Advances in Pharmacological and Pharmaceutical Sciences最新文献

A safer alternative made of plant extracts is needed, as evidenced by the negative effects of using synthetic sunscreen. Antioxidant properties of plants with high phenolic content have been reported. The goal of this research was to ascertain the phenolic content and antioxidant characteristics of ethanolic extracts made from grape and olive leaves under various extraction settings. The extracts were subjected to both qualitative and quantitative analyses using HPLC. Soxhlet extraction with 80% ethanol (v/v) as the solvent produced a result that was satisfactory. Four components of grape leaf extract and one component of olive leaf extract were identified. Expressed as gallic acid equivalents (GAEs), the total phenolic content (TPC) of the samples, as determined by using the Folin-Ciocalteu's reagent, ranged from 38.39 to 72.78 mg/g dry extract of olive and 65.918-132.7 mg/g dry extract of grape. An ethanolic extract of Salmoni (grape leaves) had the highest TPC (132 mg GAE/g), while an ethanolic extract of Zaity (olive leaves) had the lowest (72.66 ± 0.46 GAE/g). The Folin-Ciocalteu method proved the existence of antioxidants in the plant. By scavenging free radicals such as DPPH (2,2-diphenyl-1-picrylhydrazyl), the antioxidant capacity of the plant extracts was determined. Next, the ethanolic extracts of various cultivars of grape and olive leaves were analyzed to determine their sun protection factor (SPF) value. It was 28.8 and 29.96 for grape leaf extract and olive leaf extract, respectively.

Compared with the use of a single herb alone, herb combinations can significantly increase their effectiveness in treating various diseases. The objective of this research was to determine the appropriate proportions of Garcinia mangostana (GM), Curcuma comosa (CC), and Acanthus ebracteatus (AE) to enhance their antioxidant and anti-inflammatory properties. The study employed computer modeling (in silico) and laboratory testing (in vitro). The optimal levels of phenolic and flavonoid compounds were achieved with a ratio of 15 parts GM, 5 parts CC, and 10 parts AE. In contrast, the 10 : 15 : 5 ratio resulted in the highest antioxidant activity, reducing DPPH radicals by 80.33% and ABTS radicals by 92.20%. The ratio had a synergistic effect and was within the safe range, ranging from 82.97 to 147.04 µg/mL. The ratio of 5 : 10 : 15 had the greatest anti-inflammatory effects, with an exceptional activity level of 98.86%. It effectively suppressed 23 genes or proteins, including the prominent NFE2L2 gene, and had a synergistic effect. This combination effectively inhibits inflammation (IC₅₀: 12.05 µg/mL) and is safe for macrophages at concentrations up to 50 µg/mL. These findings emphasize the potential of these herbal mixtures for antioxidant and anti-inflammatory applications.

The Trikaysornmas formula (TKM) represents a prevalent Thai traditional remedy utilized extensively in Thailand. Its traditional uses include appetite enhancement, functions as a nourishing tonic, and exhibits adaptogenic properties. Comprising Aegle marmelos fruit, Nelumbo nucifera stamen, and Jatropha multifida bark, this formula embodies the synergy among these three herbs. The objective of this study was to optimize the extraction method, determine the active compounds in the TKM, and evaluate its antioxidant activity. The optimization of the extraction method for this formula was studied using an experimental design. Phytochemical components such as total phenolics, total flavonoids, total carotenoids, and total alkaloids were assessed utilizing a colorimetric method. Antioxidant activities were assessed through DPPH free radical scavenging, ABTS radical cation decolorization, oxygen radical absorbance capacity, ferric reducing antioxidant power, metal chelating activity, and lipid peroxidation assay. For the analysis of active constituents in the formula, gallic acid, kaempferol-3-o-glucoside, imperatorin, vitexin, and scopoletin, a validated reversed-phase column high-performance liquid chromatography (HPLC) method was developed. The total active contents including phenolic, flavonoid, carotenoid, and alkaloid compounds were found in the formula. The developed HPLC method exhibited reliable results in all validation parameters. TKM demonstrated antioxidant activity in the models used in this research. The findings from this study can serve as valuable tools for standardization and quality control measures. Additionally, they can contribute to maximizing the possibilities inherent in this traditional Thai formulation.

