Iranian Journal of Pharmaceutical Research
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In Collaboration with School of Pharmacy, SBMU
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The IJ Pharmaceutical Research (IJPR) is a peer-reviewed multi-disciplinary pharmaceutical publication, scheduled to appear annually and serve as a means for scientific information exchange in the international pharmaceutical forum. Specific scientific topics of interest to the journal include but are not limited to: pharmaceutics, industrial pharmacy, pharmacognosy, toxicology, medicinal chemistry, novel analytical methods for drug characterization, computational and modeling approaches to drug design, bio-medical experience, clinical investigation, rational drug prescribing, pharmacoeconomics, biotechnology, nanotechnology, biopharmaceuticals, and physical pharmacy.
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- ItemCombinatorial Effects of Chrysin with Doxorubicin, 5-Fluorouracil, and Cyclophosphamide on Triple-Negative Breast Cancer Cell Line(Brieflands, 2025-12-31) Sedighe Yosefi; Hamid Madanchi; Abbas Pakdel; Parviz Kokhaei; Maral Hemati; Negar Sarmadi; Majid Sirati-SabetBackground: The primary challenges associated with chemotherapy treatment include the development of drug resistance. Chrysin (CH) has the potential to enhance the therapeutic efficacy of conventional chemotherapeutic agents. Additionally, CH, with its antioxidant properties, can reduce the side effects caused by reactive oxygen species (ROS) from chemotherapy. Objectives: This study focused on investigating the combination impact of CH with either 5-fluorouracil (5-FU), doxorubicin (DOX), or cyclophosphamide (CP) on the triple-negative breast cancer (TNBC) MDA-MB-231 cell line. Methods: Cytotoxicity was investigated using the MTT assay. The checkerboard microplate method was utilized to determine the effects of drug interactions. Apoptosis and cell cycle distribution were measured by flow cytometry. The classical scratch assay was used to examine cell migration ability. Results: The combination of 5-FU and DOX showed synergistic effects with CH (FIX < 1). Conversely, the interaction between CH and CP resulted in non-additive effects (FIX > 1). The combination treatment of CH with a chemotherapeutic drug was more effective in inducing early apoptosis than the drug alone and the control (P < 0.05). An increase in the sub-G1 phase was observed upon treatment with the combination of CH and chemotherapeutic drugs compared with the control and drugs alone (P < 0.05). Co-administration of CH with chemotherapeutic drugs induced a significant decrease in cell migration compared with the control and chemotherapeutic drugs alone (P < 0.05). Conclusions: The results revealed that combination therapy involving CH in conjunction with 5-FU and DOX demonstrated a more substantial therapeutic effect on TNBC cells than treatments with 5-FU and DOX individually.
- ItemPerioperative Use of Pregabalin vs. Duloxetine for Pain Management of Knee Fracture Surgery: A Double-Blind Randomized Clinical Trial(Brieflands, 2025-12-31) Mohadeseh Masoumi; Mohammad Soleimani; Tara Shekari; Maryam Alaei; Mehrdad Sheikhvatan; Mojtaba Mojtahedzadeh; Kamal Basiri; Farhad Najmeddin; Seyyed Hossein ShafieiBackground: Effective postoperative pain management, particularly in orthopedic procedures, presents significant challenges. There is increasing evidence supporting the benefits of multimodal analgesia, including the use of gabapentinoids and serotonin norepinephrine reuptake inhibitors (SNRIs), to minimize opioid consumption while effectively managing pain. However, a gold-standard treatment has not been established. Objectives: This study aims to compare the efficacy of duloxetine and pregabalin within a multimodal analgesic regimen for managing postoperative pain and their opioid-sparing effects following knee fracture surgery. Methods: In this double-blind randomized clinical trial (RCT), 54 patients undergoing knee fracture surgery were randomized to receive either 75 mg oral pregabalin or 30 mg duloxetine twice daily, starting at least 24 hours prior to surgery and continuing up to 48 hours postoperatively. Pain severity was assessed at admission and at 6, 12, 24, and 48 hours post-operation. Patients reporting a pain score greater than six on a Numeric Rating Scale (NRS) received intramuscular morphine. Additionally, total opioid dose, associated complications, and drug adverse effects were monitored within the first 48 hours post-surgery. Results: Although there was no statistically significant difference between the duloxetine and pregabalin groups at each time point, the reduction in pain at the 48-hour mark was more pronounced in the duloxetine group compared to the pregabalin group. The duloxetine group required higher doses of morphine on the first day compared to the pregabalin group (3.96 ± 3.20 mg vs. 2.14 ± 2.72 mg, P = 0.022). However, on the second day, opioid rescue was required in three patients in the pregabalin group, whereas no patients in the duloxetine group required rescue. No clinically significant adverse effects were observed in either group. Conclusions: Duloxetine 60 mg per day is an equally effective perioperative alternative to pregabalin 150 mg per day, resulting in a slight increase in rescue opioid administration with equivalent analgesic efficacy during the first 24 hours postoperatively. It demonstrates notable analgesic outcomes with no increased need for opioids between 24 to 48 hours post-surgery.
