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Molecules, Volume 19, Issue 2 (February 2014), Pages 1378-2706

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Open AccessArticle Synthesis and Biological Evaluation of Substituted Desloratadines as Potent Arginine Vasopressin V2 Receptor Antagonists
Molecules 2014, 19(2), 2694-2706; https://doi.org/10.3390/molecules19022694
Received: 2 December 2013 / Revised: 14 January 2014 / Accepted: 26 January 2014 / Published: 24 February 2014
Cited by 3 | PDF Full-text (268 KB) | HTML Full-text | XML Full-text
Abstract
Twenty-one non-peptide substituted desloratadine class compounds were synthesized as novel arginine vasopressin receptor antagonists from desloratadine via successive acylation, reduction and acylation reactions. Their structures were characterized by 1H-NMR and HRMS, their biological activity was evaluated by in vitro and in vivo
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Twenty-one non-peptide substituted desloratadine class compounds were synthesized as novel arginine vasopressin receptor antagonists from desloratadine via successive acylation, reduction and acylation reactions. Their structures were characterized by 1H-NMR and HRMS, their biological activity was evaluated by in vitro and in vivo studies. The in vitro binding assay and cAMP accumulation assay indicated that these compounds are potent selective V2 receptor antagonists. Among them compounds 1n, 1t and 1v exhibited both high affinity and promising selectivity for V2 receptors. The in vivo diuretic assay demonstrated that 1t presented remarkable diuretic activity. In conclusion, 1t is a potent novel AVP V2 receptor antagonist candidate. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle Characteristics, Composition and Oxidative Stability of Lannea microcarpa Seed and Seed Oil
Molecules 2014, 19(2), 2684-2693; https://doi.org/10.3390/molecules19022684
Received: 13 November 2013 / Revised: 6 December 2013 / Accepted: 9 December 2013 / Published: 24 February 2014
Cited by 4 | PDF Full-text (202 KB) | HTML Full-text | XML Full-text
Abstract
The proximate composition of seeds and main physicochemical properties and thermal stability of oil extracted from Lannea microcarpa seeds were evaluated. The percentage composition of the seeds was: ash (3.11%), crude oil (64.90%), protein (21.14%), total carbohydrate (10.85%) and moisture (3.24%). Physicochemical properties
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The proximate composition of seeds and main physicochemical properties and thermal stability of oil extracted from Lannea microcarpa seeds were evaluated. The percentage composition of the seeds was: ash (3.11%), crude oil (64.90%), protein (21.14%), total carbohydrate (10.85%) and moisture (3.24%). Physicochemical properties of the oil were: refractive index, 1.473; melting point, 22.60°C; saponification value, 194.23 mg of KOH/g of oil; iodine value, 61.33 g of I2/100 g of oil; acid value, 1.21 mg of KOH/g of oil; peroxide value, 1.48 meq of O2/kg of oil and oxidative stability index, 43.20 h. Oleic (43.45%), palmitic (34.45%), linoleic (11.20%) and stearic (8.35%) acids were the most dominant fatty acids. Triacylglycerols with equivalent carbon number (ECN) 48 and ECN 46 were dominant (46.96% and 37.31%, respectively). The major triacylglycerol constituents were palmitoyl diolein (POO) (21.23%), followed by dipalmitoyl olein (POP) (16.47%), palmitoyl linoleyl olein (PLO) (12.03%), dipalmitoyl linolein (PLP) (10.85%) and dioleoyl linolein (LOO) (9.30%). The total polyphenol and tocopherol contents were 1.39 mg GAE g−1 DW and 578.56 ppm, respectively. γ-Tocopherol was the major tocopherol (437.23 ppm). These analytical results indicated that the L. microcarpa seed oil could be used as a frying oil and in the cosmetic industry. Full article
(This article belongs to the Section Natural Products Chemistry)
Open AccessArticle Comparative Diagnostic Techniques for Cryptosporidium Infection
Molecules 2014, 19(2), 2674-2683; https://doi.org/10.3390/molecules19022674
Received: 25 December 2013 / Revised: 20 January 2014 / Accepted: 21 January 2014 / Published: 24 February 2014
Cited by 8 | PDF Full-text (302 KB) | HTML Full-text | XML Full-text
Abstract
Diarrhoea caused by Cryptosporidium is usually mild in immune competent individuals but severe in the young and those with underlying disease leading to compromised immunity. The conventional diagnosis of Cryptosporidium requires observation of the infective oocysts however, their tiny size yields indistinct results,
