Two new prenylated chalcones from the leaves of Artocarpus lowii King

Two minor prenylated chalcones were isolated for the first time from the leaves of Artocarpus lowii King. These prenylated chalcones were identified as 2- hydroxyparatocarpin C (1) and 2ʹ,3,4ʹ,4-tetrahydroxy-3ʹ-prenylchalcone (2). The structures of these prenylated chalcone were elucidated by utilizing the data values obtained from1H NMR,13C NMR, DEPT, COSY, IR, UV and MS, as well as by comparison with literature values

Modulatory Effect of Phytoestrogens and Curcumin on Induction of Annexin 1 in Human Peripheral Blood Mononuclear Cells and their Inhibitory Effect on Secretory Phospholipase A2

Purpose: To investigate the modulatory effects of phytoestrogens (coumestrol, daidzein and genistein) and curcumin on the induction and secretion of annexin-1 (ANXA-1) in human peripheral blood mononuclear cells (PBMCs) under inflammatory and non-inflammatory conditions, as well as their effect on the activity of phospholipase A2-V (sPLA2-V).Methods: The modulatory effects of phytoestrogens and curcumin on the induction ofANXA1 were investigated via sandwich ELISA method, while their effects on the activity of sPLA2-V were determined by photometric assays. Besides, the cell viability of these compounds was determined by standard trypan blue exclusion method using PBMCs.Results: The results indicate a significant increase (p < 0.05) in the total content ofANXA1, particularly by coumestrol (p < 0.01), in both inflammatory and non-inflammatory cells. Besides, the compounds also exhibited a dose-dependent inhibition of sPLA2-V activity; however, among these compounds, curcumin and genistein were the strongest inhibitors with an IC50 value of 11.1 ± 0.3 μM and13.6 ± 0.6 μM respectively.Conclusion: The investigated compounds have a potential to induce synthesis and secretion ofANXA1 as well as inhibitory activity of sPLA2-V, suggesting their inhibitory role in phospholipid metabolism and inflammation.Keywords: Inflammation, Annexin-1, Phospholipase A2, Phytoestrogens, Curcumin

Evaluation of the Antioxidant Activities of Ya-hom Intajak, a Thai Herbal Formulation, and its Component Plants

Purpose: To evaluate the antioxidant effect of 80 % ethanol extract and its n-hexane and dichloromethane fractions of Ya-hom Intajak, and its 47 medicinal plants components.Methods: The 80 % ethanol extract and its n-hexane and dichloromethane fractions were investigated on human low-density lipoprotein (LDL)  peroxidation by thiobarbituric acid reactive substances (TBARS) assay. Antioxidant effect was also determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity and ferric reducing antioxidant power (FRAP) assays.Results: The extract of Ya-hom Intajak exhibited moderate DPPH  scavenging activity with an IC50 value of 99.08 µg/ml and a FRAP value of 1.12 mmol FeSO4/g. Among the individual plants, Terminalia chebula Retz., Caesalpinia sappan L., Cinnamomum bejolghota (Buch.-Ham.) and Ci. verum J. Presl, showed strong antioxidant activities. T. chebula was the most potent plant in the DPPH assay while Ca. sappan had the highest FRAP value. Among the extracts, the dichloromethane fraction showed the highest inhibitory effect on LDL peroxidation with a half maximal inhibitory concentration (IC50) value comparable to that of probucol (0.82 µg/ml). Pearson correlation analysis revealed that total phenolic content (TPC) showed high positive correlations with FRAP (r = 0.908, p < 0.01) and DPPH activities (r= 0.648, p < 0.01).Conclusion: Ya-hom Intajak is a valuable source of natural antioxidants and has a potential application as a cardiovascular protective formulation.Keywords: Ya-hom Intajak, Antioxidant activity, Terminalia chebula Retz., Caesalpinia sappan L., Cinnamomum bejolghota (Buch.-Ham.), Ci. verum J. Presl , Phenolic conten

Screening for thalassaemia among group of students of a higher institution – our experience

Introduction: Thalassaemia is an inherited blood disorder and is a significant public health alarm in Malaysia with many not knowing they are carriers of this haemoglobin disorders. Materials and methods: This study conducted a one off collection of blood samples from 72 Malays students of International Islamic University Malaysia (IIUM) in Kuantan. Blood samples were subjected to conventional haemoglobin analyses that include full blood count and picture, HPLC, Haemoglobin electrophoresis and H-inclusion test. All samples were also genotyped for alpha thalassaemia–1 of Southeast Asia (a-Thal1SEA). Result: There were 17(23.6%) students who were diagnosed as thalassaemia carriers. Out of this, four (5.5 %) and six (8.3 %) students were presumptive β-thalassaemia trait and Haemoglobin-E trait as determined by the HPLC assay respectively. Nine (12.5%) students were genotyped a-Thal1SEA among whom two were also β-thalassaemia carriers. All thalassaemia cases had MCH of < 27pg. Nonetheless, two out of six Haemoglobin-E trait and three out of nine a-Thal1SEA carrier had MCV value of >80fL. Two out of four (50%) presumptive β -thalassaemia trait and one out of six (17%) students of presumptive Haemoglobin-E trait had family history of thalassaemia respectively. Conclusion: The high occurrence of the three common types of thalassaemia carrier (β, Hb-E and a-Thal1SEA thalassaemia) in our small group of subjects could be due to better participation of students who had family history of thalassaemia. The study reaffirmed the importance of molecular study for detection of alpha-thalassaemia and the use of MCH value of <27pg rather than MCV value of < 80fL for prediction of thalassaemia. KEYWORDS: Thalassaemia, screening, diagnosis, genetic carriers