Colitis-associated colon cancer (CAC) arises from prolonged inflammation of the inner colon lining. An alternative approach to treating or preventing CAC involves the use of natural products such as Manilkara zapota (L.) P. Royen or M. zapota, which has been studied for its medicinal and pharmacological properties. Previous research has demonstrated the anticancer effects of M. zapota leaf aqueous extract (MZLAE) on colon cancer cells. However, no animal study has investigated the effects of MZLAE on CAC. Therefore, this study aimed to assess the potential anti-inflammatory effects of MZLAE on CAC in mice. In the present study, CAC was induced using azoxymethane (AOM) and dextran sodium sulphate (DSS). The mice were randomly assigned into five groups: (a) normal, (b) AOM/DSS, (c) AOM/DSS + 50 mg/kg MZLAE, (d) AOM/DSS + 100 mg/kg MZLAE, and (e) AOM/DSS + 200 mg/kg MZLAE. Various parameters including disease activity index (DAI), colon length and weight, reactive oxygen species (ROS), superoxide, superoxide dismutase (SOD), histopathological assessment, and proinflammatory cytokines expression were analysed. The results indicated that MZLAE improved DAI scores, colon length, colon histological dysplasia and inflammation scores, and SOD level, while also reducing ROS production and expression of proinflammatory cytokines (tumour necrosis factor-alpha (TNF- α) and interleukin 6 (IL-6)). In conclusion, this study suggests that MZLAE may serve as a promising source of antioxidants and anti-inflammatory agents for alleviating CAC.

The medicinal value of Centella asiatica leaf extract was evaluated as an alternative treatment. The chemical composition of the leaf extract was analyzed, and the biological activities were determined. High-performance liquid chromatography coupled with a photodiode array detector (HPLC-PDA) was used to identify the asiatic acid, madasiatic acid, and madecassic acid/Brahmic acid isolated from the ethanolic extract. The plant extract at 25 mg/disk was found to inhibit both Gram-positive and Gram-negative pathogenic bacteria by the agar disk diffusion test. The MIC and MBC of the ethanolic extracts were better than those of the aqueous extracts. The ethanolic extracts showed antibacterial activity against Gram-positive bacteria with MICs and MBCs ranging from 1.024 to 2.048 mg/mL and 2.048 to 4.096 mg/mL, respectively. The remarkable antibacterial activities were observed against S. mutans. The ethanolic extract at a concentration of 1/2 × MIC exhibited the inhibition effect on S. mutans biofilm formation like the activity of 0.2% chlorhexidine and significantly modified hydrophobicity of the bacterial cell surface. The effects were confirmed via molecular docking analysis. The binding affinities of asiatic acid, madecassic acid, and madasiatic acid with glucosyltransferase C (GtfC) of S. mutans exhibited superior strength in comparison with alpha-acarbose and chlorhexidine. Moreover, the nitric oxide (NO) secretion of RAW247.6 cells was determined after treating the cells with concentrations of the extract. The C. asiatica ethanolic extract can inhibit the secretion of NO, which can inhibit the inflammatory process. The findings indicate the applications of the C. asiatica ethanolic extract as the alternative anti-S. mutans agent and could be used for further formulation for the treatment and prevention of dental diseases and inflammatory injury in the oral cavity.

Asiatic acid (AA) has previously shown its neuroprotective effects, but low oral bioavailability limits its penetration into the brain. This study aimed to investigate the effect of intranasal AA administration in mice with memory dysfunction induced by scopolamine. Mice received either intranasal AA (INAA), oral AA (POAA3 or POAA30), or donepezil, followed by scopolamine for 10 days. Morris water maze (MWM) was performed on days 0-5, 30 min after treatment. Locomotor activity was conducted on day 6 followed by brain collection. In MWM, INAA treatment had significantly reduced escape latency on days 2-4, while POAA3 decreased escape latency on day 3 and POAA30 and donepezil decreased escape latency on day 4. INAA inhibited acetylcholinesterase activity, increased catalase protein expression, and decreased malondialdehyde levels in the brain tissue. Therefore, intranasal administration of AA produced a rapid onset in the protection of learning and memory deficits induced by scopolamine through acetylcholinesterase inhibition and antioxidant effect.

Curcumin has shown beneficial effects on pulmonary diseases with chronic inflammation or abnormal inflammatory responses, including chronic obstructive pulmonary disease, asthma, and pulmonary fibrosis. Clinical applications of curcumin are limited due to its chemical instability in solution, low water solubility, poor oral bioavailability, and intestinal and liver first-pass metabolism. Pulmonary delivery of curcumin can address these challenges and provide a high concentration in lung tissues. The purpose of the current work was to prepare a novel inhalable dry powder of curcumin nanocrystals without added excipients using electrospray drying (ED) with improved dissolution and aerosolization properties. ED of curcumin was performed at 2 and 4% w/v concentrations in acetone. Physicochemical properties of the formulated powders were evaluated by powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), density and powder flow measurements, and in vitro dissolution. The in vitro deposition studies were conducted using next-generation impactor (NGI) and aerosol performance and aerodynamic particle size parameters were calculated for prepared formulations. ED could produce agglomerates of nanocrystals with a size of about 500 nm at an acceptable yield of about 50%. PXRD and FTIR data revealed that prepared nanocrystals were in a stable crystalline state. The bulk and tapped density of prepared agglomerates were in the range appropriate for pulmonary delivery. Formed nanocrystals could significantly improve the dissolution rate of water-insoluble curcumin. The optimized formulation exhibited acceptable recovered dose percentage, high emitted dose percentage, optimum mean mass median aerodynamic diameter, small geometric standard deviation, and high fine-particle fraction that favors delivery of curcumin to the deep lung regions. The ED proved to be an efficient technique to prepare curcumin nanocrystals for pulmonary delivery in a single step, at a mild condition, and with no surfactant.

