglu
Aims: The aim of this study was to investigate the effects of pterostilbene (PTS) (trans-3,5-dimethoxy-4'-hydroxystilbene) and resveratrol (RSV) (trans-3,5,4' trihydroxystilbene) applied at different doses for the treatment of streptozotocin- (STZ-) induced diabetic rats. Materials and Methods: At the end of the 5-week experimental period, the right gastrocnemius muscles of the rats were examined biomechanically, while the left ones were examined histologically...
2018: Evidence-based Complementary and Alternative Medicine: ECAM
José L González-Alfonso, David Rodrigo-Frutos, Efres Belmonte-Reche, Pablo Peñalver, Ana Poveda, Jesús Jiménez-Barbero, Antonio O Ballesteros, Yoshihiko Hirose, Julio Polaina, Juan C Morales, María Fernández-Lobato, Francisco J Plou
The synthesis of a novel α-glucosylated derivative of pterostilbene was performed by a transglycosylation reaction using starch as glucosyl donor, catalyzed by cyclodextrin glucanotransferase (CGTase) from Thermoanaerobacter sp. The reaction was carried out in a buffer containing 20% ( v / v ) DMSO to enhance the solubility of pterostilbene. Due to the formation of several polyglucosylated products with CGTase, the yield of monoglucoside was increased by the treatment with a recombinant amyloglucosidase (STA1) from Saccharomyces cerevisiae ( var...
May 25, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Megan Beetch, Katarzyna Lubecka, Heather Kristofzski, Matthew Suderman, Barbara Stefanska
SCOPE: Searching for correlations between dietary polyphenols and risk of chronic diseases has been a challenge due to the lack of quantitative evaluation methods of long-term exposure. We previously observed substantial DNA methylation changes in human cancer cells upon treatment with polyphenols of the stilbenoid class. When induced in normal cells, such molecular changes might persist and reflect chronic exposure. METHODS AND RESULTS: Using Illumina-450K microarray, we delineated a genome-wide DNA methylation landscape in MCF10A human immortalized mammary epithelial cells exposed to resveratrol at non-cytotoxic 15μM dose for 9 days...
May 24, 2018: Molecular Nutrition & Food Research
Yun Yao, Kehai Liu, Yueliang Zhao, Xiaoqian Hu, Mingfu Wang
Pterostilbene (Pte) and 4′-Methoxyresveratrol (4MR) are methylated derivatives of resveratrol. We investigated the anti-inflammatory effect of Pte and 4MR in lipopolysaccharide (LPS)-stimulated RAW264.7 murine macrophages. Both Pte and 4MR significantly reduced LPS-induced nitric oxide release by inhibiting the inducible nitric oxide synthase mRNA expression. Moreover, both of them inhibited LPS-induced mRNA expression of inflammatory cytokines including monocyte chemoattractant protein (MCP)-1, interleukin (IL)-6 and IL-1β, and tumor necrosis factor α (TNF-α), and attenuated LPS-induced nuclear factor-κB (NF-κB) activation by decreasing p65 phosphorylation...
May 11, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Qiushi Li, Long Chen, Xuewen Liu, Xidong Li, Yue Cao, Yang Bai, Fengjiao Qi
Neuroinflammation has been known as an important pathogenetic contributor of Alzheimer's disease (AD). Pterostilbene is a natural compound which has neuroprotective activity. However, the effect of pterostilbene on amyloid-β (Aβ)-induced neuroinflammation has not been clarified. The aim of the present study was to investigate the effect of pterostilbene on Aβ-induced neuroinflammation in microglia. The results indicated that pterostilbene attenuated Aβ1-42 -induced cytotoxicity of BV-2 cells. Aβ1-42 induced NO production and iNOS mRNA and protein expression, while pterostilbene inhibited the induction...
May 8, 2018: Journal of Cellular Biochemistry
Jing Sun, Huixia Huo, Yuelin Song, Jiao Zheng, Yunfang Zhao, Wenzhe Huang, Yonghua Wang, Jingbo Zhu, Pengfei Tu, Jun Li
Although wide applications towards ischemic stroke in clinic, the therapeutic materials of Longxuetongluo Capsule (LTC) that is composed of total phenolic extract of Chinese dragon's blood, are still largely unclear. Exposure pattern characterization of those drug-derived components in vivo, notably in circulation system has been recommended as a viable approach to disclose the effective components of a given herbal medicine. Herein, we aimed to develop a robust method being capable of multi-component quantification in either rat plasma or tissues following oral administration of LTC, and to clarify the kinetic profiles of 11 primary drug-derived phenolic derivatives...
