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Chiang-Wen Lee, Miao-Ching Chi, Tsung-Ming Chang, Ju-Fang Liu
Osteosarcoma is a malignant primary bone tumor that responds poorly to both chemotherapy and radiation therapy. However, because of side effects and drug resistance in chemotherapy and the insufficiency of an effective adjuvant therapy for osteosarcoma, it is necessary to research novel treatments. This study was the first to investigate the anticancer effects of the flavonoid derivative artocarpin in osteosarcoma. Artocarpin induced cell apoptosis in three human osteosarcoma cell lines-U2OS, MG63, and HOS...
December 13, 2018: Journal of Cellular Physiology
Abdi Wira Septama, Ibrahim Jantan, Pharkphoom Panichayupakaranant
OBJECTIVES: To investigate the effects of flavonoids isolated from Artocarpus heterophyllus. heartwood on chemotaxis, phagocytosis, reactive oxygen species (ROS) production and myeloperoxidase (MPO) activity of human phagocytes. METHODS: Chemotaxis was evaluated using a modified Boyden chamber and phagocytosis was determined by flowcytometer. Respiratory burst was investigated by luminol-based chemiluminescence assay while MPO activity was determined by colorimetric assay...
September 2018: Journal of Pharmacy and Pharmacology
Chiang-Wen Lee, Lee-Fen Hsu, Ming-Hsueh Lee, I-Ta Lee, Ju-Fang Liu, Yao-Chang Chiang, Ming-Horng Tsai
Glioblastoma multiforme (GBM) is an extremely aggressive and devastating malignant tumor in the central nervous system. Its incidence is increasing and the prognosis is poor. Artocarpin is a natural prenylated flavonoid with various anti-inflammatory and anti-tumor properties. Studies have shown that artocarpin is associated with cell death of primary glioblastoma cells. However, the in vivo effects and the cellular and molecular mechanisms modulating the anticancer activities of artocarpin remain unknown. In this study, we demonstrated that treating the glioblastoma cell lines U87 and U118 cells with artocarpin induced apoptosis...
2018: Frontiers in Pharmacology
Jutatip Kwankaew, Preeyawass Phimnuan, Sombat Wanauppathamkul, Jarupa Viyoch
Artocarpus altilis heartwood extract contains the bioactive compound artocarpin which exhibits melanogenesis inhibitory activity. However, the extract has poor solubility which affects the skin permeability of the compound. A chitosan hydrogel patch incorporating A. altilis heartwood extract was formulated to enhance the delivery of an amount of artocarpin sufficient for depigmenting the skin. The extract was prepared as an o/w microemulsion before blending with an aqueous solution of chitosan. The hydrogel patch was formulated by blending in a 1:1 ratio by weight of 4% w/w chitosan solution and 0...
July 2017: Journal of Cosmetic Science
Wei Qu, Xuezheng Liu
Artocarpin isolated from an agricultural plant Artocarpus communis has shows anti-inflammation and anticancer activities. In this study, we utilized recombinant human UDP-glucuronosyltransferasesupersomes (UGTs) and human liver microsomes to explore its inhibitory effect on UGTs and cytochrome p450 enzymes (CYPs). Chemical inhibition studies and screening assays with recombinant human CYPs were used to identify if CYP isoform is involved in artocarpin metabolism. Artocarpin showed strong inhibition against UGT1A3, UGT1A6, UGT1A7, UGT1A8, UGT1A9, UGT1A10, UGT2B7, CYP2C8 and CYP3A4...
April 2018: Biomedical Chromatography: BMC
Chung-Ju Yeh, Chin-Chuan Chen, Yann-Lii Leu, Ming-Wei Lin, Mei-Miao Chiu, Shu-Huei Wang
The skin protects the body against harmful substances and microorganisms. When the skin is damaged, wound healing must be finely regulated to restore the normal function of skin tissue. Artocarpin (ARTO), a prenylated flavonoid purified from the plant Artocarpus communis, has been reported to have anti-inflammatory and anti-cancer properties. The aim of the present study was to evaluate the wound healing potential and therapeutic mechanism of ARTO. Immunohistochemical staining of neutrophils and macrophages and mouse cytokine array analysis demonstrated that ARTO accelerates inflammatory progression and subsequently decreases persistent inflammation...
November 15, 2017: Scientific Reports
Narisara Tiraravesit, Philippe Humbert, Sophie Robin, Marion Tissot, Céline Viennet, Jarupa Viyoch
This study aimed to evaluate the protective effect of artocarpin-enriched (Artocarpus altilis) heartwood extract on the mechanical properties of UVB-irradiated fibroblasts. Human skin fibroblasts were pretreated with 50 μg/mL-1 extract and later irradiated with UVB (200 mJ/cm-2 ). They were then cultured within three-dimensional of free-floating and tense collagen lattices. The pretreatment of fibroblasts with the extract prior to UVB radiation showed cells protection against UVB-induced suppression of α-SMA expression, fibroblast migration and contraction...