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Diarrhoea caused by Cryptosporidium is usually mild in immune competent individuals but severe in the young and those with underlying disease leading to compromised immunity. The conventional diagnosis of Cryptosporidium requires observation of the infective oocysts however, their tiny size yields indistinct results, thus limiting the effectiveness of the conventional diagnostic technique, modified Ziehl-Neelsen (ZN) differential staining. Consequent to the abovementioned limitation, ZN staining, sandwich antigen detection enzyme linked immunosorbent assay (sad-ELISA) and a direct polymerase chain reaction (PCR) assay techniques were evaluated for diagnostic efficacy. Stool samples were collected from 180 consenting adult patients attending outpatient and inpatient clinics at Victoria Hospital, Alice, Eastern Cape Province of South Africa. Subjects were stratified as; 35 HIV-positive and diarrhoeagenic, 125 HIV-negative diarrhoeagenic and 20 apparently healthy controls. Cryptosporidium incidence following diagnostic techniques were 13 (37.1%; ZN staining), 26 (74.3%; sad-ELISA) and 23 (65.7%; PCR), respectively, among HIV-positive diarrhoeagenic patients and 34 (27.2%; ZN staining), 96 (76.8%; sad-ELISA) and 89 (71.2%; PCR) among HIV-negative diarrhoeagenic patients. Sensitivity, specificity and predictive values of the diagnostic techniques’ efficiency were: sensitivity: 46.2% (HIV-positive) and 32.3% (HIV-negative) against the ZN technique and 96.9% against sad-ELISA and PCR, respectively, for both HIV-positive and -negative patients; specificity was 88.9% (HIV-positive) and 96.6% (HIV-negative) against the ZN technique. Lastly, the predictive values were 92.3% (HIV-positive) and 96.9% (HIV-negative), respectively, following ZN staining. The sad-ELISA technique proved more suitable for the determination of the presence of Cryptosporidium oocysts. The high incidence of Cryptosporidium in HIV-positive subjects as compared to the HIV-negative population accentuates the significance of cryptosporidiosis diagnosis in the treatment and management of HIV cases. Full article
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Open AccessArticle Discovery of Novel c-Met Inhibitors Bearing a 3-Carboxyl Piperidin-2-one Scaffold
Molecules 2014, 19(2), 2655-2673; https://doi.org/10.3390/molecules19022655
Received: 21 January 2014 / Revised: 13 February 2014 / Accepted: 14 February 2014 / Published: 24 February 2014
Cited by 4 | PDF Full-text (528 KB) | HTML Full-text | XML Full-text
Abstract
A series of compounds containing a novel 3-carboxypiperidin-2-one scaffold based on the lead structure BMS-777607 were designed, synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against MKN45 cancer cell lines. The results indicated that five compounds exhibited significant inhibitory effect on
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A series of compounds containing a novel 3-carboxypiperidin-2-one scaffold based on the lead structure BMS-777607 were designed, synthesized and evaluated for their c-Met kinase inhibition and cytotoxicity against MKN45 cancer cell lines. The results indicated that five compounds exhibited significant inhibitory effect on c-Met with IC50 values of 8.6−81 nM and four compounds showed potent inhibitory activity against MKN45 cell proliferation, with IC50s ranging from 0.57−16 μM. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessArticle Synthesis of A New Class of Pyridazin-3-one and 2-Amino-5-arylazopyridine Derivatives and Their Utility in the Synthesis of Fused Azines
Molecules 2014, 19(2), 2637-2654; https://doi.org/10.3390/molecules19022637
Received: 27 January 2014 / Revised: 11 February 2014 / Accepted: 17 February 2014 / Published: 24 February 2014
Cited by 3 | PDF Full-text (516 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
A general route for the synthesis of a novel class of pyridazin-3-one derivatives 3 by the reaction in acetic anhydride between 3-oxo-2-arylhydrazonopropanals 1 and some active methylene compounds like p-nitrophenylacetic acid and cyanoacetic acid was established. Under these conditions the pyridazin-3-one derivatives