July 15, 2018: Journal of Pharmaceutical and Biomedical Analysis
Heikki Eräsalo, Mari Hämäläinen, Tiina Leppänen, Ilari Mäki-Opas, Mirka Laavola, Raisa Haavikko, Jari Yli-Kauhaluoma, Eeva Moilanen
Stilbenoids are a group of polyphenolic compounds found in plants, trees, berries, and nuts. Stilbenoids have been shown to serve an antimicrobial and antifungal function in plants. There is also evidence that as a part of the human diet, stilbenoids play an important role as antioxidants and may have anti-inflammatory effects. The PI3K/Akt pathway is a well-characterized signaling pathway controlling cellular functions involved in growth and cell cycle and in metabolism. There is also increasing evidence to show the involvement of this pathway in the regulation of inflammatory responses...
May 25, 2018: Journal of Natural Products
Ramoji Kosuru, Yin Cai, Vidya Kandula, Dan Yan, Chunyan Wang, Hong Zheng, Yalan Li, Michael G Irwin, Sanjay Singh, Zhengyuan Xia
BACKGROUND/AIMS: Pterostilbene (PT) exerts antidiabetic effects by decreasing blood glucose and modulating lipid metabolism and has been shown to attenuate myocardial ischemia-reperfusion (IR) injury in non-diabetic subjects. However, whether PT can protect against myocardial IR injury in diabetes is unknown. AMPK stimulation is indispensable in offering cardioprotection against myocardial IR injury in diabetes by limiting cardiac apoptosis. Thus, we hypothesized that PT may confer protection against myocardial IR injury in diabetes via AMPK activation...
2018: Cellular Physiology and Biochemistry
Yunxiaozhu Zheng, Xiaoming Qiang, Rui Xu, Qing Song, Chaoquan Tian, Hongyan Liu, Wei Li, Zhenghuai Tan, Yong Deng
A series of pterostilbene β-amino alcohol derivatives were designed, synthesized and evaluated as multifunctional agents for the treatment of Alzheimer's disease (AD). In vitro assays demonstrated that most of the derivatives were selective acetylacholinesterase (AChE) inhibitors with moderate multifunctional properties. Among them, compound 5f exhibited the best inhibitory activity for EeAChE (IC50  = 24.04 μM), that was better than pterostilbene under our experimental condition. In addition, compound 5f displayed reasonable antioxidant activity and could confer significant neuroprotective effect against H2 O2 -induced PC-12 cell injury...
August 2018: Bioorganic Chemistry
Ramoji Kosuru, Vidya Kandula, Uddipak Rai, Swati Prakash, Zhengyuan Xia, Sanjay Singh
PURPOSE: Oxidative stress has a pivotal role in the pathogenesis of diabetes-associated cardiovascular problems, which has remained a primary cause of the increased morbidity and mortality in diabetic patients. It is of paramount importance to prevent the diabetes-associated cardiac complications by reducing oxidative stress with the help of nutritional or pharmacological agents. Pterostilbene (PT), the primary antioxidant in blueberries, has recently gained attention for its promising health benefits in metabolic and cardiac diseases...
April 2018: Cardiovascular Drugs and Therapy
Yizi Xia, Ying Chen, Luming Tang, Zheng Wang, Yu Zheng
Acute kidney injury (AKI) is a severe complication of sepsis with a high mortality and morbidity. Pterostilbene (Pte) has been suggested to confer anti-apoptotic and anti-inflammatory effects. In the current study, the effects of Pte on AKI were evaluated in septic mice. Cecal ligation and puncture surgery was performed to induce sepsis. The results suggested that Pte administration significantly decreased the levels of serum urea nitrogen and creatinine, and improved the survival rate of septic mice. Additionally, the renal injury induced by sepsis was attenuated by pterostilbene treatment...
April 2018: Experimental and Therapeutic Medicine
Guang Ren, Agnes M Rimando, Suresh T Mathews
Pterostilbene, a bioactive component of blueberries and grapes, shows structural similarity to resveratrol, and exhibits antioxidant, anti-inflammatory, anti-cancer, hypoglycemic, and cholesterol lowering effects. Recent evidence indicates that pterostilbene is an agonist of the nuclear receptor, peroxisome proliferator-activated receptor-alpha (PPAR-α). Since PPAR-α agonists induce peroxisomal proliferation and fatty acid oxidation, we examined gene expression of acyl CoA oxidase (ACO) and carnitine palmitoyl transferase-1 (CPT-1)...
April 6, 2018: Biochemical and Biophysical Research Communications
Bolanle C Akinwumi, Kimberly-Ann M Bordun, Hope D Anderson
Stilbenoids are a group of naturally occurring phenolic compounds found in various plant species. They share a common backbone structure known as stilbene, but differ in the nature and position of substituents. Stilbenoids are classified as phytoalexins, which are antimicrobial compounds produced de novo in plants to protect against fungal infection and toxins. In this review, the biological effects of stilbenoids such as resveratrol, pterostilbene, gnetol and piceatannol are discussed. Stilbenoids exert various biological activities ranging from cardioprotection, neuroprotection, anti-diabetic properties, depigmentation, anti-inflammation, cancer prevention and treatment...
