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Drug Research
Journal Prestige (SJR): 0.334
Citation Impact (citeScore): 1
Number of Followers: 3  
 
  Hybrid Journal Hybrid journal (It can contain Open Access articles)
ISSN (Print) 2194-9379 - ISSN (Online) 2194-9387
Published by Thieme Publishing Group Homepage  [233 journals]
  • Effect of Nigella Sativa in Improving Blood Glucose Level in T2DM:
           Systematic Literature Review of Randomized Control Trials

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      Authors: Hoda; Farazul, Khanam, Afifa, Thareja, Mehak, Arshad, Mawrah, Ahtar, Mohd, Najmi, Abul Kalam
      Abstract: Background Diabetes mellitus is a highly prevalent condition that affects people of all ages, races, and genders. Medicinal herbs have received a lot of attention from researchers, and they have suggested it to be a good adjuvant to oral diabetes medications because of their combined effects. Objectives The purpose of this systematic review is to summarize the available evidences and literature of Randomized Control Trials (RCTs) on Nigella sativa (NS) in the management of Type 2 Diabetes Mellitus (T2DM). Methods A computerised database search was performed to obtain the relevant clinical trial studies. We searched the following PubMed and Google Scholar databases. Randomized controlled trials (RCTs) comparing NS versus any treatment for the management of T2DM in adults were eligible for inclusion. Results A total of 7 articles were retrieved for interpretation, complete assessment and data extraction in this systematic review. This systematic review seeks to give thorough information on the effects of NS on glucose and insulin profile status in patients with T2DM. Interpretation & Conclusion Different mechanisms are proposed which contribute to the anti-diabetic activity of NS. Various outcome parameters evaluated demonstrate a significant improvement in the management of T2DM and its complications upon intervention with NS.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-09-27T09:34:37+01:00
      DOI: 10.1055/a-1936-8412
       
  • Development and Evaluation of Topical Ethosomal Gel for Fungal Infections

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      Authors: Gupta; Preeti, Hafeez, Abdul, Kushwaha, Poonam
      Abstract: Background Fungal infections are one of the most common dermatological issues worldwide. Candida species-caused fungal infections are frequent on the cutaneous surface. Eberconazole (EBZ) has the strongest antifungal action against Candida spp., the major source of fungal infections. Method In the present study, the cold method followed by probe sonication was used to create EBZ-loaded ethosomal dispersion. The solubility of ethosomes in different lipids and surfactants was used to choose these components. Under magnetic stirring, the dispersion was absorbed into a carbopol 934 gel. In vitro antifungal activity was performed using the Agar well diffusion method, and their topical effectiveness against pathogenic Candida albicans was compared to that of a marketed formulation containing EBZ. Results Eberconazol incorporated into gel displayed sustained release in an in vitro release assay. Based on the zone of inhibition diameters, EBZ formulation was determined to be efficient against C. albicans when compared to the commercialized cream and plain gel. Conclusion Based on these findings, the current study found that EBZ possesses significant antifungal efficacy against C. albicans.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-09-22T07:41:23+01:00
      DOI: 10.1055/a-1924-7818
       
  • Synergetic Effect of Lupeol and Naringin Against Bile Duct Ligation
           Induced Cardiac Injury in Rats via Modulating Nitrite Level (eNos) and
           NF-kB /p65 Expression

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      Authors: Alam; Firoj, Kharya, Anil Kumar, Srivastav, Ritesh Kumar, Akhtar, Juber, Khan, Mohammad Irfan, Ahmad, Mohammad
      Abstract: Cardiac dysfunction such as cirrhotic cardiomyopathy is more common in liver cirrhosis related disorders including primary biliary cholangitis or biliary cirrhosis and primary sclerosing cholangitis. Bile duct ligation (BDL) is an effective model of biliary cholestasis, producing oxidative damage and fibrosis. This research was designed to evaluate the effect of Lupeol and Naringin and its combination on bile duct ligation induced cardiac injury in rats. For pharmacological evaluation, rats were randomly divided into seven groups; intrahepatic cholestasis induced by ligation of the bile duct might lead to cirrhotic cardiomyopathy. The results were analyzed by physical, biochemical and histological examination. The Lupeol (100 mg/kg, p.o.), Naringin (100 mg/kg, p.o.) and its combination (100 mg/kg each) treated group significantly improved physical infarct size, biochemical (Nitrite, SOD, CAT, and GSH) and histological (heart tissue- mitochondrial function/integrity and fibrosis) alterations occurs due to BDL-ligation. This study was concluded that oral administration of Lupeol, Naringin, and its combination has a curative potential against BDL-induced cardiac injury in rats by reducing oxidative stress and inflammatory reactions, resulting in reduced heart necrosis/myocardial infarction and increased myocardial activity. It also inhibits cardiac damage in the rat heart, these effects may be linked to the NO level (eNOS) is increased and the inactivation of the NF-kB-p65 expression pathways.This study also provides new insights into the development of lupeol and Naringin combination that can be used as supportive therapy for cardiovascular diseases.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-09-22T07:39:20+01:00
      DOI: 10.1055/a-1879-2944
       
