RGD Peptide ‐Based Target Drug Delivery of Doxorubicin Nanomedicine
ABSTRACT
Doxorubicin (DOX) is commonly used for the treatment of breast cancer and lymphoma. However, its clinical use has been severely limited due to cardiotoxicity, requiring the development of safer and more efficient pharmaceutical formulations of DOX. Advances in nanotechnology have provided new ways to administer chemotherapeutic drugs like DOX are conveyed into the body and to tumor sites. These Nanotechnology approaches have aided in the selective accumulation of DOX into tumor sites via the enhanced permeability and retention. However, the absence of active targeting ligands still hinders the effective del...
Source: Drug Development Research - August 16, 2017 Category: Drugs & Pharmacology Authors: Yuan Sun, Chen Kang, Fei Liu, You Zhou, Lei Luo, Hongzhi Qiao Tags: Research Overview Source Type: research
Issue Information ȃ TOC
(Source: Drug Development Research)
Source: Drug Development Research - August 14, 2017 Category: Drugs & Pharmacology Tags: Issue Information ȃ TOC Source Type: research
Recent Advances in GLP ‐1 Receptor Agonists for Use in Diabetes Mellitus
ABSTRACT
Mimetics of Glucagon‐like peptide 1 (GLP‐1) represent a useful alternative or complementary treatment choice to insulin in the treatment of diabetes mellitus. The lack of hypoglycemia as a side effect when GLP‐1 receptor agonists are used along with the tendency of these therapeutic agents to prevent or even reduce weight gain makes them valuable targets in therapy development. However, native GLP‐1 and many of its early analogues have very short half‐lives, requiring repeated treatment to maintain therapeutic levels. As all current treatments are injected subcutaneously, a large focus has been ma...
Source: Drug Development Research - August 8, 2017 Category: Drugs & Pharmacology Authors: Dominic N. McBrayer, Yftah Tal ‐Gan Tags: Research Overview Source Type: research
Supra ‐Additive Interaction of Docosahexaenoic Acid and Naproxen and Gastric Safety on the Formalin Test in Rats
ABSTRACT
The aim of this work was to evaluate the effect of docosahexaenoic acid (DHA) on the pharmacokinetics and pharmacodynamics—nociception—of naproxen in rats, as well as to determine the gastric safety resulting from this combination versus naproxen alone. Female Wistar rats were orally administered DHA, naproxen or the DHA‐naproxen mixture at fixed‐ratio combination of 1:3. The antinociceptive effect was evaluated using the formalin test. The gastric injury was determined 3 h after naproxen administration. An isobolographic analysis was performed to characterize the antinociceptive interaction between...
Source: Drug Development Research - August 3, 2017 Category: Drugs & Pharmacology Authors: Arlette Guadalupe Arroyo ‐Lira, Fernando Rodríguez‐Ramos, Mario I. Ortiz, Gilberto Castañeda‐Hernández, Aracely Evangelina Chávez‐Piña Tags: Research Article Source Type: research
Limiting Assumptions in the Design of Peptidomimetics
ABSTRACT
Limiting the flexibility of organic compounds to enhance their affinity and selectivity for targeting a macromolecule involved in molecular recognition has become a well‐developed paradigm in medicinal chemistry. While the role of reverse‐turn motifs as peptidomimetics has received the most attention, β‐sheets and helices are also important motifs for protein/protein interactions. The more complicated problem of mimicking the interacting surface of noncontiguous epitopes will not be considered in this review. This limited overview focuses on efforts to use amino acid synthons as secondary‐structure...