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A general route for the synthesis of a novel class of pyridazin-3-one derivatives 3 by the reaction in acetic anhydride between 3-oxo-2-arylhydrazonopropanals 1 and some active methylene compounds like p-nitrophenylacetic acid and cyanoacetic acid was established. Under these conditions the pyridazin-3-one derivatives 3 were formed as the sole isolable products in excellent yield. The 6-acetyl-3-oxopyridazine derivative 3l was reacted with DMF-DMA to afford the corresponding enaminone derivative 4, which reacts with a variety of aminoazoles to afford the corresponding azolo[1,5-a]pyrimidine derivatives 57. Also, in order to explore the viability and generality of a recently uncovered reaction between 3-oxo-2-arylhydrazonopropanals and active methylene compounds, a variety of 2-amino-6-aryl-5-arylazo-3-aroylpyridines 1619 were prepared by reacting 3-oxo-2-arylhydrazonopropanals with miscellaneous active methylene compounds like 3-oxo-3-phenylpropionitrile, hetaroylacetonitriles and cyanoacetamides. These 2-aminopyridine derivatives undergo smooth reactions with cyanoacetic acid that led to the formation in high yield of a new class of 1,8-naphthyridine derivatives 24. The structures of all new substances prepared in this investigation were determined by the different analytical spectroscopic methods, in addition to the X-ray crystallographic analysis. Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessArticle Three New Tetranorditerpenes from Aerial Parts of Acerola Cherry (Malpighia emarginata)
Molecules 2014, 19(2), 2629-2636; https://doi.org/10.3390/molecules19022629
Received: 15 January 2014 / Revised: 19 February 2014 / Accepted: 20 February 2014 / Published: 24 February 2014
Cited by 2 | PDF Full-text (267 KB) | HTML Full-text | XML Full-text | Supplementary Files
Abstract
Acerola cherry is a world famous fruit which contains abundant antioxidants such as vitamin C, anthocyanins, flavonoids, and phenolics. However, studies concerning bioactivity components from aerial parts of acerola (Malpighia emarginata) are scarce. In view of this, we have examined the
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Acerola cherry is a world famous fruit which contains abundant antioxidants such as vitamin C, anthocyanins, flavonoids, and phenolics. However, studies concerning bioactivity components from aerial parts of acerola (Malpighia emarginata) are scarce. In view of this, we have examined the constituents of aerial parts of acerola, and three new tetranorditerpenes acerolanins A–C (13) with a rare 2H-benz[e]inden-2-one substructure were isolated. Their structures were determined on the basis of spectral studies and acerolanin C was confirmed by X-ray crystallographic analysis. Furthermore, three new compounds have been studied for their cytotoxic activity. Full article
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Open AccessArticle Triptolide Induces S Phase Arrest and Apoptosis in Gallbladder Cancer Cells
Molecules 2014, 19(2), 2612-2628; https://doi.org/10.3390/molecules19022612
Received: 31 December 2013 / Revised: 13 February 2014 / Accepted: 13 February 2014 / Published: 24 February 2014
Cited by 16 | PDF Full-text (5918 KB) | HTML Full-text | XML Full-text
Abstract
Gallbladder carcinoma is the most common malignancy of the biliary tract, with a very low 5-year survival rate and extremely poor prognosis. Thus, new effective treatments and drugs are urgently needed for the treatment of this malignancy. In this study, for the first
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Gallbladder carcinoma is the most common malignancy of the biliary tract, with a very low 5-year survival rate and extremely poor prognosis. Thus, new effective treatments and drugs are urgently needed for the treatment of this malignancy. In this study, for the first time we investigated the effects of triptolide on gallbladder cancer cells and identified the mechanisms underlying its potential anticancer effects. The MTT assay showed that triptolide decreased cell viability in a dose- and time-dependent manner. The results of the colony formation assay indicated that triptolide strongly suppressed colony formation ability in GBC-SD and SGC-996 cells. Flow cytometric analysis revealed that triptolide induced S phase arrest in gallbladder cancer cells. In addition, triptolide induced apoptosis, as shown by the results of annexin V/propidium iodide double-staining and Hoechst 33342 staining. Furthermore, triptolide decreased mitochondrial membrane potential (ΔΨm) in a dose-dependent manner. Finally, western blot analysis of triptolide-treated cells revealed the activation of caspase-3, caspase-9, PARP, and Bcl-2; this result demonstrated that triptolide induced apoptosis in gallbladder cancer cells by regulating apoptosis-related protein expression, and suggests that triptolide may be a promising drug to treat gallbladder carcinoma. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Glycosylation of a Newly Functionalized Orthoester Derivative
Molecules 2014, 19(2), 2602-2611; https://doi.org/10.3390/molecules19022602
Received: 26 January 2014 / Revised: 20 February 2014 / Accepted: 21 February 2014 / Published: 24 February 2014