  • Identification and Screening of Novel Anti-Cancer Compounds for Aurora
           Kinase-A from Chemical Database

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      Authors: Singh; Ipsa A., Lokhande, Kiran Bharat, Swamy, K. Venkateswara
      Abstract: Aurora kinase is a group of enzymes that belongs to a serine-threonine family and plays a critical role in cellular division. Aurora Kinase A is overexpressed and distributed beyond the nucleus and is involved in tumorigenesis. Flavones are a class of flavonoids that are present in plants that show anticancer activity. Similar compounds of 2’Fluoroflavones are retrieved from the PubChem database. Then drug-like filters viz. REOS and PAINS were applied to remove toxic compounds using Canvas software, resulting in 3882 compounds being subjected to Glide docking with Aurora kinase A. The lead compounds were selected on the merit of hydrogen bonding, salt bridge, as well as pi-pi interactions, 4-(6-Fluoro-4-oxychromen-2yl) benzoic acid, has been found one of the best molecules from docking studies. The binding mode of the lead compound with AURKA reveals that the amino acid residues viz, Lys162, Ala213, and His280 are more important for binding with the binding affinity of -11.760 kcal/mol. The molecular dynamics simulations of 100 ns were done, which shows the mean RMSD value of 1.77 Å for all 3 complexes of the protein and Fluoroflavone and its analogs. This shows that Fluoroflavone and its 2 best analogs are tightly attached to the active sites and thus have conformational stability. Our finding suggests that 4-(6-fluoro-4-oxochromen-2-yl)benzoic acid and 4-(4-Oxochromen-2-yl)benzoate can be further used in vitro and in vivo experiments and can probably serve as a novel drug for cancer treatment.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-09-22T07:36:39+01:00
      DOI: 10.1055/a-1877-4693
       
  • Effect Produced by a Cyclooctyne Derivative on Both Infarct Area and Left
           Ventricular Pressure via Calcium Channel Activation

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      Authors: Lauro; Figueroa-Valverde, Marcela, Rosas-Nexticapa, Maria, López-Ramos, Francisco, Díaz-Cedillo, Magdalena, Alvarez-Ramirez, Virginia, Mateu-Armad Maria, Montserrat, Melgarejo-Gutierrez
      Abstract: Background There are reports which indicate that some cyclooctyne derivatives may exert changes in cardiovascular system; however, its molecular mechanism is not very clear. Objective The aim of this study was to evaluate the biological activity of four cyclooctyne derivatives (compounds 1 to 4) produced on infarct area and left ventricular pressure. Methods Biological activity produced by cyclooctyne derivatives on infarct area was determinate using an ischemia/reperfusion injury model. In addition, to characterize the molecular mechanism of this effect, the following strategies were carried out as follows; i) biological activity produced by cyclooctyne derivative (compound 4) on either perfusion pressure or left ventricular pressure was evaluated using an isolated rat heart; ii) theoretical interaction of cyclooctyne derivative with calcium channel (1t0j protein surface) using a docking model. Results The results showed that cyclooctyne derivative (compound 4) decrease infarct area of in a dose-dependent manner compared with compound 1 to 3. Besides, this cyclooctyne derivative increase both perfusion pressure and left ventricular pressure which was inhibited by nifedipine. Other theoretical data suggests that cyclooctyne derivative could interact with some aminoacid residues (Met83, Ile85, Ser86, Leu108, Glu114) involved in 1t0j protein surface. Conclusions All these data indicate that cyclooctyne derivative increase left ventricular pressure via calcium channel activation and this phenomenon could be translated as a decrease of infarct area.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-11-29T06:54:25+0100
      DOI: 10.1055/a-1967-2004
      Issue No: Vol. eFirst
       
