International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (4), pp. 001-006, April, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
Fluvastatin Reduces Amyloid Beta Production in Rat Brain by Modulating APP Processing and Secretase Expression
Yun Shi1, Min Yao1, Lian-Guo Hou1, Jing Li1, Hai-Bao Zhu2, Jie Liu1, and Ling-Ling Jiang1*
1Department of Biochemistry and Molecular Biology, Hebei Medical University, Shijiazhuang 050017, PR China.
2Department of Neurology, Chengde Central Hospital, Chengde 067000, PR China.
Accepted 5 March, 2025
The aim of the present study was to determine the effects of fluvastatin, a relatively hydrophilic 3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMGR) inhibitor, on endogenous amyloid beta (A ) production and if such effects would be associated with changes in brain total cholesterol in rats. Wistar male rats were treated with fluvastatin at a dose of 20 mg/kg/day or vehicle (controls) by oral gavage for 28 days. We examined serum and brain cholesterol levels by CHOD-PAP method, brain A levels by radioimmunoassay, mRNA levels of HMGR and cholesterol 24S-hydroxylase (CYP46) involving in cholesterol balance, -secretase (BACE1) and -secretase (ADAM10) involving in amyloid beta precursor protein (A PP) processing by RT-PCR and protein levels of A PP by immunohistochemistry. Serum total cholesterol and brain A levels were significantly reduced in fluvastatin-treated rats. There was no change in total cholesterol levels, HMGR and CYP46 mRNA levels in the brain of fluvastatin-treated rats. Fluvastatin reduced A PP protein levels and up-regulated ADAM10 but down-regulated BACE1 mRNA expression in rat brain under used condition. These results suggest that reduction of brain A levels by fluvastatin is associated with changes in level of A PP and A PP cleavage-related enzyme mRNA, and is independent of brain total cholesterol. It may contribute to one of neuroprotective effects of fluvastatin and reveal that administration of fluvastatin could be beneficial in the preventation of AD.
Key words: Alzheimer’s disease, cholesterol, amyloid, amyloid-protein precursor, fluvastatin, statin.
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (4), pp. 001-005, April, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
Diabetic Wound Healing: Stimulatory Effects of Omega-3 and Omega-6 Polyunsaturated Fatty Acids in Rats
Jafari Naveh H. R.1, Taghavi M. M.1*, Shariati M.1,2, Vazeirnejad R.3 and Rezvani M. E.4
1Department of Anatomy, School of Medicine, Rafsanjan University of Medical Sciences, Rafsanjan, Iran.
2Department of Anatomy, School of Medicine, Mashhad University of Medical Sciences, Mashhad, Iran.
3Department of Medical society, School of Medicine, Rafsanjan University of Medical Sciences, Rafsanjan, Iran. 4Department of Physiology and Pharmacology, School of Medicine, Rafsanjan University of Medical Science, Rafsanjan, Iran.
Accepted 7 September, 2024
The potential role of omega-3 ( -3) and omega-6 ( -6) fatty acids on wound healing in chronic diabetic diseases is of interest and controversial. In this experimental study, the effect of topical application of fish and corn oils containing -3 and -6 fatty acids on skin wound healing in chronic diabetic rat has been evaluated. Rats were randomly divided into five groups (n = 7). First group was served as normal or control group. In diabetic groups, one group was non-treated group (shame group) and two groups received fish and corn oil (FO-group and CO-group), respectively. The last diabetic group was treated with both fish and corn oil (FCO-group) . Treatment was done from 4 weeks after the induction of diabetes till complete wound healing. All animals were wounded by a 2 cm2 incision in their dorsum. Wound surface area and required time for full healing were measured at various post-operated periods. The histological characteristics were studied by using hematoxilin and Eosin (H & E) method. Our results showed that surface area of wound in FCO- group was lesser than that non-treated group at 11th, 15th and 20th post-operative days significantly. Moreover the percentage of the wound healing in FCO-treated and non-treated groups was 98 and 70% at the 20th day, respectively. Histological studies showed that epidermal growth, cellular diffusion, density of collagen in FCO-group approximately were the same as control group. Topical application of fish and corn oil together may result in an acceleration of skin wound healing in chronic diabetic rats.
Key words: Fish oil, corn oil, wound healing, chronic diabetes.
