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Pharmaceuticals, Volume 5, Issue 8 (August 2012), Pages 779-889

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Research

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Open AccessArticle The Chemical Components of Sesbania grandiflora Root and Their Antituberculosis Activity
Pharmaceuticals 2012, 5(8), 882-889; doi:10.3390/ph5080882
Received: 2 July 2012 / Revised: 24 July 2012 / Accepted: 3 August 2012 / Published: 23 August 2012
Cited by 7 | PDF Full-text (179 KB) | HTML Full-text | XML Full-text
Abstract
Three isoflavanoids, isovestitol (1), medicarpin (2), and sativan (3), along with another known compound, betulinic acid (4), were isolated from the root of Sesbania grandiflora. The structures of the isolated compounds were characterised by means of spectroscopic techniques (UV, IR, MS, 1
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Three isoflavanoids, isovestitol (1), medicarpin (2), and sativan (3), along with another known compound, betulinic acid (4), were isolated from the root of Sesbania grandiflora. The structures of the isolated compounds were characterised by means of spectroscopic techniques (UV, IR, MS, 1H- and 13C-NMR, DEPT, COSY, HMQC, HMBC, and MS analysis). All the tested compounds 1–4 exhibited antituberculosis activity against Mycobacterium tuberculosis H37Rv, with MIC values of 50 µg/mL for compounds 1–3, and 100 µg/mL for compound 4, whereas, the methanol extract exhibited antituberculosis activity of 625 µg/mL. This is the first report on the occurrence of isoflavonoids in this plant and their antituberculosis activity. Full article
(This article belongs to the Special Issue Antituberculosis Drugs)