Source: Drug Development Research - August 1, 2017 Category: Drugs & Pharmacology Authors: Garland R. Marshall, Flavio Ballante Tags: Research Overview Source Type: research
Ultra ‐Low Doses of Naltrexone Enhance the Antiallodynic Effect of Pregabalin or Gabapentin in Neuropathic Rats
The objective of the present study was to assess the antiallodynic synergistic interaction between gabapentinoids and naltrexone in rats. Oral administration of pregabalin (ED50 = 2.79 ± 0.16 mg/kg) or gabapentin (ED50 = 21.04 ± 2.87 mg/kg) as well as intrathecal naltrexone (ED50 = 0.11 ± 0.02 ng) reduced in a dose‐dependent manner tactile allodynia in rats. Maximal antiallodynic effects (∼100%) were reached with 30 mg/kg of pregabalin, 300 mg/kg of gabapentin or 0.5 ng of naltrexone. Co‐administration of pregabalin or gabapentin and naltrexone in a fixed‐dose ratio (1:1) remarkably reduc...
Source: Drug Development Research - August 1, 2017 Category: Drugs & Pharmacology Authors: Jorge B. Pineda ‐Farias, Nadia L. Caram‐Salas, Ana B. Salinas‐Abarca, Jorge Ocampo, Vinicio Granados‐Soto Tags: Research Article Source Type: research
Peptide Mimetics: Fast ‐Forward Look
(Source: Drug Development Research)
Source: Drug Development Research - August 1, 2017 Category: Drugs & Pharmacology Authors: David Gurwitz Tags: Editorial Source Type: research
Peptide Mimetic Drugs for Modulating Thrombosis and Hemostasis
ABSTRACT
Hemostasis is the complex physiological process that stems bleeding at an injury site while simultaneously maintaining unobstructed circulation in other areas of the body. This system is kept in balance with finely tuned regulation by pro‐ and antithrombotic agents. When this balance is thrown out of equilibrium, uncontrolled bleeding, or thrombotic complications can occur. Because of the high number of hemostatic disorders, researchers are continually searching for improved technologies for controlling coagulation. Recently, peptide mimetic strategies have been employed to target and regulate various sta...
Source: Drug Development Research - August 1, 2017 Category: Drugs & Pharmacology Authors: Kimberly Nellenbach, Ashley C. Brown Tags: Research Overview Source Type: research
The Neurotensin NTS1 Receptor Agonist PD149163 Produces Antidepressant ‐Like Effects in the Forced Swim Test: Further Support for Neurotensin as a Novel Pharmacologic Strategy for Antidepressant Drugs
ABSTRACT
Neurotensin is a nonbrain penetrant neuropeptide neurotransmitter that alters dopaminergic and serotonergic neurotransmission. Previous animal behavioral studies have demonstrated that intra‐ventral tegmental administration of neurotensin and system administration of the selective neurotensin NTS1 receptor agonist, PD149163 produce antidepressant‐like effects in a forced swim test and a differential reinforcement of low rate task, respectively. The present study sought to expand upon these past findings by assessing systemic administration of PD149163 in a forced swim test, a primary antidepressant prec...
Source: Drug Development Research - July 24, 2017 Category: Drugs & Pharmacology Authors: Lawrence M. Carey, Remington J. Rice, Adam J. Prus Tags: Research Article Source Type: research
Phytochemical Investigation, Antitumor Activity, and Hepatoprotective Effects of Acrocarpus fraxinifolius Leaf Extract
ABSTRACT
Nine known phenolic compounds were isolated from an aqueous methanolic extract of Acrocarpus fraxinifolius Weight and Arn leaves (AFL) family Fabaceae. This extract of AFL contained approximately 169 mg gallic acid/g as assessed by HPLC. The AFL extract had marginal antitumor activity (IC50 > 200 µL/mL) but showed a concentration‐dependent hepatoprotective effect against CCl4‐induced hepatotoxicity in vitro. Cell viability was increased, ALT and AST activity declined and reduced GSH concentration and SOD activity were restored as compared with silymarin. In vivo concurrent administration of AFL ...