- ItemAssessment of the Efficacy and Safety of Sublingual Melatonin on Symptom Severity, Quality of Life, and Sleep Disorders in Patients with Irritable Bowel Syndrome(Brieflands, 2025-12-31) Shabnam Shahrokh; Niloofar Namazi; Mohammad Abbasinazari; Ali Abazarikia; Amir Sadeghi; Arash MahboubiBackground: Previous studies have demonstrated the efficacy of melatonin in alleviating symptoms of irritable bowel syndrome (IBS) and improving quality of life (QoL). Objectives: Due to its superior bioavailability, this trial was designed to compare the effects of sublingual melatonin (SL melatonin) with a placebo in alleviating IBS symptoms, enhancing QoL, and addressing sleep disorders. Methods: The IBS patients were randomly assigned to receive either 3 mg of SL melatonin or a matching placebo for eight weeks. Participants completed the IBS symptom severity score (IBS-SSS), IBS-quality of life 34 items (IBS-QoL 34), and Pittsburgh Sleep Quality Index (PSQI) questionnaires immediately before and after the study period. Results: A total of 76 patients completed the trial over six months. The results indicated that the severity of IBS symptoms and QoL scores were significantly better in the SL melatonin group compared to the placebo group (P = 0.032 and P = 0.045, respectively). No participants withdrew from the trial due to serious side effects in either the SL melatonin or placebo groups. Conclusions: Sublingual melatonin may be administered to IBS patients as a complementary treatment to alleviate symptoms and improve QoL.
- ItemThe Protective Effects of Mitochondrial Therapy Against Vincristine- Induced Nephrotoxicity in the Rat’s Renal Proximal Tubular Cells(Brieflands, 2025-12-31) Armaghan Lohrasbi; Abdollah Arjmand; Farzaneh Kamranfar; Mehdi Aghsami; Jalal PourahmadBackground: The application of vincristine (VCR) in treating a range of cancers is well-documented, showcasing its considerable effectiveness. Nevertheless, its clinical application is constrained by its impact on healthy tissues and various organ systems. Specifically, it can compromise kidney function, resulting in toxicological concerns. Studies have demonstrated that vincristine contributes to nephrotoxicity via the induction of oxidative stress. Objectives: The present research focused on assessing the influence of mitochondrial transplantation in mitigating the mitochondrial and cellular toxicity associated with VCR in renal proximal tubular cells (RPTCs). Methods: This investigation evaluated specific toxicity metrics, including cell death, reactive oxygen species (ROS) generation, decreased mitochondrial membrane potential (MMP), glutathione (GSH) concentration, succinate dehydrogenase (SDH) activity, lipid peroxidation (LPO), and adenosine triphosphate (ATP) levels. Freshly prepared active mitochondria were obtained from the kidneys of Wistar rats. Results: The data demonstrated the cytotoxic effects of VCR on RPTCs. It was further observed that vincristine triggered oxidative stress, characterized by heightened ROS levels, diminished GSH content, decreased SDH activity, and increased lipid peroxidation. Furthermore, VCR caused notable damage to both mitochondrial and lysosomal membranes, along with a significant decrease in ATP content. The innovative strategy of mitochondrial transplantation mitigated oxidative stress, alleviated mitochondrial membrane damage, and prevented ROS-mediated apoptosis signaling induced by vincristine in RPTCs. Our results also indicated an increase in ATP levels within these cells. Conclusions: Our investigation suggests that the proposed treatment modality may prove beneficial in addressing drug-induced nephrotoxicity.