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Abstract
Tandem glycosylation of the 6-O-Fmoc-substituted benzyl orthoester derivative 2a was carried out in moderate yields by electrogenerated acid (EGA). The Fmoc group was effectively removed under mild basic conditions, and the product was submitted to the subsequent glycosylation. Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessArticle Inhibition of Human Cytochrome P450 Enzymes by Bacopa monnieri Standardized Extract and Constituents
Molecules 2014, 19(2), 2588-2601; https://doi.org/10.3390/molecules19022588
Received: 21 January 2014 / Revised: 19 February 2014 / Accepted: 19 February 2014 / Published: 24 February 2014
Cited by 15 | PDF Full-text (1637 KB) | HTML Full-text | XML Full-text
Abstract
Bacopa monnieri and the constituents of this plant, especially bacosides, possess various neuropharmacological properties. Like drugs, some herbal extracts and the constituents of their extracts alter cytochrome P450 (CYP) enzymes, causing potential herb-drug interactions. The effects of Bacopa monnieri standardized extract and the
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Bacopa monnieri and the constituents of this plant, especially bacosides, possess various neuropharmacological properties. Like drugs, some herbal extracts and the constituents of their extracts alter cytochrome P450 (CYP) enzymes, causing potential herb-drug interactions. The effects of Bacopa monnieri standardized extract and the bacosides from the extract on five major CYP isoforms in vitro were analyzed using a luminescent CYP recombinant human enzyme assay. B. monnieri extract exhibited non-competitive inhibition of CYP2C19 (IC50/Ki = 23.67/9.5 µg/mL), CYP2C9 (36.49/12.5 µg/mL), CYP1A2 (52.20/25.1 µg/mL); competitive inhibition of CYP3A4 (83.95/14.5 µg/mL) and weak inhibition of CYP2D6 (IC50 = 2061.50 µg/mL). However, the bacosides showed negligible inhibition of the same isoforms. B. monnieri, which is orally administered, has a higher concentration in the gut than the liver; therefore, this herb could exhibit stronger inhibition of intestinal CYPs than hepatic CYPs. At an estimated gut concentration of 600 µg/mL (based on a daily dosage of 300 mg/day), B. monnieri reduced the catalytic activities of CYP3A4, CYP2C9 and CYP2C19 to less than 10% compared to the total activity (without inhibitor = 100%). These findings suggest that B. monnieri extract could contribute to herb-drug interactions when orally co-administered with drugs metabolized by CYP1A2, CYP3A4, CYP2C9 and CYP2C19. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Synthetic Fosmidomycin Analogues with Altered Chelating Moieties Do Not Inhibit 1-Deoxy-D-xylulose 5-phosphate Reductoisomerase or Plasmodium falciparum Growth In Vitro
Molecules 2014, 19(2), 2571-2587; https://doi.org/10.3390/molecules19022571
Received: 6 February 2014 / Revised: 18 February 2014 / Accepted: 19 February 2014 / Published: 24 February 2014
Cited by 6 | PDF Full-text (387 KB) | HTML Full-text | XML Full-text
Abstract
Fourteen new fosmidomycin analogues with altered metal chelating groups were prepared and evaluated for inhibition of E. coli Dxr, M. tuberculosis Dxr and the growth of P. falciparum K1 in human erythrocytes. None of the synthesized compounds showed activity against either enzyme or
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Fourteen new fosmidomycin analogues with altered metal chelating groups were prepared and evaluated for inhibition of E. coli Dxr, M. tuberculosis Dxr and the growth of P. falciparum K1 in human erythrocytes. None of the synthesized compounds showed activity against either enzyme or the Plasmodia. This study further underlines the importance of the hydroxamate functionality and illustrates that identifying effective alternative bidentate ligands for this target enzyme is challenging. Full article
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Open AccessArticle Synthesis, Spectroscopic and Theoretical Studies of New Quasi-Podands from Bile Acid Derivatives Linked by 1,2,3-Triazole Rings
Molecules 2014, 19(2), 2557-2570; https://doi.org/10.3390/molecules19022557
Received: 17 December 2013 / Revised: 19 February 2014 / Accepted: 20 February 2014 / Published: 24 February 2014
Cited by 8 | PDF Full-text (467 KB) | HTML Full-text | XML Full-text
Abstract
A novel method for the synthesis of bile acid derivatives has been developed using “click chemistry”. Intermolecular 1,3-dipolar cycloaddition of the propargyl ester of bile acids and azide groups of 1,3,5-tris(azidomethyl)benzene gave a new quasi-podands with 1,2,3-triazole rings. The structures of the products
