Anticancer Potential of a Synthetic Quinoline, 9IV-c, by Inducing Apoptosis in A549 Cell and BALB/c Mice Models.

Background: In a previous work from the author of this study, the compound of 9IV-c, ((E)-2-(3,4- dimethoxystyryl)-6,7,8-trimethoxy-N-(3,4,5-trimethoxyphenyl)quinoline-4-amine) was synthesized, and the effects of potent activity on the multiple human tumor cell lines were evaluated considering the spindle formation together with the microtubule network.

Methods: Accordingly, cytotoxic activity, apoptotic effects, and the therapeutic efficiency of compound 9IV-c on A549 and C26 cell lines were investigated in this study.

Results: The compound 9IV-c demonstrated high cytotoxicity against A549 and C26 cell lines with IC = 1.

Carnosic acid mitigates doxorubicin-induced cardiac toxicity: Evidence from animal and cell model investigations.

Objectives: Utilization of doxorubicin (DOX) as a chemotherapy medication is limited due to its cardiotoxic effects. Carnosic acid exerts antioxidant, anti-inflammatory, besides cytoprotective effects. The objective of this study was to investigate the ability of carnosic acid to protect rat hearts and the MCF7 cell line against cardiotoxicity induced by DOX.

Alpha-mangostin decreases high glucose-induced damage on human umbilical vein endothelial cells by increasing autophagic protein expression.

Objectives: Diabetes is a chronic disorder that occurs as a result of impaired glucose metabolism. In hyperglycaemic states, the balance between oxidative stress and antioxidant enzymes is disrupted leading to oxidative damage and cell death. In addition, impaired autophagy leads to the storage of dysfunctional proteins and cellular organelles in the cell.

Evaluating the effect of alpha-mangostin on neural toxicity induced by acrylamide in rats.

Acrylamide (ACR) is known to be a neurotoxic agent for humans and animals that has many applications in industry. Alpha-mangostin is a natural antioxidant that is extracted from mangosteen. This study aimed to investigate the protective effects of alpha-mangostin against ACR-induced neurotoxicity in rats and PC12 cells.

Preparation and Evaluation of the Gel-forming Chitosan Hydrogels for Nasal Delivery of Morphine in a Single Unit dose in Rats to Enhance the Analgesic Responses.

Introduction: In this study, an gel-forming chitosan hydrogel was prepared with the use of glutamate salt of chitosan (Ch-Ga), β-glycerophosphate (Gp), and morphine (Mor). The paper is focused on physicochemical properties and analgesic effects of the prepared chitosan hydrogel.

Method: The thermosensitive properties of prepared chitosan hydrogel were evaluated during the different temperatures and times.

In-vitro and in-vivo evaluation of sustained-release buprenorphine using in-situ forming lipid-liquid crystal gels.

Aims: Sustained-release systems reduce the incidence of drug side effects and the need for frequent drug consumption, thus increasing patient compliance with treatment. In this study, we aimed to produce sustained-release buprenorphine (BP) using lipid-liquid crystal gels.

Main Methods: The three experimental groups in this study included: group I: lipid-liquid crystal formulation 5 (F5) containing BP, group II: BP-free F5, group III: BP solution in NMP, and group IV: control (no treatment).

Lipid-liquid crystals for 2 months controlled risperidone release: In-vitro evaluation and pharmacokinetics in rabbits.

In this study, a drug delivery system based on lipid liquid crystal (LLC) was developed for the long-term delivery of risperidone to improve psychological treatment. Optimal LLC formulation was achieved based on maximum release after 60 days with different ratios of phosphatidylcholine (PC) to sorbitol monooleate (PC: SMO), tween grade 80 (w/w %), and tocopherol acetate (TA) (w/w %) using the Box-Behnken method. In vitro and ex vivo studies, pharmacokinetics, and histopathological examination in rabbits were conducted to compare the optimal LLC with Risperdal CONSTA®.

Cardioprotective effects of alpha-mangostin on doxorubicin-induced cardiotoxicity in rats.

