Journal of Advanced Pharmaceutical Technology & Research最新文献

Rhododendron cowanianum is an endemic shrub of Nepal. This study investigated the phytochemical profile along with the antioxidant, antimicrobial, and cytotoxic properties of its methanolic extract. Qualitative phytochemical screening showed the presence of alkaloids, phenols, flavonoids, tannins, terpenoids, steroids, and carbohydrates. Quantitatively, the extract contained 105.4 ± 3.42 mg gallic acid equivalent/g of phenolics and 881.2 ± 5.70 mg quercetin equivalent/g of flavonoids. The extract showed the antioxidant IC₅₀ values of 97.77 μg/mL and 39.63 μg/mL by 2,2-diphenyl-1-picrylhydrazyl and 2,2'- azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) methods. It showed the zones of inhibition of 19.0 mm, 19.33 mm, 14.83 mm, and 10.67 mm and minimum inhibitory concentrations of 156.25 μg/mL, 312.5 μg/mL, 156.25 μg/mL, and 312.5 μg/mL against Bacillus subtilis, Enterococcus faecalis, Staphylococcus aureus, and Salmonella enterica, respectively. The minimum bactericidal concentration for S. enterica was 1.25 mg/mL and 0.625 mg/mL for the other three strains. The high-resolution liquid chromatography-mass spectrometry profiling of crude extract identified diverse classes of bioactive compounds, including lucidenic acid A, isopimaric acid, euphorin, and ganoderic acid F, which are linked with different pharmacological properties. This study profiles the phytochemicals of R. cowanianum and integrates them with bioactivity, highlighting its potential as a medicinal plant.

[This corrects the article on p. 171 in vol. 16, PMID: 41234347.].

CD4⁺ T-cells and interleukin-2 (IL-2) are key regulators of the immune response, particularly during Salmonella infections. Saurauia vulcani Korth., commonly referred to as pirdot, is a traditional medicinal plant rich in flavonoids known for their anti-inflammatory effects. This study aimed to evaluate the impact of ethanol extract of pirdot leaves on hepatic CD4⁺T-cell expression and serum IL-2 levels in rats challenged with Salmonella typhimurium. A posttest-only control group design was used with 32 male Wistar rats divided into four groups: Group I (normal/K0), Group II (negative/Kneg), Group III (positive control, Imboost^® 22.5 mg/kg BW), and Group IV (treatment, pirdot extract 500 mg/kg BW). On day 4, all groups except the normal control were infected with S. typhimurium. At day 14, blood and liver samples were collected. Serum IL-2 concentrations were measured, and liver tissues were examined histologically and assessed for CD4⁺ T-cell immunoreactivity score (IRS) by immunohistochemistry (IHC). Kruskal-Wallis analysis followed by Mann-Whitney test showed that the group given pirdot extract had the highest IL-2 levels (2.23 ± 0.18 ng/ml), followed by positive (1.86 ± 0.33 ng/ml), normal (1.71 ± 0.40 ng/ml), and negative (1.64 ± 0.28 ng/ml) with a significant difference (P = 0.009). Then, histopathology scores were observed for hydropic degeneration, necrosis, inflammation, granuloma formation, and portal triad damage in all groups, followed by calculating the CD4⁺ T-cell IRS by Immunohistochemistry (IHC) examination. The results showed statistically significantly different values between all groups (P = 0.004). The ethanol extract of pirdot leaves at a dose of 500 mg/kg BW was found to enhance CD4⁺ T-cell expression and elevate serum IL-2 levels, indicating its potential as an immunomodulatory agent against Salmonella infection.

Annona squamosa contains some secondary metabolites and has significant biological activities, including antioxidant. The toxicity of n-hexane and dichloromethane (DCM) extracts from A. squamosa leaves was evaluated using the Brine Shrimp Lethality Test, while their antioxidant activity was evaluated through the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The antioxidant activity results showed inhibition concentration 50 (IC₅₀) values of 152.76 ppm for the n-hexane extract and 57.87 ppm for the DCM extract. Toxicity tests of both extracts had lethal concentration 50 (LC₅₀) values below 1000 ppm that indicated that the extracts are considered toxic. The results of fraction testing showed that fraction F6 was the most active as an antioxidant, with an IC₅₀ of 86.49 ppm, and F5 had the highest toxicity with an LC₅₀ of 75.30 ppm. Further gas chromatography-mass spectrometry (GC-MS) analysis of the most active extract and fraction identified 1,2,3,4-tetrahydroisoquinoline and benzenepropanoic acid derivatives, which are suggested to contribute to the observed antioxidant and toxicity-related activities.