Source: Drug Development Research - July 24, 2017 Category: Drugs & Pharmacology Authors: Heba A. S. El ‐Nashar, Omayma A. Eldahshan, Omama E. Elshawi, Abdel Nasser B. Singab Tags: Research Article Source Type: research
Synergism between Naproxen and Rutin in a Mouse Model of Visceral Pain
ABSTRACT
The aim of the present study was to evaluate the antinociceptive interaction between naproxen and the glycoside flavonoid, rutin in the acetic acid‐induced writhing test in mice. Naproxen (5, 20, 50, and 100 mg/kg p.o.) or rutin (10, 25, 50, and 100mg/kg p.o.) were administered 60 min before the intraperitoneal administration with acetic acid. The dose‐response curve of each individual compound and the experimental effective dose 50 (ED50) value were obtained to determinate different proportions of the combinations between the two compounds (naproxen‐rutin 1:1, 3:1, and 3:1) in the writhing test. The ...
Source: Drug Development Research - June 22, 2017 Category: Drugs & Pharmacology Authors: Angel Josabad Alonso ‐Castro, Joceline Estefanía Rangel‐Velázquez, Mario A. Isiordia‐Espinoza, Luis Enrique Villanueva‐Solís, Othoniel H. Aragon‐Martinez, Juan Ramón Zapata‐Morales Tags: Research Article Source Type: research
Antiestrogenic Activity of Triptolide in Human Breast Cancer Cells MCF ‐7 and Immature Female Mouse
ABSTRACT
To investigate the antiestrogenic activity of triptolide in human breast cancer cell line MCF‐7 and immature female C57BL/6 mouse. The effects of triptolide on cell proliferation, cell cycle, and the expression of estrogen receptor alpha (ERα) and progesterone receptor (PR) were examined in MCF‐7 cells. In vivo antiestrogenic effects of triptolide were observed after cotreatment of mice with E2 and triptolide for 4 days. Triptolide dose‐ and time‐dependently inhibited cell growth in untreated or E2‐treated MCF‐7 cells, which was associated with increased S phase arrest. Furthermore, triptolide ...
Source: Drug Development Research - June 12, 2017 Category: Drugs & Pharmacology Authors: Yi Tang, Jun Wang, Jinghua Cheng, Lijun Wang Tags: Research Article Source Type: research
Toxicity and Protective Effect of Phenolic ‐Enriched Ethylacetate Fraction of Ocimum gratissimum (Linn.) Leaf against Acute Inflammation and Oxidative Stress in Rats
ABSTRACT
Ocimum gratissimum L. leaves have attracted considerable attention from researchers because of their medicinal value that include anti‐inflammatory, analgesic, antimicrobial, and antioxidant activities. In the present study, the toxicity and the protective effect of phenolic extract of O. gratissimum leaf (EAFOg) against acute inflammation and oxidative stress in rats was assessed. EAFOg, enriched in phenols had no cytotoxic effect against CHO‐k1 cells, and no lethality against brine shrimp eggs or mice at a dose of 2000 mg/kg. EAFOg (50 and 100 mg/kg) reduced paw edema by 47% and 61%, compared to 29% w...
Source: Drug Development Research - June 12, 2017 Category: Drugs & Pharmacology Authors: Abayomi M. Ajayi, Solomon Umukoro, Benneth Ben ‐Azu, Bulus Adzu, Olusegun G. Ademowo Tags: Research Article Source Type: research
Issue Information – TOC
(Source: Drug Development Research)
Source: Drug Development Research - June 12, 2017 Category: Drugs & Pharmacology Tags: Issue Information – TOC Source Type: research
On BH3 Mimetics and Ca2+ Signaling
ABSTRACT
BH3 mimetics are anticancer agents that reproduce the spatial arrangement of the BH3 domain of Bcl‐2 family proteins. Just like the BH3‐only proteins, these compounds bind to the hydrophobic cleft of the pro‐survival Bcl‐2 members such as Bcl‐2 or Bcl‐xL, and disrupt their heterodimerization with pro‐apoptotic Bax or Bak, sensitizing cells to chemotherapy. In recent years, it has become clear that Bcl‐2 family proteins are engaged in regulation of intracellular Ca2+ homeostasis, including Ca2+ release from the intracellular stores as well as Ca2+ fluxes across the plasma membrane. Given that...
Source: Drug Development Research - June 1, 2017 Category: Drugs & Pharmacology Authors: Pawel E. Ferdek, Monika A. Jakubowska Tags: Research Commentary Source Type: research