March 9, 2018: International Journal of Molecular Sciences
Hui-Ping Chang, Chi-Cheng Lu, Jo-Hua Chiang, Fuu-Jen Tsai, Yu-Ning Juan, Je-Wei Tsao, Hong-Yi Chiu, Jai-Sing Yang
Pterostilbene is a natural polyphenolic compound that is primarily found in fruits, such as blueberries and has a similar structure to resveratrol. Pterostilbene exhibits antioxidant, anti-inflammatory and antitumor activity but the effects of pterostilbene on drug-resistant oral cancer cells and its underlying mechanisms of action have not yet been explored. Therefore, the present study was performed to clarify the anticancer effects of pterostilbene on cisplatin-resistant human oral cancer CAR cells. The results demonstrated that CAR cells exhibited marked shrinkage, cell membrane breakage and autophagic vacuole formation following treatment with pterostilbene...
March 2, 2018: International Journal of Oncology
Kaushiki Chatterjee, Dina AlSharif, Christina Mazza, Palwasha Syar, Mohamed Al Sharif, Jimmie E Fata
Cervical cancer is one of the most common cancers in women living in developing countries. Due to a lack of affordable effective therapy, research into alternative anticancer compounds with low toxicity such as dietary polyphenols has continued. Our aim is to determine whether two structurally similar plant polyphenols, resveratrol and pterostilbene, exhibit anticancer and anti-HPV (Human papillomavirus) activity against cervical cancer cells. To determine anticancer activity, extensive in vitro analyses were performed...
February 21, 2018: Nutrients
Ascensión Martínez-Márquez, Jaime A Morante-Carriel, Javier Palazon, Roque Bru-Martínez
Stilbenes are naturally scarce high-added-value plant compounds with chemopreventive, pharmacological and cosmetic properties. Bioproduction strategies include engineering the metabolisms of bacterial, fungal and plant cell systems. Strikingly, one of the most effective strategies consists in the elicitation of wild grapevine cell cultures, which leads to vast stilbene resveratrol accumulation in the extracellular medium. The combination of both cell culture elicitation and metabolic engineering strategies to produce resveratrol analogs proved more efficient for the hydroxylated derivative piceatannol than for the dimethylated derivative pterostilbene, for which human hydroxylase HsCYP1B1- and grapevine O-methyltransferase VvROMT-transformed cell cultures were respectively used...
May 25, 2018: New Biotechnology
Ka-Wai Tam, Chi-Tang Ho, Shih-Hsin Tu, Wen-Jui Lee, Ching-Shui Huang, Ching-Shyang Chen, Chih-Hsiung Wu, Chia-Hwa Lee, Yuan-Soon Ho
Vitamin E (Vit. E) is considered an essential dietary nutrient for humans and animals. An enormous body of evidence indicates the biological and protective effects of Vit. E consumption. Tocopherol-associated protein (TAP) is a major tocopherol-binding protein affecting Vit. E stimulation and downstream signaling transduction. However, how Vit. E utilizes TAP as an anti-cancer mechanism remains unclear. Microarray analysis of signature gene profiles in breast cancer cells treated with α-tocopheryl succinate (α-TOS, a Vit...
January 12, 2018: Oncotarget
Dan Gao, Sanhui Jing, Qian Zhang, Ge Wu
Previous studies have demonstrated that pterostilbene (Pter) prevents oxidative stress, suppresses cell growth and exhibits anti-fungal and anti-inflammatory effects. Pter is used to treat a number of clinical diseases, including Alzheimer's disease, various malignancies and hypercholesteremia. The aim of the present study was to investigate whether Pter protects against acute renal ischemia reperfusion injury (IRI) and inhibits oxidative stress, inducible nitric oxide synthase (iNOS) expression and inflammation in rats...
January 2018: Experimental and Therapeutic Medicine
Yu-Yuan Qian, Zhi-Su Liu, Zidong Zhang, Anait S Levenson, Kun Li
Pterostilbene (Pter) is reported to exhibit an anticancer effect in hepatocellular carcinoma (HCC). In order to explore the anticancer mechanism in HCC cells, the present study aimed to investigate whether pterostilbene (Pter) may increase phosphatase and tensin homolog (PTEN) expression through targeted downregulation of microRNA (miRNA/miR)-19a in hepatocellular carcinoma (HCC). The proliferation, apoptosis and cell cycle was analyzed in the SMMC‑7721 HCC cell line by MTT assays and flow cytometry methods...
April 2018: Molecular Medicine Reports
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