  • Curcumin-Loaded Chitosan Nanoparticle Preparation and Its Protective
           Effect on Celecoxib-induced Toxicity in Rat isolated Cardiomyocytes and
           Mitochondria

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      Authors: Ebrahimi; Hossein Ali, Esmaeli, Samira, Khezri, Saleh, Salimi, Ahmad
      Abstract: Curcumin has a wide range of pharmacological activities, including antioxidant, anti-inflammatory and tissue protective. In here we hypothesized that curcumin-loaded chitosan-coated solid lipid nanoparticles (CuCsSLN) are able to increase its overall bioavailability and hence its antioxidant and mitochondria;/lysosomal protective properties of curcumin. CuCsSLN were prepared using solvent diffusion technique for formation of solid lipid nanoparticles (SLNs) and electrostatic coating of positive-charged chitosan to negative surface of SLNs. CuCsSLN showed the encapsulation efficiency of 91.4±2.7%, the mean particle size of 208±9 nm, the polydispersity index of 0.34±0.07, and the zeta potential of+53.5±3.7 mV. The scanning electron microscope (SEM) images of nanoparticles verified their nanometric size and also spherical shape. Curcumin was released from CuCsSLN in a sustain release pattern up to 24 hours. Then isolated cardiomyocytes and mitochondria were simultaneously treated with (1) control (0.05% ethanol), (2) celecoxib (20 µg/ml) treatment, (3) celecoxib (20 µg/ml)+++CuCsSLN (1 µg/ml) treatment, (4) CuCsSLN (1 µg/ml) treatment, (5) celecoxib (20 µg/ml)+++curcumin (10 µM) treatment and (6) curcumin (10 µM) treatment for 4 h at 37°C. The results showed that celecoxib (20 µg/ml) induced a significant increase in cytotoxicity, reactive oxygen species (ROS) formation, mitochondria membrane potential (ΔΨm) collapse, lipid peroxidation, oxidative stress and mitochondrial swelling while CuCsSLN and curcumin reverted the above toxic effect of celecoxib. Our data indicated that the effect of CuCsSLN in a number of experiments, is significantly better than that of curcumin which shows the role of chitosan nanoparticles in increasing effect of curcumin.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-11-24T18:18:20+0100
      DOI: 10.1055/a-1960-3092
      Issue No: Vol. eFirst
       
  • The Possible Protective Effects of Ondansetron and Tropisetron on Optic
           Nerve Crush Injury in Rats

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      Authors: Shayan; Maryam, Eslami, Faezeh, Khosravi, Ayda, Rashidian, Amir, Jafari, Razie Mohammad, Maroufi, Seyed Farzad, Golroudbari, Hasti Tashak, Dehpour, Ahmad Reza
      Abstract: Background This study aimed to evaluate the potential neuroprotective effect of cyclosporine – a calcineurin inhibitor–, ondansetron, and tropisetron-5-hydroxytryptamine (serotonin) 3 receptor (5-HT3R) antagonists–, on optic nerve crush (ONC) injury in rats. Moreover, underlying signaling activities of their beneficial neuroprotective effects were studied. Methods Adult male rats were treated with the intravitreal administration of cyclosporine (1.6 mM), ondansetron (100 nM), and tropisetron (100 nM) immediately after the induction of ONC. Subsequently, on 7th day after surgery, the rats’ retinas were extracted, and the expression of apoptotic regulators (Bax and Bcl-2) and calcineurin were studied by western blot analysis. Results The induction of ONC injury was associated to higher expression of Bax and calcineurin, while Bcl-2 expression was considerably decreased in these animals. Intravitreal treatment with cyclosporine (1.6 mM), ondansetron (100 nM), and tropisetron (100 nM) significantly attenuated the increased expression of Bax and calcineurin. Moreover, the treatment with these agents resulted in an elevated expression of Bcl-2 in the retina. Conclusion Our findings indicate that cyclosporine, ondansetron, and tropisetron protect against ONC injury in rats, possibly via the suppression of apoptosis and modulation of calcineurin activity directly and via 5-HT3 receptors. Moreover, immunoblotting showed that tropisetron was more effective as opposed to ondansetron. Further studies are needed to evaluate the precise mechanism behind cyclosporine, ondansetron, and tropisetron activities.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-11-24T18:18:19+0100
      DOI: 10.1055/a-1969-4600
      Issue No: Vol. eFirst
       