- ItemTherapeutic Mechanisms of Phenothiazine Drugs: A Mini-Review of Advances in Cancer Treatment and Antibiotic Resistance(Brieflands, 2025-12-31) Xuewei Zou; Bai XieContext: Cancer and antibiotic resistance are critical global health challenges. Phenothiazines, initially developed as antipsychotics, have demonstrated diverse biological activities, including antitumor, antibacterial, and antioxidant effects. Advances in phenothiazine synthesis have produced derivatives with broader therapeutic potential by modulating receptors, ion channels, and inducing lysosomal cell death. This review explores the therapeutic potential of phenothiazines in oncology and infectious disease management, focusing on their mechanisms of action and future clinical applications. Evidence Acquisition: This narrative review synthesizes insights from relevant preclinical studies on phenothiazines' applications in oncology and infectious diseases. Mechanistic pathways and experimental outcomes were analyzed to highlight therapeutic potentials and limitations. Results: Phenothiazines demonstrate significant potential in oncology by inhibiting tumor growth via apoptosis induction, pathway modulation (e.g., PDK1/Akt, MAPK/ERK1/2, and Akt/mTOR), angiogenesis suppression through vascular endothelial growth factor (VEGF) production inhibition, and enhancing the effectiveness of monoclonal antibody therapies. They disrupt key cancer-promoting pathways and induce lysosomal cell death. Beyond oncology, phenothiazines exhibit antibacterial activity, targeting efflux pumps (Eps) and restoring antibiotic susceptibility in multidrug-resistant (MDR) pathogens. These multifaceted actions position phenothiazines as promising agents for combination therapies in cancer treatment and antibiotic-resistant infections. Conclusions: Phenothiazines hold promise as adjuvants in cancer and antibiotic resistance management. Further research should focus on optimizing their pharmacological profiles, elucidating molecular mechanisms, and validating their efficacy through clinical trials.
- ItemExcretion of Acebutolol and its Major Metabolite Diacetolol into Infant Blood Circulation and the Breast Milk(Brieflands, 2003-07-31) S. Abolfazl Mostafavi; Dora A. Stinson; Kent Dooly; Fakhreddin JamaliAcebutolol (AC) is a chiral β-adrenergic blocking drug, which is useful clinically as the racemate in treating hypertension and is metabolized to an equipotent chiral metabolite, diacetolol (DC). In this paper we report a case of a 32 year old woman who was receiving AC during her pregnancy and lactating time for management of hypertension. The maternal plasma level and breast milk as well as cord blood collected to see whether the drug is transferred to the fetus through the mother stereoselectively. A stereospecific high-performance liquid chromatographic (HPLC) assay was used to measure the enantiomeric concentrations of AC and DC. AC and DC enantiomers are stereoselectively excreted into the milk, although the concentrations of DC enantiomers were higher than those of AC. AC concentrations were very low in both cord artery and vein samples four hours after taking the drug however, the stereoselective concentrations of metabolite, DC, was found in these samples. In conclusion, AC and DC enantiomers are excreted in human breast milk in concentrations much higher than that in maternal plasma. Furthermore, DC was found in the infant's plasma indicating that accumulation of metabolite did occur in this infant.
