Title: Nanoparticles and targeted drug delivery in cancer therapy
Authors: Bahrami, B (Bahrami, Behdokht); Hojjat-Farsangi, M (Hojjat-Farsangi, Mohammad); Mohammadi, H (Mohammadi, Hamed); Anvari, E (Anvari, Enayat); Ghalamfarsa, G (Ghalamfarsa, Ghasem); Yousefi, M (Yousefi, Mehdi); Jadidi-Niaragh, F (Jadidi-Niaragh, Farhad)
Surgery, chemotherapy, radiotherapy, and hormone therapy are the main common anti-tumor therapeutic approaches. However, the non-specific targeting of cancer cells has made these approaches non-effective in the significant number of patients. Non-specific targeting of malignant cells also makes indispensable the application of the higher doses of drugs to reach the tumor region. Therefore, there are two main barriers in the way to reach the tumor area with maximum efficacy. The first, inhibition of drug delivery to healthy non-cancer cells and the second, the direct conduction of drugs into tumor site. Nanoparticles (NPs) are the new identified tools by which we can deliver drugs into tumor cells with minimum drug leakage into normal cells. Conjugation of NPs with ligands of cancer specific tumor biomarkers is a potent therapeutic approach to treat cancer diseases with the high efficacy. It has been shown that conjugation of nanocarriers with molecules such as antibodies and their variable fragments, peptides, nucleic aptamers, vitamins, and carbohydrates can lead to effective targeted drug delivery to cancer cells and thereby cancer attenuation. In this review, we will discuss on the efficacy of the different targeting approaches used for targeted drug delivery to malignant cells by NPs.
Title: Docking study, synthesis and antimicrobial evaluation of some novel 4-anilinoquinazoline derivatives
Authors: Nasab, RR (Nasab, Rezvan Rezaee); Hassanzadeh, F (Hassanzadeh, Farshid); Khodarahmi, GA (Khodarahmi, Ghadam Ali); Rostami, M (Rostami, Mahboubeh); Mirzaei, M (Mirzaei, Mahmoud); Jahanian-Najafabadi, A (Jahanian-Najafabadi, Ali); Mansourian, M (Mansourian, Mahboubeh)
A series of novel 4-anilinoquinazoline derivatives were designed and synthesized from benzoic acid through ring closure, chlorination or nucleophilic substitution. The structures of compounds were characterized by IR, H-1-NMR and mass spectroscopy. All synthesized derivatives were screened for their antimicrobial activities against Gram-positive (Staphylococcus aurous, Bacillus subtilis, Listeria monocitogenes) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa, Salmonella entritidis) bacteria and also for antifungal activities against Candida albicans using the conventional micro dilution method. Most of the compounds have shown good antibacterial activities, especially compound 4c having highest activities against E. coli at 32 mu g/mL concentration while the tested compounds did not exhibited remarkable antifungal activities. The potential DNA gyrase inhibitory activity of these compounds was investigated in silico using molecular docking simulation method. All compounds showed good results especially compound 4c which showed the lowest Delta G(bind) results (-8.16 Kcal/mol).
Title: Hepatoprotective effect of Stachys pilifera ethanol extract in carbon tetrachloride-induce hepatotoxicity in rats
Authors: Kokhdan, EP (Kokhdan, Esmaeel Panahi); Ahmadi, K (Ahmadi, Kyomarth); Sadeghi, H (Sadeghi, Heibatollah); Sadeghi, H (Sadeghi, Hossein); Dadgary, F (Dadgary, Fahemeh); Danaei, N (Danaei, Nazanin); Aghamaali, MR (Aghamaali, Mahmoud Reza)
Context: Stachys pilifera Benth (Lamiaceae) has long been used to treat infectious diseases, respiratory and rheumatoid disorders in Iranian folk medicine. Antitumor and antioxidant activity of the plant have been reported.
Objective: The study was designed to assess the hepatoprotective activity of ethanol extract of Stachys pilifera in carbon tetrachloride (CCl4)-induced hepatotoxicity in rats.
Materials and methods: The rats were randomly divided into six equal groups (n = 7). Group I was treated with normal saline; Group II received CCl4 (1 mL/kg. i. p., twice a week) for 60 consecutive days; Groups III, IV and V were given CCl4 plus Stachys pilifera (100, 200 and 400 mg/kg/d, p. o.); Group VI received the extract (400 mg/kg/d, p.o.). Histopathological analysis and measurement of serum aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), malondialdehyde (MDA), total protein (TP) and albumin (ALB) were performed.
