Phy-Blica-D is a traditional Thai polyherbal formula that has reduced oxidative stress in non-communicable diseases. However, evidence supporting the gastroprotective effects of Phy-Blica-D has not been previously reported. Therefore, this study aimed to evaluate the gastroprotective effects of Phy-Blica-D against gastric ulcers in rats and investigate the potential underlying mechanism. To estimate the possible mechanisms of action, we examined the levels of oxidative stress markers, such as reactive oxygen species (ROS) and malondialdehyde (MDA), as well as antioxidant enzymes, including catalase (CAT), superoxide dismutase (SOD), and glutathione (GSH). According to our results, rats treated with only 80% ethanol (vehicle group) exhibited significant increases in their ulcer area and ulcer index (UI). Moreover, the levels of ROS and MDA markedly increased in the vehicle group compared with the normal control group. Daily oral administration of Phy-Blica-D (500 and 1000 mg/kg) for 7 days not only significantly decreased the ulcer area and UI, but also remarkably decreased the ROS and MDA levels in gastric tissue. Gastric ulcers induced by ethanol had significantly decreased antioxidant enzyme activities (CAT and SOD) and non-enzymatic antioxidant (GSH), whereas pretreatment with Phy-Blica-D significantly improved the activities of CAT, SOD, and GSH. Moreover, after exposure to ethanol, the rats exhibited a significantly increased level of inducible nitric oxide synthase (iNOS), which was reduced after treatment with Phy-Blica-D. These findings suggest that Phy-Blica-D potentially exerts its gastroprotective effects by suppressing oxidative stress and stimulating antioxidant enzymes, which is one of the causes of destruction of cell membranes, and it is involved in the pathogenesis of acute gastric ulcers induced by ethanol.
1 January 2024 in Advances in Pharmacological and Pharmaceutical Sciences
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.
Tri-Yannarose is a Thai traditional herbal medicine formula composed of Areca catechu, Azadirachta indica, and Tinospora crispa. It possesses antipyretic, diuretic, expectorant, and appetite-stimulating effects. This study aimed to evaluate the antioxidant activities, cytotoxicity, and chemical constituents of an aqueous extract following a Tri-Yannarose recipe and its plant ingredients. The phytochemical analysis was performed using LC-QTOF-MS. Antioxidant activities were determined using DPPH, ABTS, TPC, TFC, FRAP, NBT, MCA, and ORAC assays. Cytotoxicity was investigated using a methyl thiazol tetrazolium (MTT) assay. In addition, the relationship between the chemical composition of Tri-Yannarose and antioxidant activities was investigated by examining the structure–activity relationship (SAR). The results of the LC-QTOF-MS analysis revealed trigonelline, succinic acid, citric acid, and other chemical constituents. The aqueous extract of the recipe showed significant scavenging effects against ABTS and DPPH radicals, with IC50 values of 1054.843 ± 151.330 and 747.210 ± 44.173 µg/mL, respectively. The TPC of the recipe was 92.685 mg of gallic acid equivalent/g of extract and the TFC was 14.160 mg of catechin equivalent/g of extract. All extracts demonstrated lower toxicity in the Vero cell line according to the MTT assay. In addition, the SAR analysis indicated that prenyl arabinosyl-(1–6)-glucoside and quinic acid were the primary antioxidant compounds in the Tri-Yannarose extract. In conclusion, this study demonstrates that Tri-Yannarose and its plant ingredients have potent antioxidant activities with low toxicity. These results support the application of the Tri-Yannarose recipe for the management of a range of disorders related to oxidative stress.
Nigella sativa L. and black seeds are traditionally used for cooking and medicinal purposes in Arab and other countries. Although N. sativa seed extract has many known biological effects, the biological effects of cold-pressed N. sativa oil are poorly understood. Therefore, the objective of this study was to investigate the gastroprotective effects and subacute oral toxicity of black seed oil (BSO) in an animal model. The gastroprotective effects of oral BSO (50% and 100%; 1 mg/kg) were tested using acute experimental models of ethanol-induced gastric ulcers. Gross and histological gastric lesions, ulcerated gastric areas, ulcer index score, percentage of inhibition rate, gastric juice pH, and gastric wall mucus were all evaluated. The subacute toxicity of BSO and its thymoquinone (TQ) content were also examined. The results indicated that the administration of BSO exerted gastroprotective effects by increasing the gastric wall mucus and decreasing gastric juice acidity. In the subacute toxicity test, the animals behaved normally, and their weight and water and food intake did not show significant variations. High-performance liquid chromatography detected 7.3 mg/mL TQ in BSO. These findings suggest that BSO may be a safe therapeutic drug for preventing gastric ulcers.
30 April 2024 in Advances in Pharmacological and Pharmaceutical Sciences
Krom Luang Chumphon Khet Udomsak remedy (KKR) has traditionally been used as an alternative treatment, particularly for hyperglycemia; however, its therapeutic efficacy has not been scientifically validated. Thus, this study aims to investigate the potential inhibitory and antioxidant effects of α-glucosidase enzyme and characterize the chemical profile of KKR extracts using gas chromatography-mass spectrometry (GC-MS). The investigation highlights both KKR extracts as potent inhibitors of α-glucosidase, with the ethanolic extract of KKR (KKRE) displaying an IC50 value of 46.80µg/mL and a noncompetitive mode of action. The combination of ethanolic and aqueous extracts of KKR (KKRE and KKRA, respectively) with acarbose exhibited a synergistic effect against the α-glucosidase. The KKRE extract displayed strong scavenging effects in the DPPH assay (IC50 156.3µg/mL) and contained significant total phenolic (172.82mg GAE/g extract) and flavonoid (77.41mg QE/g extract) contents. The major component of KKRE is palmitic acid (15.67). Molecular docking revealed that the major compounds interacted with key amino acid residues (ASP215, GLU277, HIS351, ASP352, and ARG442), which are crucial for inhibiting α-glucosidase. Notably, campesterin had a more significant influence on α-glucosidase than acarbose, with low binding energy. These findings underscore the significance of KKR in traditional medicine and suggest that it is promising treatment for diabetes mellitus. Further studies using animal model will provide valuable insights for advancing this research.
Five Flower Remedy (FFR), a Thai traditional medicine, has a history of use for various ailments. This study investigated its antidiabetic potential by examining its impact on key carbohydrate‐metabolizing enzymes, α‐amylase, and α‐glucosidase. We explored FFR’s inhibitory effects, synergistic interactions with the standard antidiabetic drug acarbose, and the underlying mechanisms involved. In vitro analysis revealed that FFRA significantly inhibited both α‐amylase and α‐glucosidase. Importantly, a synergistic effect was observed when FFRA extract was combined with acarbose, particularly at low concentrations for α‐amylase and α‐glucosidase inhibition. This suggests a potential benefit in combination therapy. Furthermore, FFRE demonstrated greater inhibitory potency against both enzymes compared to acarbose. Mechanistically, FFRE inhibited α‐amylase through competitive inhibition and α‐glucosidase through noncompetitive inhibition, indicating distinct modes of action. These findings provide scientific validation for the traditional use of FFR in managing diabetes and offer valuable insights into its pharmacological properties. The observed synergistic effects and distinct inhibition mechanisms highlight FFR’s potential as a therapeutic agent. This study serves as a foundation for future research, including identifying the specific bioactive components responsible for FFR’s antidiabetic effects, in vivo studies to confirm these findings in living organisms, and ultimately, clinical trials to evaluate its efficacy and safety in human subjects. Further investigation could pave the way for developing FFR as a novel therapeutic approach for diabetes management.