The main adverse effect of doxorubicin is cardiotoxicity. Oxidative stress and apoptosis induction have been suggested as mechanisms involved in its cardiotoxicity. In this study, cardioprotective effects of alpha-mangostin against doxorubicin-induced cardiotoxicity have been investigated in rats.

Comparison of lipid liquid crystal formulation and Vivitrol® for sustained release of Naltrexone: In vitro evaluation and pharmacokinetics in rats.

Camurus' FluidCrystal® injection depot is a lipid liquid crystal (LLC) phase formation-based method, comprising of glycerol dioleate (GDO) and soy phosphatidylcholine (SPC), together with minute quantities of N-methyl-2-pyrrolidone solvent (NMP). The present study aimed to develop a method for LLC using sorbitan monooleate (LLC-SMO) instead of GDO to prepare a one-month sustained-release formulation of naltrexone (NTX) that is applied for the treatment of autism and treating alcohol dependence. The optical characteristics of the LLC were assessed by polarizing light microscopy (PLM) to reveal the presence of lamellar, hexagonal, and cubic mesophases.

Quercetin and its role in modulating endoplasmic reticulum stress: A review.

The endoplasmic reticulum (ER) is the place where proteins and lipids are biosynthesized and where transmembrane proteins are folded. Both pathological and physiological situations may disturb the function of the ER, resulting in ER stress. Under stress conditions, the cells initiate a defensive procedure known as the unfolded protein response (UPR).

In Vivo and In Vitro Protective Effects of Rosmarinic Acid against Doxorubicin-Induced Cardiotoxicity.

Doxorubicin (DOX) is an anticancer medicine that may trigger cardiomyopathy. Rosmarinic acid (RA) has shown antioxidant, anti-inflammatory, and anticancer effects. This investigation assessed the cardioprotective effect of RA on DOX-induced-toxicity in both in vivo and in vitro experiments.

Design, synthesis and biological evaluation of novel imidazole-chalcone derivatives as potential anticancer agents and tubulin polymerization inhibitors.

Novel imidazole-chalcone derivatives were designed and synthesized as tubulin polymerization inhibitors and anticancer agents. The antiproliferative activity of the imidazole-chalcone was assessed on some human cancer cell lines including A549 (adenocarcinoma human alveolar basal epithelial cells), MCF-7 (human breast cancer cells), MCF-7/MX (mitoxantrone resistant human breast cancer cells), and HEPG2 (human hepatocellular carcinoma cells). Generally, the imidazole-chalcone derivatives exhibited more cytotoxicity on A549 cancer cells in comparison to the other three cell lines, among them compounds 9j' and 9g showed significant cytotoxicity with IC values ranging from 7.

Design and synthesis of new carbamates as inhibitors for fatty acid amide hydrolase and cholinesterases: Molecular dynamic, in vitro and in vivo studies.

As anandamide (N-arachidonoylethanolamine, AEA) shows neuroprotective effects, the inhibition of its degradative enzyme, fatty acid amide hydrolase (FAAH) has been considered as a hopeful avenue for the treatment of neurodegenerative diseases, like Alzheimer's disease (AD). Memory loss, cognitive impairment and diminution of the cholinergic tone, due to the dying cholinergic neurons in the basal forebrain, are common hallmarks in patients with AD. By taking advantage of cholinesterase inhibitors (ChEIs), the degradation of acetylcholine (ACh) is decreased leading to enhanced cholinergic neurotransmission in the aforementioned region and ultimately improves the clinical condition of AD patients.

Design, synthesis, and biological evaluation of novel 5,6,7-trimethoxy quinolines as potential anticancer agents and tubulin polymerization inhibitors.

Objectives: Microtubules have key roles in essential cellular processes such as mitosis, cell motion, and intracellular organelle transport. Increasing interest has been given to tubulin binding compounds after the introduction of taxanes into clinical oncology. The object of this study was synthesis and biological evaluation of novel 5,6,7-trimethoxy quinolines as tubulin inhibitors.