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (4), pp. 001-010, April, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
Inotropic Activity Assessment of a Newly Synthesized Estradiol Derivative Using Isolated Rat Heart Preparations
Figueroa-Valverde L.1*, Díaz-Cedillo F.2, López-Ramos M.1, García-Cervera E1 and Pool-Gómez E.1
1Laboratory of Pharmaco-Chemistry, Faculty of Chemical Biological Sciences, Universidad Autonóma de Campeche, Av. Agustín Melgar s/n, Col Buenavista C.P.24039 Campeche Cam., México. 2Escuela Nacional de Ciencias Biológicas del Instituto Politécnico Nacional. Prol. Carpio y Plan de Ayala s/n Col. Santo Tomas, México, D.F. C.P. 11340.
Accepted 8 January, 2025
Several studies indicate that some steroid derivatives have inotropic activity; nevertheless, there is scarce information about the effects of the estradiol derivatives at cardiovascular level. Therefore, in this study, estradiol derivative was synthetized with the objective of evaluating its inotropic activity. In this first stage, the Langendorff technique was used to measure perfusion pressure and coronary resistance changes in isolated rat heart in absence or presence of estradiol derivative. In second stage, the inotropic activity of estradiol derivative was evaluated by measuring left ventricular pressure in absence or presence of following compounds; tamoxifen, prazosin, metoprolol, indomethacin and nifedipine. The results showed that the estradiol derivative significantly increase the perfusion pressure and coronary resistance in isolated heart. Additionally, other data indicate that estradiol derivative increase left ventricular pressure in a dose-dependent manner [10-9 to 10 -4 mmol]; nevertheless, this phenomenon was significantly inhibited by nifedipine at a dose of 1 × 10-6 mmol. In conclusion, these data suggest that the estradiol derivative induces positive inotropic activity through of activation the L-type calcium channel.
Key words: Estradiol derivative, Langendorff, inotropic activity.
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-008, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
Regulation of Connexin Expression by Angiotensin Modulators (Losartan and Ramipril) in Vascular Injury
Xujuan Li, Deqiang Li, Jinfeng Duan, Junzhu Chen, Wei Cai* and Voonthow Kok
The First Affiliated Hospital, College of Medicine, Zhejiang University, No.79, Qingchun Road, Hangzhou, Zhejiang Province, P. R. China, 310003.
Accepted 27 July, 2024
Intercellular gap junction (GJ) plays a pivotal role in the proliferation and transformation of vascular smooth muscle cells (VSMCs). This study was designed to test the hypothesis that expressions of the component proteins of gap junctions, connexins40 and 43 (Cx40 and Cx43), are up-regulated in arteries subjected to balloon injury and that this up-regulation can be suppressed by statin therapy. Transmission electron microscopy (TEM) revealed that there were abundant GJ between neointimal SMCs but fewer and smaller GJ after losartan and ramipril treatment. Reverse transcription–polymerase chain reaction and Western blot analysis showed the messenger ribonucleic acid (mRNA) and protein expressions of Cx40 and Cx43 were elevated after injury, and these elevations were suppressed by losartan and ramipril. Immunostaining showed the Cx40 and Cx43 expressions were consistently enhanced in the neointimal area after injury, which was decreased by losartan and ramipril treatment. Balloon injury causes up -regulation of Cx40 and Cx43 in neointimal SMCs. angiotensin -converting enzyme inhibitors (ACEIs) and AT1 antagonist losartan can reduce the proliferation of SMCs, suggesting the rennin-angiotensin system (RAS) system plays an important role in the remodeling of GJ in the VSMCs under pathological conditions.
Key words: Vascular smooth muscle cell, gap junction, connexin, balloon angioplasty, statin.
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-005, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
The Influence of Chloroquine on Chlorpropamide Pharmacokinetics in Healthy Volunteers
Danlami U.1*, Odunola M. T.2, Magaji G.2 and Thomas S. A.1
1Sheda Science and Technology Complex (SHESTCO), P.M.B. 186, Garki, Abuja, Nigeria. 2Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ahmadu Bello University, Zaria, Nigeria.
Accepted 07 October, 2024
The effect of chloroquine on the pharmacokinetics of chlorpropamide was investigated in human volunteers. The study was carried out by administering chlorpropamide alone on healthy volunteers, and then chlorpropamide was co-administered with chloroquine. High performance liquid chromatography (HPLC) was used for the analysis of the plasma levels of chlorpropamide. The solvent used was acetonitrile/water (6:4) at pH 6.7. Ultrasphere ODS column, 4.6 × 25 cm, USA was used. The result from the chlorpropamide plasma level analysis shows that the absorption half-life (t1/2a) and the time to maximum peak concentration (tmax) increased by 10% (P < 0.04) and 20% (P < 0.01), respectively. The absorption rate constant (Ka) and the maximum concentration (Cmax) decreased by 30 and 16% (P < 0.02), respectively. The area under the curve (AUC0-168) decreased significantly by 50% (P < 0.03). The plasma clearance of chlorpropamide increased significantly by 86% (P < 0.01).The volume of distribution (Vd) and the elimination half life(t1/2el) decreased by 10%(p<0.03) and 47% (P < 0.01), respectively, while the elimination constant (kel) increased by 100% (P < 0.02). Co-administration of chlorpropamide with chloroquine significantly (P < 0.05) impaired the absorption and elimination of chlorpropamide.