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A novel method for the synthesis of bile acid derivatives has been developed using “click chemistry”. Intermolecular 1,3-dipolar cycloaddition of the propargyl ester of bile acids and azide groups of 1,3,5-tris(azidomethyl)benzene gave a new quasi-podands with 1,2,3-triazole rings. The structures of the products were confirmed by spectral (1H-NMR, 13C-NMR, and FT-IR) analysis, mass spectrometry and PM5 semiempirical methods. Estimation of the pharmacotherapeutic potential has been accomplished for synthesized compounds on the basis of Prediction of Activity Spectra for Substances (PASS). Full article
(This article belongs to the Section Organic Chemistry)
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Open AccessArticle In Vivo and In Vitro Anti-Tumor Effects of Fungal Extracts
Molecules 2014, 19(2), 2546-2556; https://doi.org/10.3390/molecules19022546
Received: 7 January 2014 / Revised: 6 February 2014 / Accepted: 20 February 2014 / Published: 21 February 2014
Cited by 9 | PDF Full-text (714 KB) | HTML Full-text | XML Full-text
Abstract
Fungal extracts are extensively used as nutritional supplements in Far-Eastern Asia. In this study, we aimed to evaluate the anti-cancer activities of some different fungal species against different cancer cell lines. The water or ethanol extracts of Fomitopsis pinicola (F. pinicola),
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Fungal extracts are extensively used as nutritional supplements in Far-Eastern Asia. In this study, we aimed to evaluate the anti-cancer activities of some different fungal species against different cancer cell lines. The water or ethanol extracts of Fomitopsis pinicola (F. pinicola), Ganoderma sinense, Fomitopsis officinalis, Polyporus melanopus, and Taiwanofungus camphorates were used to evaluate the anti-cancer activities in various cancer cells. We found that all of the fungi ethanol extracts used in this study exert anti-cancer activities in vitro, whereas water extracts show lower inhibitory activities as determined by 3-(4,5-methylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays. Among the tested fungi species, F. pinicola ethanol extract exerts the most significant anti-cancer activity (growth inhibitory ratio 82.8%, p < 0.001) by increasing cell apoptosis. Moreover, F. pinicola ethanol extract significantly decreased tumor size (tumor growth inhibitory ratio 54%, p < 0.05) and increased the lifespan in mice bearing sarcoma-180 tumors. Taken together, this is the first study indicating the anti-tumor effect of F. pinicola in vivo and in vitro. F. pinicola ethanol extract induces cell apoptosis to exert a significant anti-tumor activity, with potential to be a new alternative anti-tumor medicine. Full article
(This article belongs to the Section Medicinal Chemistry)
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Open AccessCommunication Skullcap (Scutellaria baicalensis) Extract and Its Active Compound, Wogonin, Inhibit Ovalbumin-Induced Th2-Mediated Response
Molecules 2014, 19(2), 2536-2545; https://doi.org/10.3390/molecules19022536
Received: 3 January 2014 / Revised: 10 February 2014 / Accepted: 18 February 2014 / Published: 21 February 2014
Cited by 10 | PDF Full-text (499 KB) | HTML Full-text | XML Full-text
Abstract
Skullcap (Scutellaria baicalensis) has been widely used as a dietary ingredient and traditional herbal medicine owing to its anti-inflammatory and anticancer properties. In this study, we investigated the anti-allergic effects of skullcap and its active compounds, focusing on T cell-mediated responses ex
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Skullcap (Scutellaria baicalensis) has been widely used as a dietary ingredient and traditional herbal medicine owing to its anti-inflammatory and anticancer properties. In this study, we investigated the anti-allergic effects of skullcap and its active compounds, focusing on T cell-mediated responses ex vivo and in vivo. Splenocytes from mice sensitized with ovalbumin (OVA) were isolated for analyses of cytokine production and cell viability. Mice sensitized with OVA were orally administered skullcap or wogonin for 16 days, and then immunoglobulin (Ig) and cytokine levels were measured by enzyme-linked immunosorbent assays. Treatment with skullcap significantly inhibited interleukin (IL)-4 production without reduction of cell viability. Moreover, wogonin, but not baicalin and baicalein, suppressed IL-4 and interferon-gamma production. In vivo, skullcap and wogonin downregulated OVA-induced Th2 immune responses, especially IgE and IL-5 prediction. Wogonin as an active component of skullcap may be applied as a therapeutic agent for IgE- and IL-5-mediated allergic disorders. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessArticle Synthesis and Antiproliferative Activity of Some Novel Triazole Derivatives from Dehydroabietic Acid