Results: CCl4 caused a significant increase in the serum levels of AST, ALT, ALP and MDA as well as decreased ALB, and TP serum levels (p<0.001). The extract (200 and 400 mg/kg/d) significantly normalized the CCl4-elevated levels of ALT, AST, ALP and MDA (p<0.001). The extract (200 and 400mg/kg/d) also increased the serum levels of TP compared to CCl4 group (p<0.01). The extract (200 and 400mg/kg/d) also decreased the histological injuries (inflammation and fatty degeneration) by CCl4.
Discussion: The results revealed that the Stachys pilifera extract could provide considerable protection against CCl4 hepatotoxicity in rats that may be related to its antioxidant properties.
Title: Pramipexole reduces inflammation in the experimental animal models of inflammation
Authors: Sadeghi, H (Sadeghi, Heibatollah); Parishani, M (Parishani, Mohammad); Touri, MA (Touri, Mehdi Akbartabar); Ghavamzadeh, M (Ghavamzadeh, Mehdi); Barmak, MJ (Barmak, Mehrzad Jafari); Zarezade, V (Zarezade, Vahid); Delaviz, H (Delaviz, Hamdollah); Sadeghi, H (Sadeghi, Hossein)
Pramipexole is a dopamine (DA) agonist (D2 subfamily receptors) that widely use in the treatment of Parkinson's diseases. Some epidemiological and genetic studies propose a role of inflammation in the pathophysiology of Parkinson's disease. To our knowledge, there is no study regarding the anti-inflammatory activity of pramipexol. Therefore, the aim of the study was to investigate antiinflammatory effect of pramipexol. Anti-inflammatory effects of pramipexole were studied in three well-characterized animal models of inflammation, including carrageenan-or formalin-induced paw inflammation in rats, and 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced ear edema in mice. The animals received pramipexol (0.25, 0.5 and 1mg/kg, I.P.) 30 min before subplantar injection of carrageenan or formalin. Pramipexol (0.5 and 1 mg/kg) was also injected 30 min before topical application of TPA on the ear mice. Serum malondialdehyde (MDA) levels were evaluated in the carrageenan test. Finally, pathological examination of the inflamed tissues was carried out. Pramipexole significantly inhibited paw inflammation 1, 2, 3 and 4 h after carrageenan challenge compared with the control group (p <. 001). Pramipexol also showed considerable anti-inflammatory activity against formalin-evoked paw edema over a period of 24 h (p <. 001). TPA-induced ear edema was markedly decreased by pramipexol (p <. 001). The pathological evaluation of the paws and ears revealed that pramipexole reduced tissue injury, neutrophil infiltration, and subcutaneous edema. Pramipexole did not alter the increased serum levels of MDA due to carrageenan injection. These data clearly indicate that pramipexol possesses significant anti-inflammatory activity. It seems that its antioxidants do not play an important role in these effects.
Title: Preconcentration of carbamate insecticides in water samples by using modified stir bar with ZnS nanoparticles loaded on activated carbon and their HPLC determination: Response surface methodology
Authors: Talebianpoor, MS (Talebianpoor, Mohammad Sharif); Khodadoust, S (Khodadoust, Saeid); Mousavi, A (Mousavi, Abdmohammad); Mahmoudi, R (Mahmoudi, Reza); Nikbakht, J (Nikbakht, Jafar); Mohammadi, J (Mohammadi, Jamshid)
In this paper, a zinc sulphide nanoparticles loaded on activated carbon (AC) (ZnS-AC) as well as 1-ethyl-3-methylimidazolium hexafluorophosphate ([EMIK[PF6]) ionic liquid using sol gel technique was used as the adsorbent for the stir bar sorptive extraction (SBSE) of N-methylcarbamates (NMCs) (carbofuran, carbaryl and promecarb) in water samples followed by high performance liquid chromatography-ultraviolet detection (HPLC-UV). The fractional factorial design (FFD) was used to find the most important factors, which were then optimized by the central composite design (CCD) and response surface methodology (RSM). At optimum conditions values of factors set as 2.75% (w/v) NaCl, 23 min extraction time, 300 mu L methanol (as desorption solvent), natural pH, and 500 rpm stirring speed. Under the optimal experimental conditions, the proposed method has linear ranges over 0.002-30 g mL(-1) with detection limit 0.0003-0.0005 mu g mL(-1) and good RSD5 (and n = 6) of 3.3-4.5% for NMCs. The dgveloped method has been successfully applied to the determination of three NMCs in environmental water samples such as tap water, river water, and mineral water.