Key words: Pharmacokinetics, chlorpropamide, chloroquine, high performance liquid chromatography, half-life, absorption rate constant, elimination constant.
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-008, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
Transdermal Delivery of Ligustrazine Phosphate Using Microemulsions: A Formulation Investigation
Ying Cui1,2, Lingzhi Li1,2, Jun Gu1, Ting Zhang3* and Li Zhang1
1Department of Medicine Chemistry, Logistics University of Chinese People’s Armed Police Forces, Tianjin 300162,
P. R. China.
2Tianjin Key Laboratory of Occupational and Environmental Hazards Biomarkers, Tianjin 300162, P. R. China.
3Department of Pharmacy, Xiangya Hospital, Central South University, Changsha 410008, P. R. China.
Accepted 10 January, 2025
Ligustrazine phosphate is commonly used as an efficient drug to treat a variety of cardiovascular disorders with frequent administration for a short biological half-life. The purpose of the present study was to investigate a microemulsion system for transdermal delivery of ligustrazine phosphate for the convenient, efficient and safe administration. The existence regions of microemulsions containing isopropyl myristate, labrasol, plurol oleique® and water were investigated in pseudo-ternary phase diagrams, according to which microemulsion vehicles were prepared to observe average diameter, pH value, stability and evaluate respective effect of each component on percutaneous delivery in vitro. The prepared microemulsions had average diameters ranging from 32.1 to 108.7 nm, mild pH values and suitable stability. The optimized microemulsion with permeation flux of 41.01 g/cm2/h across rat skin in vitro, showed no obvious irritation on back skin of rabbits. The results indicated that the studied microemulsion system might be a promising vehicle for transdermal delivery of ligustrazine phosphate.
Key words: Microemulsion, transdermal delivery, ligustrazine phosphate.
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-007, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
Bioavailability Study of Four Aspirin Brands Marketed in Nigeria: An In Vitro-In Vivo Correlation Analysis
Bamigbola E. A.1*, Ibrahim M. A.2, Attama A. A.3 and Uzondu A. L.1
1Department of Pharmaceutics and Pharmaceutical Microbiology, Faculty of Pharmacy, Madonna University,
Elele, Rivers State, Nigeria.
2Department of Pharmaceutics and Pharmaceutical Technology, University of Jos, Plateau State, Nigeria.
3Department of Pharmaceutics, University of Nigeria, Nsukka 410001, Enugu State, Nigeria.
Accepted 30 January, 2025
The study investigated the possibility of developing an in vitro – in vivo correlation for four commercial brands of aspirin tablets using USPXXI rotating basket apparatus and urinary excretion profiles from eight human volunteers. Various dissolution and pharmacokinetic parameters were obtained for all the brands. Significant rank order correlations were observed between all the in vitro dissolution parameters such as percent dissolved at 30 min, dissolution rate constants (k) and time for 50% dissolution (DT50%) and all the in vivo bioavailability parameters such as cumulative amount excreted up to 8 h (E8), maximum excretion rate (dE/dt)max and time for maximum excretion rate (Tmax). However, no correlation could be established between the cumulative amount excreted up to 24 h (E24) and any of the in vitro dissolution parameters. Moreover, statistical analysis showed no significant inter-subject variation among the subjects that participated in the experiments.
Key words: Aspirin tablets, dissolution rate constant, maximum excretion rate, cumulative amount excreted, in vitro-in vivo correlation (IV-IVC).
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-010, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Review
Exploring the Phytochemical Profile and Therapeutic Potential of Kaempferia galanga L.
Muhammad Ihtisham Umar1*, Mohammad Zaini Bin Asmawi1, Amirin Sadikun2, Rabia Altaf1 and Muhammad Adnan Iqbal3
1Department of Pharmacology, School of Pharmaceutical Sciences, University Sains Malaysia,
11800 Pulau Pinang Malaysia.
2Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, University Sains Malaysia, 11800 Pulau
Pinang Malaysia.