Apricot (Prunus armeniaca L.) kernels have been widely employed in phytomedicine for treating different ailments. This study aims to unveil the phytochemical composition by HPLC-ESI-MS, in vitro antioxidant activity, and examine certain pharmacological effects of the hydro-ethanolic extract from bitter apricot kernels (BAK). Obtained results indicated that the BAK extract presents a content of 4.58 ± 0.15 mg GAE/g extract of TPA and 1.68 ± 0.09 mg QUE/g extract of TFA, respectively. HPLC-ESI-MS analysis discovered the presence of 17 phenolic compounds including phenolic acids and flavonoids like 3,4-dihydroxybenzoic acid, gallic acid, caffeic acid, (+)-catechin, epicatechin, and others, with associated antioxidant power. Regarding the studied potential pharmacological effects, notable analgesic activity at a dosage of 100 mg/kg BW was recorded with 63.46% protection. In the anti-inflammatory test, significant inhibition was observed after 6 hours of treatment (77.4%) compared to untreated animals. Moreover, the daily application of ointment formulated with 10% BAK extract resulted in a remarkable healing of wounds and burns in rats. These findings underscore the increasing evidence supporting the potential use of apricot kernel extracts in treating various diseases.

The aim of the present study was to assay the in vivo anthelminthic activity of Anogeissus leiocarpa (Al) family of the Asteraceae and Adansonia digitata (Ad) family of Malvaceae leaf powder against the nematode Haemonchus contortus (Hc) in sheep. Twenty-eight sheep were artificially infected with 3000 Infective larvae (L3) of Hc and divided into four groups. Groups 1 and 2 received 3.2 g/kg of Ad and Al leaf powder according to the body weight for three days by oral route. This treatment was repeated after 14 days. Group 3 received albendazol 5 mg/kg and group 4 received water. The treatment was repeated 14 days later. Examination of faecal samples, packed cell volume and biochemical analyses and necropsy were carried out to determine egg counts, worm burdens, and reduction in worm fecundity and changes in blood parameters. The results showed a reduction in egg excretion of 72.22% and 88.49%, respectively, with Al and Ad leaf powder. Egg laying of adult female worms was reduced by 55.22% and 64.96% with Ad and Al, respectively. FAMACHA score (≤2 in the treated animals) and packed cell volume were improved with Ad and Al. The results of this study revealed that Ad and Al powder may be used as an alternative anthelminthic to control haemonchosis in small ruminants.

Background: Sitagliptin functions similarly to GLP-1RAs by incretin and insulin secretion and has a renoprotective effect. Diabetic kidney disease (DKD) is a kidney complication that increases the mortality rate in type 2 diabetes mellitus (T2DM) patients. The important parameters that predict appropriate sitagliptin treatment are known as factors. This study aimed to assess factors that correlated with the renoprotective effect of sitagliptin in patients with T2DM.

Methods: This retrospective study collected data from a tertiary hospital in Thailand. All T2DM patients who were treated with sitagliptin and had complete data were recruited to analyze the outcome. The primary outcome was a correlation between demographics, laboratory data, and kidney outcome. The secondary outcome was the different laboratory results between pre- and posttreatment of patients treated with sitagliptin.

Results: The number of patients who were treated for T2DM with sitagliptin was 191. Only 102 patients had complete laboratory parameters. Results showed a positive correlation between baseline FBS, Hb_A1c, and Scr change (p value = 0.042 and 0.005) at 6 months and baseline age, TG, and Scr change (p value = 0.010 and 0.022) at 18 months; while a negative correlation was observed between baseline FBS, Hb_A1c, and eGFR change (p value = 0.017 and 0.007) at 6 months and baseline age and eGFR change (p value = 0.010) and between HDL-cholesterol and Scr change at 18 months (p value = 0.044). The eGFR stage 1 subgroup showed a positive correlation between baseline Hb_A1c and Scr change (p value <0.001) and baseline DM duration and eGFR change (p value = 0.004). Moreover, sitagliptin showed statistically significant FBS, Hb_A1c, LDL-cholesterol, and TC reduction. Furthermore, HDL-cholesterol showed statistically significant elevation.

Conclusion: FBS, HbA1c, and age were factors that correlated with the renoprotective effect of sitagliptin. The eGFR ≥90.00 ml/min/1.73 m² patients group showed a duration of DM in which factors correlated with renoprotective effect. Moreover, sitagliptin also can improve glucose levels and lipid profile.