Male fertility preservation can be achieved through assisted reproductive technology, in which sperm cryopreservation plays an essential role. However, the freezing-thawing process induces cellular stress, primarily through intracellular ice crystal formation, which damages membranes, organelles, and exacerbates osmotic and oxidative stress. This study aims to determine whether sperm cryopreservation and preparation affect sperm concentration and motility, cryosurvival rate (CSR), DNA fragmentation, and ultrastructure after thawing. A total of 10 human sperm samples were rapidly frozen in cryovials, with prefreeze and postthaw analyses compared against fresh controls, assessing sperm parameters, DNA fragmentation, and ultrastructure (scanning electron microscope). Statistical analysis included paired comparisons for two groups and multigroup tests with post hoc analysis. CSR was compared to 100% using a one-sample t-test. P < 0.05 was considered statistically significant. Sperm concentration decreased both after washing and after thawing compared to before freezing, while motility increased after washing, but it significantly decreased after thawing. The sperm motility result was confirmed by a significantly reduced CSR and DNA fragmentation index, which significantly increased at after thawing. Ultrastructure analysis also revealed more sperm damage after thawing. Cryopreservation impairs sperm motility, CSR, DNA fragmentation, and ultrastructure. Since in vitro fertilization requires sperm with good morphology and motility, new strategies are needed to minimize cryodamage.

Studies have shown onion peels to have potential anticancer effects on prostate cancer (PCa) development but with limited understanding of the underlying mechanisms. Therefore, this study aimed to explore potential bioactive compounds, molecular mechanisms, target proteins, and synergistic interactions of onion peels against PCa development. This study employed literature searching and pharmacokinetic property prediction to identify candidate compounds in onion peels. Swiss Target Prediction and Similarity Ensemble Approach were used to screen for potential compounds' targets, while GeneCards was searched for PCa related targets. Ten candidate compounds were identified, and target screening yielded 117 intersecting targets, used to construct protein-protein interaction (PPI) networks. Topological parameter analyses identified 21 core targets, while computationally enriched pathways include endocrine resistance, HIF 1 and PI3K-AKT signaling pathway, PCa, and pathways in cancer. Molecular docking was performed for all candidate compounds paired with each core target and revealed RAC alpha serine/threonine protein kinase 1 as the primary target, involved in all five highest affinity pairs: Quercetin, morin, isorhamnetin, kaempferol, and epicatechin. Potential essential amino acid residues included leucine 264, tryptophan 80, lysine 268, valine 270, threonine 211, and leucine 210. In conclusion, these findings provide computational evidence supporting the predicted underlying mechanisms, bioactive compounds, and targets potentially associated with the anticancer effects of onion peels in PCa development, although further experimental validation may be necessary.

Owing to less efficiency of currently available antiepileptic medications, research is continuing toward the most effective solution. It was observed that the antidiabetic drug metformin (MET) is getting more attention in the modern world due to its good anti-inflammatory and neuroprotective characteristics, and this is the main purpose of this investigation for assessing the antiepileptic impact of MET. In this study, we sought to assess MET's antiepileptic effectiveness in a model of mice by examining its effects on the duration, frequency, and intensity of seizures. Furthermore, we aimed to figure out the neurological mechanisms behind MET's antiepileptic effects. Six groups of 48 mice were allocated. The first group was administered normal saline (vehicle group), while in the second group, to induce seizure, administered pentylenetetrazol (PTZ; 45 mg/kg). Valproic acid (300 mg/kg) was given to the third group as the positive group. The remaining groups were injected with prophylactic doses of MET at 200, 250, and 300 mg/kg for 7 days. After 30 min of the last dose, Groups 3, 4, 5, and 6 were induced by PTZ. The results showed that MET exerted antiepileptic and neuroprotective effects across behavioral, biochemical, and mortality parameters. The mortality rate, the length of generalized tonic-clonic seizures, the frequency of seizures, and the seizure scores (P < 0.001) were all substantially reduced by the MET. Additionally, MET raised levels of peroxisome proliferator-activated receptor gamma, nuclear factor-kappa B, and matrix metalloproteinase 2 (P < 0.001) while lowering blood levels of caspase-3 (P < 0.001). Findings revealed MET's antiepileptic role, lowering both seizure activity and mortality in the target mouse.