- ItemQuercetine, a Major Flavonol Aglycon from Tanacetum balsamita L.(Brieflands, 2003-10-31) Bahman Nickavar; Gholamreza Amin; Nacim MehreganFrom the aerial parts of Tanacetum balsamita L. (Compositae) a flavonol aglycon was iso-lated using chromatographic techniques. The structure of this compound was determined usingspectroscopic methods (UV, H-NMR and MS) as 3',4',5,7-Tetrahydroxy flavonol (Quercetin).
- ItemPreparation and Characterization of Poly-(methyl ethyl cyanoacrylate) Particles Containing 5-Aminosalicylic acid(Brieflands, 2005-01-31) Hashem Montaseri; MS Sayyafan; Hosnieh TajerzadehPoly-(alkylcyanoacrylate) ester particles have been used for the preparation of different formulations ranging from ophthalmic delivery systems to cancer chemotherapy carriers in clinic. The aim of this study was to prepare and characterize poly-(methyl ethyl cyanoacrylate) (PMECA) particles containing 5-aminosalicylic acid (5-ASA). PMECA particles were prepared using the inverse emulsification polymerization technique. The effects of various formulation parameters such as dispersed phase volume, polymer to drug weight ratio, and surfactant concentration on loading efficiency and size of the prepared particles were investigated. The amount of drug was determined by UV spectrophotometery at 331 nm. Morphological characteristics of particles and particle size analysis were studied by Scanning Electron Microscopy (SEM) and Laser Light Scattering techniques, respectively. The results showed that there was no linear relationship between the dispersed phase volume (DPV) and loading efficiency of 5-ASA in the range of 20-50%. Increasing polymer/drug weight ratio in the range of 1-15, enhanced the loading efficiency from 11.4 to 78.2% in a linear mode (r=0.987). Increasing the surfactant concentration in the range of 1-3% did not increase the loading efficiency of the prepared particles, and increasing the concentration to 5% even decreased the loading efficiency of particles. Laser light scattering and SEM evaluations showed that in all prepared formulations, particles were in a mixture of micro and nanospheres and micro and nanocapsules and 50 percent of particles had mean sizes in the range of 6.4-10.1 micrometer. Although our results showed significant differences in the mean particle size between some of the prepared formulations, this variation was not practically important. It was concluded that by using proper conditions, it is possible to use PMECA as a polymeric matrix for loading of 5-ASA and the other hydrophilic drugs.
- ItemThe Pharmacological Effects of Odonthobuthus doriae Scorpion Venom and Its Extracted Fractions on Neuro-Muscular Transmission(Brieflands, 2006-04-30) Amir Jalali; Zahra Hossininasab; Zynab Ehsani; Amir-Abbas Zare; Afshin Zarghi; Hossein VatanpourThe effect of Odonthobuthos doriae (O.d) scorpion venom at 0/3, 1 and 3, 10 µg/ml concentrations were investigated on nerve-muscle transmission, using the Twitch tension technique. A concentration of 0.3 µg/ml caused a small change in the twitch height in response to indirect muscle stimulation, but higher concentrations (1, 3, 10 µg/ml) caused a transient augmentation in twitch response followed by a large contracture in the chick biventer cervices (CBC) preparation. This effect could be defined as a complex action of the venom, predominately presynaptic, in which its’ effects on postjunctional synapses is also maintained.