Effect of carnosic acid on acrylamide induced neurotoxicity: and experiments.

Acrylamide (ACR), one of the most toxic chemical agents in humans and animals has several uses in different industries. Carnosic acid is an important biological antioxidant extracted from rosemary. In this study, the protective effect of carnosic acid on ACR-induced neurotoxicity in rat and PC12 cells has been investigated.

Injectable In-Situ Forming Depot of Doxycycline Hyclate/α-Cyclodextrin Complex Using PLGA for Periodontitis Treatment: Preparation, Characterization, and In-Vitro Evaluation.

Background: Doxycycline (DOX) is used in treating a bacterial infection, especially for periodontitis treatment.

Objective: To reduce irritation of DOX for subgingival administration and increase the chemical stability and against enzymatic, the complex of α-cyclodextrin with DOX was prepared and loaded into injectable in situ forming implant based on PLGA.

Methods: FTIR, molecular docking studies, X-ray diffraction, and differential scanning calorimetry was performed to characterize the DOX/α-cyclodextrin complex.

Combination therapy using Smac peptide and doxorubicin-encapsulated MUC 1-targeted polymeric nanoparticles to sensitize cancer cells to chemotherapy: An in vitro and in vivo study.

Targeting inhibitors of apoptosis proteins (IAPs) family comprising high level expression in many cancer cells, could sensitize tumor cells to conventional chemotherapies. In the present study, we designed both doxorubicin and SmacN6 (an antagonist of the IAPs) encapsulated polymeric nanoparticles (NPs) and investigated their synergistic effect of combination therapy in vitro and in vivo. According to the results, NPs-SmacN6 significantly enhanced the cytotoxicity effect of NPs-DOX and reduced its IC in MCF-7, 4T1 and C26 cancer cells.

Anticancer Potential of Aguerin B, a Sesquiterpene Lactone Isolated from in Metastatic Breast Cancer Cells.

Background: Breast carcinoma is a malignant disease that represents the most common non-skin malignancy and a chief reason of cancer death in women. Large interest is growing in the use of natural products for cancer treatment, especially with goal of suppression angiogenesis, tumor cell growth, motility, as well as invasion and metastasis with low/no toxicity. It is evident from recent patents on the anticancer properties of sesquiterpene lactones such as parthenolide.

Design, synthesis and biological evaluation of novel 5,6,7-trimethoxy-N-aryl-2-styrylquinolin-4-amines as potential anticancer agents and tubulin polymerization inhibitors.

A new series of styrylquinolines was designed and synthesized as anticancer agents and tubulin polymerization inhibitors. The in vitro anticancer activity of the synthesized quinolines was evaluated against four human cancer cell lines including A-2780 (human ovarian carcinoma), A-2780/RCIS (cisplatin resistant human ovarian carcinoma), MCF-7 (human breast cancer cells), MCF-7/MX (mitoxantrone resistant human breast cancer cells) and normal Huvec cells. Generally, among the forty-eight newly synthesized quinolines, compounds possessing N-trimethoxy phenyl showed stronger cytotoxic activity with IC values ranging from 0.

The effects of Ginkgo biloba on metabolic syndrome: A review.

The Ginkgo biloba (G. biloba), commonly known as ginkgo, brings considerable benefit to common medicine, including weight loss effects, as well as antidiabetic, antihypertensive, and antilipidemic properties that could be effective in the treatment of Metabolic syndrome (MetS) associated with increased risk of cardiovascular disease events. Major compounds of G.

Effects of curcumin on ion channels and pumps: A review.

Curcumin, an orange-yellow lipophilic polyphenolic molecule, is the active component of Curcuma longa, which is extensively used as a spice in most of the Asian countries. This natural compound is able to interact with a large number of molecular structures like proteins, enzymes, lipids, DNA, RNA, transporter molecules, and ion channels. It has been reported to possess several biological effects such as antioxidant, anti-inflammatory, wound healing, antimicrobial, anticancer, antiangiogenic, antimutagenic, and antiplatelet aggregation properties.