  • Mitochondrial Transplantation Therapy against Ifosfamide Induced Toxicity
           on Rat Renal Proximal Tubular Cells

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      Authors: Arjmand; Abdollah, Mashhadi, Melika, Kaveh, Armin, Kamranfar, Farzaneh, Seydi, Enayatollah, Pourahmad, Jalal
      Abstract: Mitochondrial dysfunction is a basic mechanism leading to drug nephrotoxicity. Replacement of defective mitochondria with freshly isolated mitochondria is potentially a comprehensive tool to inhibit cytotoxicity induced by ifosfamide on renal proximal tubular cells (RPTCs). We hypothesize that the direct exposure of freshly isolated mitochondria into RPTCs affected by ifosfamide might restore mitochondrial function and reduce cytotoxicity. So, the aim of this study was to assess the protective effect of freshly isolated mitochondrial transplantation against ifosfamide-induced cytotoxicity in RPTCs. Therefore, the suspension of rat RPTCs (106 cells/ml) in Earle’s solution with the pH of 7.4 at 37°C was incubated for 2 h after ifosfamide (4 mM) addition. Fresh mitochondria were isolated from the rat kidney and diluted to the needed concentrations at 4°C. The media containing suspended RPTCs was replaced with mitochondrial-supplemented media, which was exposed to cells for 4 hours in flasks-rotating in a water bath at 37°C. Statistical analysis demonstrated that mitochondrial administration reduced cytotoxicity, lipid peroxidation (LPO), reactive oxygen species (ROS) production, mitochondrial membrane potential (MMP) collapse, lysosomal membrane damage, extracellular oxidized glutathione (GSSG) level, and caspase-3 activity induced by ifosfamide in rat RPTCs. Moreover, mitochondrial transplantation increased the intracellular reduced glutathione (GSH) level in RPTCs affected by ifosfamide. According to the current study, mitochondrial transplantation is a promising therapeutic method in xenobiotic-caused nephrotoxicity pending successful complementary in vivo and clinical studies.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-11-17T14:57:38+0100
      DOI: 10.1055/a-1967-2066
      Issue No: Vol. eFirst
       
  • A Double-blind, Placebo-controlled, Randomized, Single Ascending, and
           Multiple Dose Phase 1 Study to Evaluate the Safety, Tolerability, and
           Pharmacokinetics of Oral Dose Isomyosamine Capsules in Healthy Adult
           Subjects

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      Authors: Brager; Jenna, Chapman, Chris, Dunn, Leonard, Kaplin, Adam
      Abstract: Background Aging is tightly linked to chronic disease, frailty, and death. Multi-morbidity, defined as the presence in the same patient of three or more conditions such as neoplastic, cardiovascular, neurodegenerative, metabolic, or autoimmune diseases, becomes more common with age. Methods The study was performed in a double-blind fashion. Subjects within each dose cohort (Cohorts 1, 2, 3, and 4) were randomly assigned to receive Isomyosamine doses (between 150 mg to 600 mg or placebo) or placebo in a 3:1 ratio (6 active: 2 placebo). Results Isomyosamine single daily doses each of 150 mg, 300 mg, and 450 mg for 3 days and multiple daily doses of 600 mg for 6 days were safe and well tolerated in healthy subjects. In one dose group, there was a decrease in TNF-α levels found in Isomyosamine treated subjects, but no change in the levels in subjects given placebo. The increase in Isomyosamine exposure was proportional to dose across the dose range of 300 mg to 600 mg when administered as a single dose. There was minimal accumulation of Isomyosamine following 5 days of once daily dosing of Isomyosamine 600 mg. Isomyosamine half-life ranged from approximately 15 minutes to 45 minutes across all doses in the single ascending dose and multiple ascending dose portion of the study. Elimination of Isomyosamine included the renal pathway as a minor route. Conclusion Isomyosamine will continue to be investigated in phase 2 clinical trials for the treatment of sarcopenia/frailty, hashimoto’s thyroiditis and rheumatoid arthritis.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-11-11T07:49:38+0100
      DOI: 10.1055/a-1962-6834
      Issue No: Vol. eFirst
       