- ItemDevelopment and Characterization of Bioadhesive Gel of Microencapsulated Metronidazole for Vaginal Use(Brieflands, 2010-07-31) Nayak Bhabani Shankar; Rout Prasant Kumar; Nayak Udaya Kumar; Bhowmik Benoy BrataThe present study concerned with the development and characterization of metronidazole microcapsules prepared by thermal change method using different ratios (1:1, 1:2 and 1:4) of ethyl cellulose in order to select the best microcapsule formulation with a good encapsulation efficiency and drug release profile. The obtained microcapsules were discrete, spherical with free flowing properties and evaluated for particle size, shape, flow properties, wall thickness, drug encapsulation efficiency and in vitro release performance. The drug carrier interactions were investigated in solid state by FT-IR spectroscopy and scanning electron microscopy. The microcapsules with a narrow size range of 23-68 μm showed higher encapsulation efficiency. The selected microcapsule formulation, MC3 (Drug polymer ratio 1:4) was employed for gel formulation with a variety of carbopol polymers (carbopol-934, 940, 974 and 980) by mechanical stirring method in order to develop a sustained release microencapsulated metronidazole microcapsules-containing bioadhesive gel. The prepared bioadhesive gels were evaluated for pH, spreadability, extrudability, viscosity, vaginal irritation, in vitro drug release, bioadhesion, accelerated stability and in vitro drug release kinetic. In vitro experiments indicated a sustained release over 24 h and an acceptable bioadhesion quality for formulation F3. Hence, it can be concluded that the formulation F3 has potential to deliver metronidazole in a controlled and constant manner for prolong period over other formulations and can be adopted for a successful delivery of metronidazole for vaginal use.
- ItemGastroprotective Effect of Hydroalcoholic Extract of Aloe buettneri(Brieflands, 2011-01-31) Kossi Metowogo; Kwashie Eklu-Gadegbeku; Amégnona Agbonon; Kodjo A. Aklikokou; Messanvi GbeassorAloe buettneri A. Berger is commonly used in traditional Togolese medicine to treat inflammatory and gastric ulcers. The present study examined the gastro-protection effect of the hydro-alcoholic extract of A. buettneri on mucus production and gastric pH. A gastric ulcer is induced by ethanol 95° alone (1 mL/kg body weight), after pre-treatment with indomethacin (300 mg/kg) or by utilising L-NAME (40 mg/kg IV). In addition gastric mucus was removed by scraping and subsequently weighed. The experiment focused entirely on rats that had been subjected to fasting. The hydro-alcoholic extract of A. buettneri (500 mg/kg) significantly inhibited ulcers that were induced by ethanol, indomethacin or L-NAME pre-treatment. A. buettneri was shown to increase the production of gastric mucus. Furthermore L-arginine significantly decreased the size of the induced ulcers. The results achieved in the study carried out suggest that A. buettneri posses gastro-protective properties.
- ItemCytotoxic Effect of Some 1, 4-Dihydropyridine Derivatives Containing Nitroimidazole Moiety(Brieflands, 2011-07-31) Ramin Miri; Katayoun Javidnia; Zahra Amirghofran; Seyyed Hossein Salimi; Zahra Sabetghadam; Savis Meili; Ahmad Reza MehdipourThe 1,4-dihydropyridine (DHP) derivatives are a known class of calcium channel blockers. Some derivatives of DHP showed significant cytotoxicity. It was shown that this effect may not be the result of interaction with Ca2+ channels. In this study, we performed an investigation about the intrinsic cytotoxicity of some derivatives of DHP containing nitroimidazole moiety on their C4 position on four different cancer cell lines (Raji, K562, Fen and HeLa). The result showed that these compounds had moderate-good cytotoxic activity. In addition, QSAR model shows the importance of N atom in cytotoxicity; Ca2+ channels.
- ItemThe Effects of Berberis vulgaris Fruit Extract on Serum Lipoproteins, apoB, apoA-I, Homocysteine, Glycemic Control and Total Antioxidant Capacity in Type 2 Diabetic Patients(Brieflands, 2012-04-30) Farzad Shidfar; Shima Seyyed Ebrahimi; Sharieh Hosseini; Iraj Heydari; Shahrzad Shidfar; Giti HajhassaniType 2 diabetes is a well-known endocrine and metabolic disorder which has reached epidemic proportions worldwide and represents a serious public health concern. Hyperglycemia and dyslipidemia are two major abnormalities which are major cardiovascular risk factors. Berberine is a major alkaloid in Berberis vulgaris fruit extract (BVFE) which have important role in regulation of serum glucose and fat metabolism in-vivo and in-vitro but its role in type 2 diabetes have not been extensively examined.