Burns are traumatic injuries that compromise the skin's natural barrier, initiating a complex process of inflammation, proliferation, and tissue maturation. Second-degree burns, in particular, cause extensive tissue damage and require effective treatments that both accelerate healing and reduce pain. Traditionally, the Karo community has used Bangun-Bangun (Coleus amboinicus) leaves for wound care, owing to their analgesic and anti-inflammatory properties. This study aimed to investigate the therapeutic potential of a 10% Bangun-Bangun leaf extract (BBE) gel in managing pain and enhancing wound healing in Wistar rats with second-degree burns. It was hypothesized that BBE gel would provide better pain relief and faster recovery compared to standard therapies. A total of 54 Wistar rats were divided into three main groups: Base gel (negative control), Bioplacenton® (positive control), and 10% BBE gel (treatment). Each group was further separated into subgroups based on treatment duration (days 1-3, 1-14, and 1-21). Treatments were administered twice daily for 21 days. Pain levels were measured using a standard pain scale, whereas leukocyte migration was assessed through hematoxylin and eosin staining. Data were analyzed using SPSS with one-way analysis of variance and Bonferroni post hoc tests for normally distributed data, whereas nonparametric data were evaluated with the Kruskal-Wallis test. Pain reduction in the BBE gel group was not significantly different from Bioplacenton® (P = 0.139). However, rats treated with BBE gel (Group-III) demonstrated significantly lower leukocyte counts compared to controls (P = 0.010 for Group-I; P = 0.006 for Group-II), indicating improved inflammation control. Macroscopically, Group-III exhibited the fastest wound closure. A 10% BBE gel may serve as a promising, natural topical agent for second-degree burns by regulating inflammation and promoting healing. Further studies are required to explore its molecular mechanisms and safety profile.

Oxidative stress and inflammation contribute to liver damage from xenobiotics, leading to chronic diseases. The ethanolic extract of the Benjakul remedy (BJE), a traditional Thai medicine, is recognized for its potential antioxidant and anti-inflammatory effects, though scientific validation is limited. This study assessed BJE's antioxidant effects against various radicals using chemical and cellular assays, evaluated its anti-inflammatory effects by measuring inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) levels, and determined protective effects by evaluating cell viability and oxidative damage. Total phenolic content was measured colorimetrically, and compounds were identified using liquid chromatography combined with electrospray ionization quadrupole time-of-flight mass spectrometry. BJE significantly scavenged synthetic radicals, nitric oxide radicals, and lipid radicals, with IC₅₀ values ranging from 28.76 to 113.46 μg/mL, and diminished ferrous ions with an IC₅₀ value of 1.48 ± 0.09 mg/mL. Furthermore, BJE potently neutralized superoxide anions and nitric oxide radicals within cells, yielding IC₅₀ values of 44.43 ± 6.79 and 15.89 ± 0.93 μg/mL, respectively. BJE reduced iNOS expression by 90% and COX-2 by 60% in a dose-dependent manner. BJE protected liver BNL CL.2 cells from oxidative stress and inflammation induced by pyrogallol, improving cell viability, decreasing oxidative damage, and restoring critical antioxidant enzyme activities. BJE contained 6-gingerol, alkaloid amides, and nonalkaloid amides. This study marks the antioxidant and anti-inflammatory effects of BJE at the molecular levels.

Gentamicin, an aminoglycoside antibiotic, induces nephrotoxicity mainly through oxidative stress. This study evaluated the nephroprotective potential of lercanidipine, a calcium-channel blocker, against gentamicin-induced renal injury in rats. Adult Sprague-Dawley rats were randomly divided into four groups: control, lercanidipine (3 mg/kg/day, p.o.), gentamicin (50 mg/kg/day, i.m.), and a combination group pretreated with lercanidipine for 5 days followed by concurrent gentamicin for 5 days. Serum urea, creatinine, sodium (Na⁺), and potassium (K⁺) were determined, and kidney homogenates were analyzed for malondialdehyde (MDA), glutathione (GSH), and superoxide dismutase (SOD). Gentamicin treatment produced marked renal dysfunction, with elevated serum urea and creatinine, increased Na ⁺ by 29%, and decreased K ⁺ by 27.5% relative to control, accompanied by a 37% reduction in urine volume. Co-treatment with lercanidipine restored electrolyte balance, lowering Na ⁺ by 20% and raising K ⁺ by 27% compared with gentamicin alone, while increasing urine volume by 42%. Lercanidipine also markedly attenuated oxidative stress, reducing MDA by about 65% and increasing SOD and GSH activities by approximately 183% and 140%, respectively, relative to gentamicin alone. These findings demonstrate that lercanidipine significantly protects against gentamicin-induced nephrotoxicity by improving renal function, restoring electrolyte homeostasis, and enhancing the antioxidant defence system.