October 2017: Photochemistry and Photobiology
Ming-Horng Tsai, Ju-Fang Liu, Yao-Chang Chiang, Stephen Chu-Sung Hu, Lee-Fen Hsu, Yu-Ching Lin, Zih-Chan Lin, Hui-Chun Lee, Mei-Chuan Chen, Chieh-Liang Huang, Chiang-Wen Lee
Artocarpin has been shown to exhibit cytotoxic effects on different cancer cells, including non-small cell lung carcinoma (NSCLC, A549). However, the underlying mechanisms remain unclear. Here, we explore both p53-dependent and independent apoptosis pathways in artocarpin-treated NSCLC cells. Our results showed that artocarpin rapidly induced activation of cellular protein kinases including Erk1/2, p38 and AktS473. Inhibition of these protein kinases prevented artocarpin-induced cell death. Moreover, artocarpin-induced phosphorylation of these protein kinases and apoptosis were mediated by induction of reactive oxygen species (ROS), as pretreatment with NAC (a ROS scavenger) and Apocynin (a Nox-2 inhibitor) blocked these events...
April 25, 2017: Oncotarget
Guochuan Sun, Zongping Zheng, Mee-Hyun Lee, Yijuan Xu, Soouk Kang, Zigang Dong, Mingfu Wang, Zhennan Gu, Haitao Li, Wei Chen
Artocarpus heterophyllus is an evergreen tree distributed in tropical regions, and its fruit (jackfruit) is well-known as the world's largest tree-borne fruit. Although A. heterophyllus has been widely used in folk medicines against inflammation, its potential in cancer chemoprevention remains unclear. Herein we identified artocarpin from A. heterophyllus as a promising colorectal cancer chemopreventive agent by targeting Akt kinase. Phenotypically, artocarpin exhibited selective cytotoxicity against human colon cancer cells...
May 3, 2017: Journal of Agricultural and Food Chemistry
Siti Awanis Abdullah, Shajarahtunnur Jamil, Norazah Basar, Siti Mariam Abdul Lathiff, Norzafneza Mohd Arriffin
A new dihydrochalcone, 2',4'-dihydroxy-3,4-(2″,2″-dimethylchromeno)-3'-prenyldihydrochalcone (1) together with 4-hydroxyonchocarpin (2), isobavachalcone (3), 4',5-dihydroxy-6,7-(2,2-dimethylpyrano)-2'-methoxy-8-γ,γ-dimethylallyflavone (4), artocarpin (5) and cycloheterophyllin (6) were successfully isolated from the leaves and heartwoods of Artocarpus lowii King (Moraceae). The structures of these compounds were fully characterised using spectroscopic methods and by direct comparison with published data...
May 2017: Natural Product Research
Xue Yao, Dang Wu, Ningning Dong, Ping Ouyang, Jiaqian Pu, Qian Hu, Jingyuan Wang, Weiqiang Lu, Jin Huang
Artocarpus heterophyllus, a popular tropical fruit commonly known as the jackfruit tree, is normally planted in subtropical or tropical areas. Since a variety of phytochemicals isolated from A. heterophyllus have been found to possess potently anti-inflammatory, antiviral and antimalarial activities, researchers have devoted much interest to its potential pharmaceutical value. However, the exact mechanism underlying its anti-inflammatory activity is not well characterized. In this study, seven natural products isolated from A...
July 25, 2016: International Journal of Molecular Sciences
Bruno Burlando, Marco Clericuzio, Laura Cornara
Hyperpigmentation is an abnormal darkening of the skin mostly derived from excessive melanin production. It is typical of skin disorders including melasma associated to pregnancy or age, freckles, sun freckles and photoaging, age spots, and actinic keratosis. These conditions can be uncomfortable for aesthetic reasons and specific depigmenting treatment is frequently requested. Tyrosinase (EC is the rate-limiting enzyme of melanin synthesis and the main target of antihyperpigmentation remedies. Much interest is focused on compounds able to inhibit tyrosinase activity, particularly natural products, for which there is an increasing demand in the fields of cosmetics and pharmaceutical applications...
2017: Mini Reviews in Medicinal Chemistry
Cheng-Wei Tzeng, Wen-Sheng Tzeng, Liang-Tzung Lin, Chiang-Wen Lee, Feng-Lin Yen, Chun-Ching Lin
BACKGROUND: Hepatocellular carcinoma (HCC) is the most common liver cancer worldwide, with poor prognosis and resistance to chemotherapy. This gives novel cancer treatment methods an overwhelming significance. Natural products offer great resources of developing new and effective chemopreventive or chemotherapeutic agents. Artocarpus communis extracts and its active constituent, prenylated flavonoid artocarpin induce human hepatocellular carcinoma cell death. However, the poor water solubility drawbacks of artocarpin restrict its clinical application and bioavailability...