- Item99mtc-Ubiquicidin [29–41], a Promising Radiopharmaceutical to Differentiate Orthopedic Implant Infections from Sterile Inflammation(Brieflands, 2013-04-30) Davood Beiki; Gholamali Yousefi; Babak Fallahi; Mohammad Naghi Tahmasebi; Ali Gholamrezanezhad; Armaghan Fard-Esfahani; Mostafa Erfani; Mohammad EftekhariUbiquicidin (UBI) [29-41] is a synthetic cationic antimicrobial peptide that preferentially binds to bacterial cell membrane at the site of infection. We aimed to assess diagnostic value of 99mTc-UBI [29-41] as a radiopharmaceutical in differentiation of bacterial infection from sterile inflammation in suspected orthopedic implants. Nine patients suspected for orthopedic implant infection, all males with the mean age of 41.6 ± 20.9 years, were studied. A dose of 10 MBq/Kg (range : 555-740 MBq) 99mTc-UBI [29-41] was injected intravenously. A dynamic study followed by static whole body imaging at 30, 60 and 120 min post-radiotracer injection was acquired. Periprosthetic tissue culture was considered the closest test to a gold standard for diagnosing infections and scintigraphic scans were categorized as true- or false-positive and true- or false-negative, considering the bacterial culture as the gold standard. No adverse reaction was observed during or after the radiotracer injection days. There were five true positive, four true negative and no false positive and false negative scans. Sensitivity, specificity, positive predictive value (PPV) and negative predictive value (NPV) were all calculated as 100%. We found a high diagnostic accuracy for 99mTc-UBI [29-41] scintigraphy in differentiation of bacterial infection from sterile inflammation in suspected orthopedic implants. Therefore, 99mTc-UBI [29-41] scintigraphy might be potentially recommended as a safe and promising imaging modality in these settings. However, further studies on a larger number of patients and different pathologies are still needed.
- ItemSynergistic Effect and Mechanism of Cineole and Terpineol on In-vitro Transdermal Delivery of Huperzine A from Microemulsions(Brieflands, 2013-04-30) Jun Shi; Wen-Juan Cong; Yi-Ming Wang; Qing-Fei Liu; Guo-An LuoThe aim of the present study was to investigate the influence and the mechanisms of cineole and terpineol on the in-vitro transdermal delivery of huperzine A from microemulsions, and their potential synergistic effect on the permeation enhancement. The transdermal delivery of huperzine A from microemulsions with different concentrations of cineole and terpineol through the rat abdominal skin was determined by Franz-type diffusion cells. The partition coefficient of huperzine A between the full thickness skin and microemulsion was determined. Attenuated total reflection-Fourier transform infrared spectroscopy (ATR-FTIR) was carried out to analyze the effects of cineole and terpineol on the biophysical properties of the stratum corneum (SC) and the mechanisms of permeation enhancement. These results indicated that cineole and terpineol could synergistically increase the transdermal delivery of huperzine A from microemulsions through increasing the partition and diffusion coefficients of huperzine A. ATR-FTIR studies further validated the synergistic effect and revealed that the enhancing mechanisms were due to increasing the disorderliness and fluidity of SC lipid alkyl chains, disrupting the structure of keratin in SC, and extracting SC lipids. In conclusion, cineole and terpineol, acting synergistically to enhance the transdermal delivery of huperzine A from microemulsions, might provide an alternative permeation enhancer combination for the transdermal delivery of huperzine A.