  • Aloe Vera-Containing Matrix in Transdermal Fentanyl Therapy Improves
           Adhesion, Skin Tolerance and Quality of Life: Results of a German
           Multicenter Study with a New Fentanyl Patch

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      Authors: Dietrich; Christoph G., Kottmann, Tanja, Voß, Hans Werner, Lorenz, Roxane
      Abstract: Background Chronic pain represents a significant and costly healthcare problem especially in the older patient. Transdermal opioid therapy is easy to apply and ensures constant supply of active ingredients. However, skin irritation, poor adhesion and systemic side effects complicate transdermal pain therapy. Methods In the Relief study, comprising 54 centers, all in Germany, 252 patients were recruited and data about the general care situation as well as the characteristics, effects and side effects of the Aloe vera fentanyl patch were collected. 92 patients had a prior treatment with fentanyl patch without Aloe vera, allowing a comparative analysis. Results Compared to patches without Aloe vera, the new fentanyl patch showed better adhesion. Systemic and local tolerance and pain reduction were also significantly better. Patients also reported improvements in side effects and central parameters of quality of life. The data regarding the care situation in Germany showed remarkably low use of coanalgetics and laxatives in pain patients. Discussion Aloe vera in transdermal pain treatment improves adhesion and local tolerance of the patch. Pain control and quality of life were also improved. Regional care data concerning cotreatment in pain therapy from this study indicate a lack of penetration of existing guidelines in general practitioners’ pain therapy.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-11-11T07:49:38+0100
      DOI: 10.1055/a-1960-2879
      Issue No: Vol. eFirst
       
  • Saliva Sampling in Therapeutic Drug Monitoring and Physiologically Based
           Pharmacokinetic Modeling: Review

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      Authors: Almukainzi; May
      Abstract: Therapeutic drug monitoring investigations based on saliva samples can be utilized as an alternative to blood sampling for many advantages. Moreover, the development of physiologically based pharmacokinetic (PBPK) modeling tools can further help to estimate drug exposure from saliva. This review discusses the use of saliva samples and illustrates the applications and examples of PBPK modeling systems for estimating drug exposure from saliva.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-11-11T07:49:38+0100
      DOI: 10.1055/a-1956-9313
      Issue No: Vol. eFirst
       
  • Molecular Docking Study of Isoxazole Indole Derivatives (B2A2 Series) as
           Promising Selective Estrogen Receptor Modulators & Anticancer Drugs

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      Authors: Iyer; Jayashree Monikanta, Khare, Aradhana, Pandey, Jaya, Yadav, Manish
      Abstract: A series of 7 compounds with isoxazole – indole – γ-resorcylic acid scaffold, segregated into B2 & A2 series, wherein, B2 comprises Compounds: 13, 14, 15 & 16 and A2 comprises Compounds: 10, 11 & 12, on the basis of the variable substituents at the indole, resorcinol and isoxazole end of the scaffold as in Figure: 1, were designed and docked with human estrogen receptor: 1ERRα. The Binding affinity (BA) and the interacting amino acids compared with reference selective estrogen receptor modulators (SERM’s) such as Raloxifene, Estradiol, Bazedoxifene, Bisphenol, Genistein, Daidzein, Ormiloxifene, Tamoxifen, 6-hydroxy-naphthalen-2yl-benzo(D)-isoxazol-6-ol(1) using PyRx software and their ADME properties predicted with SWISS ADME online tool. Significant similarities and minor differences in the binding pattern between the key interacting aminoacids such as Arg 394, Glu 353, Asp 351, Leu 346, Leu 525, Trp 383, Phe 404, Ala 350, Leu 387, Met 421 responsible for ER agonist/antagonist affinity found in the binding cavity of a 1 Errα -Bazedoxifene/1 Errα -raloxifene/1 Errα -estradiol docked complex AND 1 Errα -isoxazole-indole- resorcinol docked complex indicate their promising potential to serve as potent ER agonists in bone or ER antagonists against breast cancer and other cancer diseases. The Compounds with highest BA is of the order: BA (A1series)>B1series>//=BA (B2 series) exceptions: compounds: 4, 5 of B1 series & compound:13 of B2 series with identical and least BA values.BA(6)=BA(8)>BA(7)>BA(2)>BA(9)=BA(1)>BA(12)>BA(10)=BA(15)=BA(11)=BA(3)>BA(14)=BA(16)>BA(4)=BA(5)=BA(13).
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-10-27T14:27:57+01:00
      DOI: 10.1055/a-1958-3823
      Issue No: Vol. eFirst
       