May 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Elisabeth Walther, Zhongli Xu, Martina Richter, Johannes Kirchmair, Ulrike Grienke, Judith M Rollinger, Andi Krumbholz, Hans P Saluz, Wolfgang Pfister, Andreas Sauerbrei, Michaela Schmidtke
Secondary infections with Streptococcus pneumoniae cause severe pneumonia and enhance lethality during influenza epidemics and pandemics. Structural and functional similarities with viral neuraminidase (NA) suggest that the highly prevalent pneumococcal NAs, NanA and NanB, might contribute to this lethal synergism by supporting viral replication and that dual acting NA inhibitors (NAIs) will disrupt it. To verify this hypothesis, NanA and NanB were expressed in E. coli. After confirming their activity in enzyme assays, in vitro models with influenza virus A/Jena/8178/09 (Jena/8178) and the recombinant NanA or NanB (rNanA and rNanB) were established in A549 and MDCK cells to mimic the role of these pneumococcal NAs during co-infection...
2016: Frontiers in Microbiology
Abdi Wira Septama, Pharkphoom Panichayupakaranant
CONTEXT: Antibacterial resistance has dramatically increased and resulted in serious health problems worldwide. One appealing strategy to overcome this resistance problem is the use of combinations of antibacterial compounds to increase their potency. OBJECTIVE: The objective of this study is to determine the synergistic effects of artocarpin for ampicillin, norfloxacin, and tetracycline against methicillin-resistant Staphylococcus aureus (MRSA) as well as the Gram-negative bacteria Pseudomonas aeruginosa and Escherichia coli...
2016: Pharmaceutical Biology
Narisara Tiraravesit, Swanya Yakaew, Racharat Rukchay, Witoo Luangbudnark, Celine Viennet, Philippe Humbert, Jarupa Viyoch
ETHNOPHARMACOLOGICAL RELEVANCE: Artocarpus altilis (Moreceae) has been widely used as a traditional folk medicine in Southeast Asia for the treatment of many diseases, including skin disorders, such as ulcers and dermatitis. AIM OF THE STUDY: The present study aimed to investigate the ability of an artocarpin-enriched extract to prevent ultraviolet radiation B-induced photodamage. MATERIALS AND METHODS: The content of artocarpin in the extract was determined by high performance liquid chromatography (HPLC)...
December 4, 2015: Journal of Ethnopharmacology
Siti Mariam Abdul Lathiff, Noraini Jemaon, Siti Awanis Abdullah, Shajarahtunnur Jamil
Two new prenylated flavonoids, 4',5-dihydroxy-6,7-(2,2-dimethylpyrano)-2'-methoxy-8-γ,γ-dimethylallylflavone 1 and 3'-hydroxycycloartocarpin 2 along with six known flavonoids, 5,7-dihydroxy-4'-methoxy-8-prenylflavanone 3, isobavachalcone 4, pyranocycloartobiloxanthone A 5, artocarpin 6, chaplashin 7 and cycloartocarpin 8 were isolated for the first time from the leaves and the heartwoods of Artocarpus anisophyllus Miq. The structures of isolated flavonoids were elucidated spectroscopically using 1D and 2D NMR, FTIR, MS, UV and also by comparison with literature data...
March 2015: Natural Product Communications
Abdi Wira Septama, Pharkphoom Panichayupakaranant
CONTEXT: Preparations from Artocarpus heterophyllus Lam. (Moraceae) heartwoods are used in the traditional folk medicine for the treatment of inflammation, malarial fever, and to prevent bacterial and fungal infections. OBJECTIVE: The objective of this study was to isolate pure antibacterial compounds from A. heterophyllus heartwoods. MATERIALS AND METHODS: The dried and powdered A. heterophyllus heartwoods were successively extracted with the following solvents: hexane, ethyl acetate, and methanol...
2015: Pharmaceutical Biology
Stephen Chu-Sung Hu, Chi-Ling Lin, Hui-Min Cheng, Gwo-Shing Chen, Chiang-Wen Lee, Feng-Lin Yen
Artocarpin, a natural prenylated flavonoid, has been shown to have various biological properties. However, its effects on human cutaneous squamous cell carcinoma (SCC) have not been previously investigated. We set out to determine whether artocarpin has cytotoxic effects on SCC cells and whether its pharmacological activity is dependent on protein-nutrient concentration. Our results showed that treatment of HSC-1 cells (a human cutaneous SCC cell line) with artocarpin decreased cell viability and induced cell apoptosis by increasing caspase 3/7 activity...
2015: Evidence-based Complementary and Alternative Medicine: ECAM
E Walther, M Richter, Z Xu, C Kramer, S von Grafenstein, J Kirchmair, U Grienke, J M Rollinger, K R Liedl, H Slevogt, A Sauerbrei, H P Saluz, W Pfister, M Schmidtke
Streptococcus (S.) pneumoniae is a major cause of secondary bacterial pneumonia during influenza epidemics. Neuraminidase (NA) is a virulence factor of both pneumococci and influenza viruses. Bacterial neuraminidases (NAs) are structurally related to viral NA and susceptible to oseltamivir, an inhibitor designed to target viral NA. This prompted us to evaluate the antipneumococcal potential of two NA inhibiting natural compounds, the diarylheptanoid katsumadain A and the isoprenylated flavone artocarpin. Chemiluminescence, fluorescence-, and hemagglutination-based enzyme assays were applied to determine the inhibitory efficiency (IC(50) value) of the tested compounds towards pneumococcal NAs...
May 2015: International Journal of Medical Microbiology: IJMM
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