Review

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Open AccessReview Heat Shock Protein 90 and Role of Its Chemical Inhibitors in Treatment of Hematologic Malignancies
Pharmaceuticals 2012, 5(8), 779-801; doi:10.3390/ph5080779
Received: 4 June 2012 / Revised: 9 July 2012 / Accepted: 16 July 2012 / Published: 25 July 2012
Cited by 5 | PDF Full-text (317 KB) | HTML Full-text | XML Full-text
Abstract
Heat shock protein 90 (Hsp90) is a conserved and constitutively expressed molecular chaperone and it has been shown to stabilize oncoproteins and facilitate cancer development. Hsp90 has been considered as a therapeutic target for cancers and three classes of Hsp90 inhibitors have been
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Heat shock protein 90 (Hsp90) is a conserved and constitutively expressed molecular chaperone and it has been shown to stabilize oncoproteins and facilitate cancer development. Hsp90 has been considered as a therapeutic target for cancers and three classes of Hsp90 inhibitors have been developed: (1) benzoquinone ansamycin and its derivatives, (2) radicicol and its derivates, and (3) small synthetic inhibitors. The roles of these inhibitors in cancer treatment have been studied in laboratories and clinical trials, and some encouraging results have been obtained. Interestingly, targeting of Hsp90 has been shown to be effective in inhibition of cancer stem cells responsible for leukemia initiation and progression, providing a strategy for finding a cure. Because cancer stem cells are well defined in some human leukemias, we will focus on hematologic malignancies in this review. Full article
(This article belongs to the Special Issue Hsp90 Inhibitors)
Open AccessReview Involvement of Multiple Transporters-mediated Transports in Mizoribine and Methotrexate Pharmacokinetics
Pharmaceuticals 2012, 5(8), 802-836; doi:10.3390/ph5080802
Received: 28 May 2012 / Revised: 25 July 2012 / Accepted: 7 August 2012 / Published: 10 August 2012
Cited by 3 | PDF Full-text (365 KB) | HTML Full-text | XML Full-text
Abstract
Mizoribine is administered orally and excreted into urine without being metabolized. Many research groups have reported a linear relationship between the dose and peak serum concentration, between the dose and AUC, and between AUC and cumulative urinary excretion of mizoribine. In contrast, a
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Mizoribine is administered orally and excreted into urine without being metabolized. Many research groups have reported a linear relationship between the dose and peak serum concentration, between the dose and AUC, and between AUC and cumulative urinary excretion of mizoribine. In contrast, a significant interindividual variability, with a small intraindividual variability, in oral bioavailability of mizoribine is also reported. The interindividual variability is mostly considered to be due to the polymophisms of transporter genes. Methotrexate (MTX) is administered orally and/or by parenteral routes, depending on the dose. Metabolic enzymes and multiple transporters are involved in the pharmacokinetics of MTX. The oral bioavailability of MTX exhibits a marked interindividual variability and saturation with increase in the dose of MTX, with a small intraindividual variability, where the contribution of gene polymophisms of transporters and enzymes is suggested. Therapeutic drug monitoring of both mizoribine and MTX is expected to improve their clinical efficacy in the treatment of rheumatoid arthritis. Full article
(This article belongs to the Special Issue Immunosuppressant Drugs)
Open AccessReview Role of Transient Receptor Potential Vanilloid 1 in Inflammation and Autoimmune Diseases
Pharmaceuticals 2012, 5(8), 837-852; doi:10.3390/ph5080837
Received: 29 June 2012 / Revised: 2 August 2012 / Accepted: 15 August 2012 / Published: 17 August 2012
Cited by 4 | PDF Full-text (140 KB) | HTML Full-text | XML Full-text
Abstract
Transient receptor potential vanilloid 1 (TRPV1), a non-selective cation channel, is a receptor activated by high temperatures and chemical agonists such as the vanilloids and protons. Because of these properties, TRPV1 has emerged as a polymodal nocisensor of nociceptive afferent neurons. TRPV1 is
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Transient receptor potential vanilloid 1 (TRPV1), a non-selective cation channel, is a receptor activated by high temperatures and chemical agonists such as the vanilloids and protons. Because of these properties, TRPV1 has emerged as a polymodal nocisensor of nociceptive afferent neurons. TRPV1 is thought to be a central transducer of hyperalgesia and a prime target for controlling pain pharmacologically because it is a point where many proalgesic pathways converge and it is upregulated and sensitized by inflammation and injury. However, whether TRPV1 agonists promote or inhibit inflammation remains unclear. We recently demonstrated that SA13353 (1-[2-(1-adamantyl)ethyl]-1-pentyl-3-[3-(4-pyridyl)propyl]urea), a novel TRPV1 agonist, inhibits tumor necrosis factor-a production by the activation of capsaicin-sensitive afferent neurons and reduces the severity of symptoms in kidney injury, lung inflammation, arthritis, and encephalomyelitis. These results suggest that TRPV1 agonists may act as anti-inflammatories in certain inflammatory and autoimmune conditions in vivo. Given the potential deleterious effects of inhibiting the population of channels with a protective function, caution should be taken in the use of potent TRPV1 antagonists as a general strategy to treat inflammation. Further studies are required to clarify the role of TRPV1 and neuropeptides, which are released because of TRPV1 activation in inflammation and autoimmune diseases. Full article
(This article belongs to the Special Issue Emerging Pain Targets and Therapy)
Open AccessReview Phytomedicine in Otorhinolaryngology and Pulmonology: Clinical Trials with Herbal Remedies
Pharmaceuticals 2012, 5(8), 853-874; doi:10.3390/ph5080853
Received: 5 July 2012 / Accepted: 8 August 2012 / Published: 20 August 2012
Cited by 2 | PDF Full-text (226 KB) | HTML Full-text | XML Full-text
Abstract
Phytomedicine has become an important alternative treatment option for patients in the Western world, as they seek to be treated in a holistic and natural way after an unsatisfactory response to conventional drugs. Ever since herbal remedies have been introduced in the Western
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Phytomedicine has become an important alternative treatment option for patients in the Western world, as they seek to be treated in a holistic and natural way after an unsatisfactory response to conventional drugs. Ever since herbal remedies have been introduced in the Western world, clinicians have raised concerns over their efficacy and possible side-effects. A PubMed (Medline) search was performed covering the last five years (01/07–04/12) and including 55 prospective clinical randomized control trials in the medical specialities Otorhinolaryngology and Pulmonology. In this review, we present evidence-based clinical data with herbal remedies and try to enlighten the question of efficacy and reliability of phytomedicine. Full article
(This article belongs to the Special Issue Phytomedicine)
Open AccessReview A Perspective on the Comparative Antileukemic Activity of 5-Aza-2′-deoxycytidine (Decitabine) and 5-Azacytidine (Vidaza)
Pharmaceuticals 2012, 5(8), 875-881; doi:10.3390/ph5080875
Received: 31 May 2012 / Revised: 16 August 2012 / Accepted: 17 August 2012 / Published: 21 August 2012
Cited by 3 | PDF Full-text (282 KB) | HTML Full-text | XML Full-text
Abstract
5-Aza-2′-deoxycytidine (5-AZA-CdR, decitabine, Dacogen®) and 5-azacytidine (5-AC, Vidaza®) are epigenetic agents that have been approved for the clinical treatment of the hematological malignancy myelodysplastic syndrome (MDS) and are currently under clinical evaluation for the treatment of acute myeloid leukemia (AML). Most investigators currently
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5-Aza-2′-deoxycytidine (5-AZA-CdR, decitabine, Dacogen®) and 5-azacytidine (5-AC, Vidaza®) are epigenetic agents that have been approved for the clinical treatment of the hematological malignancy myelodysplastic syndrome (MDS) and are currently under clinical evaluation for the treatment of acute myeloid leukemia (AML). Most investigators currently classify 5-AZA-CdR and 5-AC as inhibitors of DNA methylation, which can reactivate tumor suppressor genes silenced by this epigenetic event. Examination of the pharmacology of these analogues reveals important differences with respect to their molecular mechanism of action. The action of 5-AZA-CdR is due to its incorporation into DNA. 5-AC is a riboside analogue that is incorporated primarily into RNA. A small fraction of 5-AC is converted to its deoxyribose form by ribonucleotide reductase and subsequently incorporated into DNA. The incorporation of 5-AC into RNA can interfere with the biological function of RNA and result in an inhibition protein synthesis. Microarray analysis revealed that both these analogues target the expression of different cohorts of genes. Preclinical studies show that 5-AZA-CdR is a more effective antileukemic agent than 5-AC. One explanation for this observation is that 5-AC blocks the progression of some leukemic cells from G1 into S phase, and this protects these cells from the chemotherapeutic action of this riboside analogue related to its incorporation into DNA. However, differences in chemotherapeutic efficacy of these related analogues have not been clearly demonstrated in clinical trials in patients with hematological malignancies. These observations should be taken into consideration in the design of new clinical trials using 5-AZA-CdR or 5-AC in patients with MDS and AML. Full article
(This article belongs to the Special Issue Epigenetic Therapies and Biomarkers)

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