Bioassay-guided isolation of a potent platelet-activating factor antagonist alkenylresorcinol from Ardisia elliptica

In the course of our search for novel platelet-activating factor (PAF) antagonists from medicinal plants, the methanol extract of the leaves of Ardisia elliptica Thunb. was investigated for its inhibitory effects on PAF receptor binding to rabbit platelets using 3H-PAF as a ligand. The methanol extract showed inhibitory activity of 53.9% and its ethyl acetate, n-butanol, and methanol fractions exhibited 48.6%, 39.0%, and 22.0% inhibition, respectively. Bioassay-guided fractionation of the ethyl acetate fraction led to the isolation of a new alkenylresorcinol, 5-(Z-heptadec-4′-enyl)resorcinol, together with 5-pentadecylresorcinol. The alkenylresorcinol showed a strong inhibition with an IC50 value of 7.1 µM. The structures of the compounds were elucidated by spectroscopic techniques

Momordica charantia (bitter melon) inhibits primary human adipocyte differentiation by modulating adipogenic genes

<p>Abstract</p> <p>Background</p> <p>Escalating trends of obesity and associated type 2 diabetes (T2D) has prompted an increase in the use of alternative and complementary functional foods. <it>Momordica charantia </it>or bitter melon (BM) that is traditionally used to treat diabetes and complications has been demonstrated to alleviate hyperglycemia as well as reduce adiposity in rodents. However, its effects on human adipocytes remain unknown. The objective of our study was to investigate the effects of BM juice (BMJ) on lipid accumulation and adipocyte differentiation transcription factors in primary human differentiating preadipocytes and adipocytes.</p> <p>Methods</p> <p>Commercially available cryopreserved primary human preadipocytes were treated with and without BMJ during and after differentiation. Cytotoxicity, lipid accumulation, and adipogenic genes mRNA expression was measured by commercial enzymatic assay kits and semi-quantitative RT-PCR (RT-PCR).</p> <p>Results</p> <p>Preadipocytes treated with varying concentrations of BMJ during differentiation demonstrated significant reduction in lipid content with a concomitant reduction in mRNA expression of adipocyte transcription factors such as, peroxisome proliferator-associated receptor γ (PPARγ) and sterol regulatory element-binding protein 1c (SREBP-1c) and adipocytokine, resistin. Similarly, adipocytes treated with BMJ for 48 h demonstrated reduced lipid content, perilipin mRNA expression, and increased lipolysis as measured by the release of glycerol.</p> <p>Conclusion</p> <p>Our data suggests that BMJ is a potent inhibitor of lipogenesis and stimulator of lipolysis activity in human adipocytes. BMJ may therefore prove to be an effective complementary or alternative therapy to reduce adipogenesis in humans.</p

Studies of synthetic chalcone derivatives as potential inhibitors of secretory phospholipase A2, cyclooxygenases, lipoxygenase and pro-inflammatory cytokines

Ibrahim Jantan,1,* Syed Nasir Abbas Bukhari,1,* Olayiwola A Adekoya,2 Ingebrigt Sylte3 1Drug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia, Kuala Lumpur, Malaysia; 2Department of Pharmacy, Faculty of Health Science, UiT The Arctic University of Norway, Troms&oslash;, Norway; 3Department of Medical Biology, Faculty of Health Science, UiT The Arctic University of Norway, Troms&oslash;, Norway *These authors contributed equally to this work Abstract: Arachidonic acid metabolism leads to the generation of key lipid mediators which play a fundamental role during inflammation. The inhibition of enzymes involved in arachidonic acid metabolism has been considered as a synergistic anti-inflammatory effect with enhanced spectrum of activity. A series of 1,3-diphenyl-2-propen-1-one derivatives were investigated for anti-inflammatory related activities involving inhibition of secretory phospholipase A2, cyclooxygenases, soybean lipoxygenase, and lipopolysaccharides-induced secretion of interleukin-6 and tumor necrosis factor-alpha in mouse RAW264.7 macrophages. The results from the above mentioned assays exhibited that the synthesized compounds were effective inhibitors of pro-inflammatory enzymes and cytokines. The results also revealed that the chalcone derivatives with 4-methlyamino ethanol substitution seem to be significant for inhibition of enzymes and cytokines. Molecular docking experiments were carried out to elucidate the molecular aspects of the observed inhibitory activities of the investigated compounds. Present findings increase the possibility that these chalcone derivatives might serve as a beneficial starting point for the design and development of improved anti-inflammatory agents. Keywords: anti-inflammatory, tumor necrosis factor-alpha, lipopolysaccharides, molecular dockin