  • Effects of Chronic Oral Administration of Midazolam on Memory and
           Circadian Rhythms in Rats

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      Authors: Murphy; Helen M., Kalinina, Anastasiya I., Wideman, Cyrilla H.
      Abstract: Studies have shown the ability of benzodiazepine drugs to cause memory loss in animals and humans. Midazolam is a benzodiazepine commonly administered intravenously during surgical procedures because it reacts rapidly, causes anterograde amnesia, and has few side effects. It has also been used in palliative medicine where, among others, an oral route has been employed for chronic administration of the drug. The current study evaluated the effects of chronic orally administered midazolam on spatial working memory and procedural memory in control and experimental female rats over a three-week experimental period utilizing the Morris water maze. Sample and test run times to a submerged platform in the maze were recorded daily. In addition, activity wheels attached to each cage were employed to monitor daily circadian activity of the animals. Spatial working memory was not impaired in either group. However, procedural memory amnesia occurred in animals receiving the drug indicative of a consolidation or retrieval problem. Concerning circadian rhythms, a phase-shift was noted in experimental animals possibly indicating that time of day of drug administration is important. The findings of the present study could shed insight into altered reactions observed in humans who have received midazolam as a component of treatment in palliative medicine.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-10-27T14:27:57+01:00
      DOI: 10.1055/a-1937-9064
      Issue No: Vol. eFirst
       
  • The Novel Gabapentinoid Mirogabalin Prevents Upregulation of α2δ-1
           Subunit of Voltage-Gated Calcium Channels in Spinal Dorsal Horn in a Rat
           Model of Spinal Nerve Ligation

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      Authors: Domon; Yuki, Kobayashi, Naoko, Kubota, Kazufumi, Kitano, Yutaka, Ueki, Hideaki, Shimojo, Yumiko, Ishikawa, Kayoko, Ofune, Yuka
      Abstract: Gabapentinoids are specific ligands for the α2δ-1 subunit of voltage-gated calcium channels. This class of drugs, including gabapentin and pregabalin, exert various pharmacological effects and are widely used for the treatment of epilepsy, anxiety, and chronic pain. The mechanism of action of gabapentinoids involves both direct modulation of calcium channel kinetics and inhibition of channel trafficking and expression, which contribute to the above pharmacological effects. In the present study, we investigated the effects of mirogabalin, a novel potent gabapentinoid, on expression levels of the α2δ-1 subunit in the spinal dorsal horn in a rat model of spinal nerve ligation (SNL) as an experimental animal model for peripheral neuropathic pain. The neuropathic pain state was induced by SNL in male Sprague – Dawley rats. After the development of mechanical hypersensitivity, the animals received 10 mg/kg mirogabalin or vehicle orally for 5 consecutive days and were subjected to immunohistochemical analysis of α2δ-1 subunit expression in the spinal cord. In the SNL model rats, expression of the α2δ-1 subunit significantly increased in the spinal dorsal horn at the ipsilateral side of nerve injury, while mirogabalin inhibited this increase. In conclusion, the α2δ-1 subunit was upregulated in the spinal dorsal horn of SNL model rats, and repeated administration of mirogabalin inhibited this upregulation. The inhibitory effect of mirogabalin on upregulation of the α2δ-1 subunit after nerve injury is considered to contribute to its analgesic effects in peripheral neuropathic pain.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-10-10T07:54:57+01:00
      DOI: 10.1055/a-1941-8907
      Issue No: Vol. eFirst
       
  • The Therapeutic Role of Rho Kinase Inhibitor, Fasudil, on Pulmonary
           Hypertension; a Systematic Review and Meta-Analysis