- ItemIsolation, Purification, Characterization and Effect upon HepG2 Cells of Anemaran from Rhizome Anemarrhena(Brieflands, 2013-10-31) Qian-Qian Jiang; Yun-Ping Zhao; Wen-Yuan Gao; Xia Li; Lu-Qi Huang; Pei-Gen XiaoThe rhizome of Anemarrhena asphodeloides is used as food and traditional Chinese medicine for its hypoglycemic effect. The aim of this study was to investigate the isolation, purification and hypoglycemic activity of Anemaran as the active component. The influence factors (isolation duration, ratio of residuals to water and extracting times) during the isolation process were evaluated. The optimal conditions for NA and AA were extraction temperature 90ºC and 100ºC, duration 1h and 1.5 h, extraction time 3 and 3, and the solid–liquor ratio 1:20 and 1:15, respectively. Neutral and acid Anemaran (NA and AA) were isolated from the rhizome of Anemarrhena asphodeloides. Five fractions of NA-1, NA-2, NA-3, AA-1 and AA-2 were obtained after crude neutral and acid Anemaran purified through DEAE- 52 cellulose anion-exchange column. The characterizations of Anemaran and its different fractions were both analyzed by Fourier transform infrared spectroscopy (FT-IR) and scanning electron micrographs (SEM). Structural properties of different fractions were examined by FT-IR. Strong characteristic absorption peaks were observed at around 1744 cm−1and 1650 cm−1 caused by the C=O group of uronic acids, and the band between 1440 cm−1 and 1395 cm−1 associated with the stretching vibration of C–O of galacturonic acid. Neither the crude neutral, nor the acid anemaran significantly inhibited the growth of HepG2 cells in-vitro, which indicated the low cytotoxicity of the anemaran. Furthermore, both neutral and acid anemaran showed hypoglycemic effect. The hypoglycemic effect of neutral anemaran was much higher than that of acid anemaran.
- ItemAnxiolytic-Like and Sedative Effects of Alcea Aucheri (Boiss.) Alef. Flower Extract in the Laboratory Rat(Brieflands, 2017-10-31) Tajmah Mombeini; Hamid Gholami Pourbadie; Mohammad Kamalinejad; Soroush Mazloumi; Ahmad Reza DehpourThe present study was conducted to investigate the possible anxiolytic and sedative of an acute administration and 4-day repeated dosing of an aqueous extract of flowers of Alcea aucheri (Boiss.) Alef. (EFA)in rats subjected to the elevated plus-maze (EPM), open-field, and horizontal wire tests. All drugs were administered intraperitoneally. Phytochemical screening confirmed the presence of phenolic compounds, flavonoids, and polysaccharides in the extract. Repeated dosing of EFA (at dose of 35 mg/kg) significantly increased percentage of time spent on open arms and of open arms entries, and also decreased percentage of time spent on closed arms and of closed arms entries; compared with saline control, 24 h after treatment. In addition, repeated dosing of EFA (at dose of 175 mg/kg) significantly increased open arm activity 48 h after treatment, versus saline group. This effect was also observed following acute administration of EFA at 175 mg/kg. In open field, acute administration of EFA at doses of 17.5, 35, 70, 175, 350, and 700 mg/kg induced a statistically significant and dose-dependent decrease in locomotor activity, compared with saline control. ED50 value for EFA-induced decrease in locomotor activity was 194 mg/kg. Furthermore, unlike diazepam; EFA didn´t decrease the percent of the rats grasping the wire.
- ItemEfficacy and Safety of Two Different Enoxaparin Doses for Thromboprophylaxis in Non-critically Ill Patients: A Randomized Controlled Trial(Brieflands, 2022-12-31) Ilad Alavi-Darazam; Kimia Forouhar; Omid Moradi; Ali Saffaei; Sara Asadi; Zahra SahraeiBackground: Recently, a few studies based on anti-factor Xa activity levels have propounded doubtful and sub-prophylactic levels by the usual dose of enoxaparin in surgical and critically ill patients. In this study, we assessed two doses of enoxaparin in adult non-critically ill patients. Methods: Patients were randomly assigned into two groups of intervention and control. While the intervention group received enoxaparin with a daily dose of 60 mg, the control group received enoxaparin 40 mg. Anti-factor Xa activity was measured based on the peak steady-state levels. The level of 0.2 to 0.4 IU/mL was considered as a prophylactic goal. All individuals were followed for bleeding or thromboembolic events during admission. Results: The mean levels of anti-factor Xa were 0.29 ± 0.13 IU/mL in the control group (n = 31) and 0.44 ± 0.19 IU/mL in the intervention group (n = 29). More patients in the control group had an optimal level of anti-factor Xa compared to the patients in the intervention group (62.1% vs. 29%). No adverse outcomes were detected in any of the groups. Conclusions: Enoxaparin dose of 60 mg daily provided anti-factor Xa level higher than desired in most patients. In non-critically ill patients, the dose of 40 mg is the proper dose for thromboprophylaxis.