Molecules 2014, 19(2), 2523-2535; https://doi.org/10.3390/molecules19022523
Received: 24 January 2014 / Revised: 18 February 2014 / Accepted: 18 February 2014 / Published: 21 February 2014
Cited by 17 | PDF Full-text (231 KB) | HTML Full-text | XML Full-text
Abstract
Dehydroabietic acid (DHA) is a naturally occurring diterpene with different and relevant biological activities. Previous studies have shown that some DHA derivatives display antiproliferative activity. However, the reported compounds did not include triazole derivatives. Starting from DHA (8,11,13-abietatrien-18-oic acid), and its alcohol dehydroabietinol
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Dehydroabietic acid (DHA) is a naturally occurring diterpene with different and relevant biological activities. Previous studies have shown that some DHA derivatives display antiproliferative activity. However, the reported compounds did not include triazole derivatives. Starting from DHA (8,11,13-abietatrien-18-oic acid), and its alcohol dehydroabietinol (8,11,13-abietatrien-18-ol), four alkyl esters were prepared. The alkyl terpenes were treated with different aromatic azides to synthesize hybrid compounds using click chemistry. Some 16 new DHA hybrids were thus synthesized and their structures were confirmed by spectroscopic and spectrometric means. The antiproliferative activity of the new compounds was assessed towards human cell lines, namely normal lung fibroblasts (MRC-5), gastric epithelial adenocarcinoma (AGS), lung cancer (SK-MES-1) and bladder carcinoma (J82) cells. Better antiproliferative effect was found for compound 5, with an IC50 of 6.1 μM and selectivity on SK-MES-1 cells. Under the same experimental conditions, the IC50 of etoposide, was 1.83 µM. Full article
(This article belongs to the Section Natural Products Chemistry)
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Open AccessReview Effects of Honey and Its Mechanisms of Action on the Development and Progression of Cancer
Molecules 2014, 19(2), 2497-2522; https://doi.org/10.3390/molecules19022497
Received: 28 November 2013 / Revised: 6 February 2014 / Accepted: 10 February 2014 / Published: 21 February 2014
Cited by 33 | PDF Full-text (517 KB) | HTML Full-text | XML Full-text
Abstract
Honey is a natural product known for its varied biological or pharmacological activities—ranging from anti-inflammatory, antioxidant, antibacterial, antihypertensive to hypoglycemic effects. This review article focuses on the role of honey in modulating the development and progression of tumors or cancers. It reviews available
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Honey is a natural product known for its varied biological or pharmacological activities—ranging from anti-inflammatory, antioxidant, antibacterial, antihypertensive to hypoglycemic effects. This review article focuses on the role of honey in modulating the development and progression of tumors or cancers. It reviews available evidence (some of which is very recent) with regards to the antimetastatic, antiproliferative and anticancer effects of honey in various forms of cancer. These effects of honey have been thoroughly investigated in certain cancers such as breast, liver and colorectal cancer cell lines. In contrast, limited but promising data are available for other forms of cancers including prostate, bladder, endometrial, kidney, skin, cervical, oral and bone cancer cells. The article also underscores the various possible mechanisms by which honey may inhibit growth and proliferation of tumors or cancers. These include regulation of cell cycle, activation of mitochondrial pathway, induction of mitochondrial outer membrane permeabilization, induction of apoptosis, modulation of oxidative stress, amelioration of inflammation, modulation of insulin signaling and inhibition of angiogenesis. Honey is highly cytotoxic against tumor or cancer cells while it is non-cytotoxic to normal cells. The data indicate that honey can inhibit carcinogenesis by modulating the molecular processes of initiation, promotion, and progression stages. Thus, it may serve as a potential and promising anticancer agent which warrants further experimental and clinical studies. Full article
(This article belongs to the Section Natural Products Chemistry)
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