3School of Chemical Sciences, University Sains Malaysia, 11800 Pulau, Pinang Malaysia.
Accepted 25 January, 2025
Kaempferia galanga L. (KG), commonly known as cekor is one of those precious medicinal herbs of Zingiberaceas that are still included in un-utilized herbs inspite of the variety of useful pharmacological properties it possesses. Extracts of KG have anti-inflammatory, analgesic, nematicidal, mosquito repellent, larvicidal, vasorelaxant, sedative, antineoplastic, antimicrobial, anti-oxidant, antiallergic and wound healing properties. Here, we have reviewed all the reported pharmacological properties of this valuable herb with an intention to highlight the effectiveness and potentials of this herb. Ethyl-p-methoxycinnamate and ethyl-cinnamate are found to be the most vital constituents responsible for most of these pharmacological properties. Antinociceptive effect of KG extracts is comparable with that of aspirin whereas its nematicidal effect is even more potent than Carbofuran and metham sodium.
Key words: Antinociceptive, nematicidal, cekor.
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-008, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
The Effects of Baicalin on Lipopolysaccharide-Induced Uterine Endometrium Damage and Implantation Failure in a Murine Model
Yantao Zhao1, Yongzhan Bao1, Wanyu Shi1,2, Xiaodan Wang2 and Xiuhui Zhong1,2*
1College of Veterinary Medicine, Agricultural University of Hebei, Baoding 071001, China.
2Institute of Traditional Chinese Veterinary Medicine, Agricultural University of Hebei, China.
Accepted 4 January, 2025
The objective of this study is to investigate the protective effects of baicalin and to elucidate its immunological modulation at maternal-fetal interface. Lipopolysaccharide (LPS) was given via intraperitoneal injection to induce embryo implantation failure in mice which received baicalin at days 0.5 to 3.5 of gestation. The IFN- /IL-10, nitric oxide synthase (NOS) activities of uterine and endometrial tissues in each group (n = 16) were detected by ELISA, respectively. The ratio of IFN- /IL- 10 and NOS activities increased significantly in the uterus of LPS-induced mice implantation failure and endometrial cells of LPS interference. In the baicalin pretreated mice followed by LPS administration, the ratio of IFN- /IL-10 and NOS activities were normalized by the middle dose baicalin to the control level, significantly lower than LPS treatment group. The same results were received in vitro study of LPS interference endometrial cells. The results indicate that baicalin has protective effects through inhibiting excessive IFN- and NO production to modulate the immunological balance at maternal-fetal interface.
Key words: Baicalin, lipopolysaccharide (LPS), implantation failure, IFN- , IL-10, nitric oxide (NO).
International Journal of Pharmacy and Pharmacology ISSN 2326-7267 Vol. 14 (3), pp. 001-005, March, 2025. Available online at www.internationalscholarsjournals.org © International Scholars Journals
Full Length Research Paper
Evaluating the Antiplasmodial Activity of Sphenocentrum jollyanum Pierre Leaf and Root Extracts In Vivo
O. S. Olorunnisola* and A. J. Afolayan
School of Biological Sciences, University of Fort Hare, Alice 5700, South Africa.
Accepted 16 January, 2025
Methanolic leaf and root extracts of Sphenocentrum jollyanum Pierre were tested in vivo for anti-malarial activity in Swiss albino mice inoculated with chloroquine resistant Plasmodium berghei NK 67 strain. The two extracts exhibited a significant (p>0.05) dose dependant anti- plasmodial activities in isolation and when combined in the 4-days curative standard test with a high mean of survival time. Although, the standard drug, Arthemether - lumefartrin, showed the highest antimalaria potency (81.4%), those of the leaf (74.4%) and root extracts (54.1%) in isolation and combination (63.4%) compared favorably. The leaf extract demonstrated higher antimalarial potency than the root or combination. The two extracts also produced a significant (p>0.05) positive effect on the weight and hematology values in the treated animals. Phytochemical screening of the plant (leaf and the root extracts) reveals the presences of flavonoids, steroids, terpenoids, tannins and alkaloids. The anti-plasmodia activity of these plant extract might be attributed to these phytochemicals compounds. The results showed that the leaf and root of S. jollyanum possesses an anti-malarial activity which was effective against chloroquine resistance strain. This work has validated the traditional uses of S. jollyanum root extract in the treatment of malaria and also reported for the first time the anti-malarial property of the S. jollyanun leaf extract.
Key words: Sphenocentrum jollyanum, Plasmodium berghei, Arthemther lumefartrin, hematological parameter, anti-plasmodium.