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      Authors: Abedi; Farshad, Omidkhoda, Navid, Arasteh, Omid, Ghavami, Vahid, Hosseinzadeh, Hossein
      Abstract: Background Pulmonary hypertension (PH) is a pathophysiological disorder, which involves multiple clinical conditions such as the upregulation of the Rho/ROCK signaling pathway. On the other hand, fasudil as a Rho kinase inhibitor has been investigated in the treatment of PH in some clinical studies. Objectives The present systematic review and meta-analysis aimed to evaluate the human clinical trials regarding the efficacy of fasudil in the management of PH. Methods Databases were searched with pre-defined search terms, up to December 2021. Efficacy measures were such as mean pulmonary arterial pressure (mPAP), systolic PAP (sPAP), pulmonary vascular resistance (PVR), systolic vascular resistance (SVR) and cardiac index (CI). Results A total of 12 studies involving 575 PH patients were included in our research. Eight short-term trials and four mid-term trials were found (no clinical trials on the long-term effects). Short-term trials had a before-after study design and measuring pulmonary hemodynamic parameters’ intervention revealed a statistically significant improvement of mPAP, sPAP, PVR, SVR, and CI in the meta-analysis of five eligible studies. Three mid-term trials also revealed improvement in some pulmonary hemodynamic parameters with fasudil and in another mid-term trial, fasudil significantly decreased rehospitalization and mortality in PH patients. No serious adverse effects with fasudil were reported in these trials. Conclusion Fasudil therapy is efficacious and probably safe in the improvement of some hemodynamics in PH patients along short and mid-term periods. However, long-term randomized controlled trials comparing fasudil with placebo and other treatments are warranted for confirmation of these benefits.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2022-10-10T07:54:57+01:00
      DOI: 10.1055/a-1879-3111
      Issue No: Vol. eFirst
       
  • Therapeutic Approach Against 2019-nCoV by Inhibition of the ACE-2 receptor

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      Authors: Kumar; Gajendra, Kumar, Dharmendra, Singh, Netra Pal
      Abstract: The continued spread of the 2019 novel coronavirus (2019-nCoV) has promptedglobal concern. The formal name given to 2019-nCoV by the World HealthOrganization is COVID-19, while the International Committee on Taxonomy hasnamed it severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2). Dueto this viral attack, nations around the world have issued lockdownrestrictions. Presently, there is no effective way to control the spread of2019-nCoV, except through social distancing and hygienic activities.World-class scientists and researchers are trying to develop vaccines andmedicines that will cure this deadly viral disease and control its spread.Our aim in presenting this article is to provide an easy therapeuticapproach that effectively combats deadly viral diseases, such as COVID-19,with minimal intervention and effort. Different Ayurvedic therapeutic agents(Curcuma longa L, green tea, and Piper nigrum) inhibit theentry of viruses in the host cell and the transmission of pathogens, whileimproving immunity. Curcumin and piperine (1-piperoylpiperidine) interactwith each other and form a π–π intermolecularcomplex that enhances the bioavailability of curcumin by inhibition ofglucuronidation of curcumin in the liver. Two molecules, curcumin andcatechin, bind directly to the receptor-binding domain of the S-protein andthe angiotensin-converting enzyme 2 receptor of the host cell, by whichthese molecules inhibit the entry of viruses in the host cell. As a result,the animal host will survive the infection.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2020-12-23T00:00:00+0100
      DOI: 10.1055/a-1337-4462
      Issue No: Vol. eFirst
       
  • Application of Carbon Nanotubes in Breast Cancer Therapy

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      Authors: Tajabadi; Mahdis
      Abstract: Conjugated single-walled carbon nanotubes (SWNT) have been shown to be promising in cancer-targeted accumulation and is biocompatible, easily excreted, and possesses little toxicity. The present study aims at reviewing the recent advancements in carbon nanotubes especially SWNT for improving the treatment of breast cancer. Nanotube drug delivery system is a potential high efficacy therapy with minimum side effects for future tumor therapy with low doses of drug.
      Citation: Drug Res (Stuttg) ; : -
      PubDate: 2019-06-28T00:00:00+01:00
      DOI: 10.1055/a-0945-1469
      Issue No: Vol. eFirst
       
 
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