- ItemHIV-1 Reverse Transcriptase/Integrase Dual Inhibitors: A Review of Recent Advances and Structure-activity Relationship Studies(Brieflands, 2021-04-30) Mohammad Mahboubi-Rabbani; Maryam Abbasi; Zahra Hajimahdi; Afshin ZarghiThe significant threat to humanity is HIV infection, and it is uncertain whether a definitive treatment or a safe HIV vaccine is. HIV-1 is continually evolving and resistant to commonly used HIV-resistant medications, presenting significant obstacles to HIV infection management. The drug resistance adds to the need for new anti-HIV drugs; it chooses ingenious approaches to fight the emerging virus. Highly Active Antiretroviral Therapy (HAART), a multi-target approach for specific therapies, has proved effective in AIDS treatment. Therefore, it is a dynamic system with high prescription tension, increased risk of medication reactions, and adverse effects, leading to poor compliance with patients. In the HIV-1 lifecycle, two critical enzymes with high structural and functional analogies are reverse transcriptase (RT) and integrase (IN), which can be interpreted as druggable targets for modern dual-purpose inhibitors. Designed multifunctional ligand (DML) is a new technique that recruited many targets to be achieved by one chemical individual. A single chemical entity that acts for multiple purposes can be much more successful than a complex multidrug program. The production of these multifunctional ligands as antiretroviral drugs is valued with the advantage that the viral-replication process may end in two or more phases. This analysis will discuss the RT-IN dual-inhibitory scaffolds’ developments documented so far.
- ItemComparative Chemical Composition and Antioxidant Properties of the Essential Oils and Aromatic Water from Teucrium persicum Boiss(Brieflands, 2012-04-30) Abdolhossein Miri; Hamid Reza Monsef-Esfahani; Mohsen Amini; Yaghoub Amanzadeh; Abbas Hadjiakhoondi; Reza Hajiaghaee; Atefeh EbrahimiThe essential oils and aromatic water, known as Arak in traditional Iranian medicine, comes from the aerial part of Teucrium persicum Boiss., which is grown in Fars Province located in Iran. The samples were collected in summer and the oils and aromatic water were obtained through steam distillation. The chemical composition of the oils was analyzed using GC-MS. An analysis of the chemical profile of the isolated oils revealed the presence of more than 80 compounds, mainly oxygenated monoterpenes and sesquiterpene hydrocarbons. The principal components of essential oil were α-cadinene (9.7%), 1,4-cadinadiene (9.2%) and α-terpinyl acetate (7.9%). The major constituents in the Arak were determined to be linalool (10.4%), α-cadinene (7.5%) and γ-terpineol (7.3%). Most of the compounds identified from different oils were similar, but their amounts differed. The oil revealed a higher content of total phenolics than the Arak (1.71 ± 0.12 mg GAE/g DW and 1.36 ± 0.11 mg GAE/g DW, respectively). The antioxidant activity of the oils was calculated by using a ferric reducing antioxidant power assay (FRAP), DPPH radical scavenging activity, and a reducing power assay (RP). The FRAP value points to a considerably higher reducing power of essential oil (220 ± 7.2 µmol Fe2+/g DW) compared to that of Arak (113 ± 5.4 µmol Fe2+/g DW). Essential oil exhibited higher radical scavenging potential (IC50 = 0.29 mg/mL) than Arak (IC50 = 4.19 mg/mL). The reducing power of essential oil (51.7 ± 4.3 µg BHA/g DW) was higher than that of Arak (34.1 ± 2.7 µg BHA/g DW). The studied essential oils showed good antioxidant activities, which were higher than those of Arak.