ABSTRACT
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 46.80 µg/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 156.3 µg/mL) and contained significant total phenolic (172.82 mg GAE/g extract) and flavonoid (77.41 mg 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.
ABSTRACT
This study presents a phytochemical investigation of Lepionurus sylvestris leaf extracts and their anti-diabetic activities. Traditionally, L. sylvestris leaves were used as vegetables and food in local recipes, but the root extracts of the plant can also be used in body tonic and erectile dysfunction treatments. Following a preliminary anti-diabetic activity screening test, the 80% ethanolic leaf extract exhibited potent anti-alpha glucosidase activity. So, the leaves' active components were selected for further investigation. Firstly, the plant was extracted via maceration using lower to higher polarity solvents such as hexane, ethyl acetate, ethanol, and water, respectively, to obtain the four crude extracts. Then, the phytochemicals contained in this plant were investigated via classical column chromatography and spectroscopy techniques. Anti-diabetic activity was evaluated via anti-alpha glucosidase and insulin secretagogue assays. The results showed that five compounds were isolated from the fractionated ethanolic leaf extract: interruptin A; interruptin C; ergosterol; diglycerol; and 15-16-epoxy-neo-cleoda-3,7(20),13(16),14-tetraene-12,17:18,19-diolide, a new diterpene derivative which is herein referred to as lepionurodiolide. Interruptin A and the new diterpene derivative exhibited the greatest effect on anti-alpha glucosidase activity, showing IC50 values of 293.05 and 203.71 µg/mL, respectively. Then, molecular docking was used to study the sites of action of these compounds. The results showed that interruptin A and the new compound interacted through H-bonds with the GLN279 residue, with a binding energy of -9.8 kcal/mol, whereas interruptin A and C interacted with HIS280 and ARG315 a with binding energy of -10.2 kcal/mol. Moreover, the extracts were investigated for their toxicity toward human cancer cells, and a zebrafish embryonic toxicity model was used to determine herbal drug safety. The results indicated that ethyl acetate and hexane extracts showed cytotoxicity to both Hela cells and human breast adenocarcinomas (MCF-7), which was related to the results derived from using the zebrafish embryonic toxicity model. The hexane and ethyl acetate presented LC50 values of 33.25 and 36.55 µg/mL, respectively, whereas the ethanol and water extracts did not show embryonic toxicity. This study is the first of its kind to report on the chemical constituents and anti-diabetic activity of L. sylvestris, the leaf extract of which has been traditionally used in southern Thailand as a herbal medicine and food ingredient.
ABSTRACT
Most modern wound dressings assist the wound-healing process. In contrast, conventional wound dressings have limited antibacterial activity and promote sporadic fibroblast growth. Therefore, wound dressings with prolonged substance release must be improved. This research aimed to develop hydrogel films. These were synthesized from alginate and pectin, incorporated with mangosteen extract (ME), and encapsulated in niosomes (ME-loaded niosomes). Subsequently, we examined the in vitro release and physical characteristics of ME-loaded niosomes. These characteristics included particle pH, size, charge, polydispersity index (PDI), and drug loading properties. These properties included drug loading content (DLC), entrapment efficiency (EE), and yield (Y). Additionally, we examined the swelling ratio and biological characteristics of the hydrogel film. These characteristics included antibacterial activity, cytotoxicity (L929), cell attachment to the tested materials, cell migration, hemocompatibility, and in vivo irritation. Significant results were obtained using a 2:1 niosome preparation containing Span60 and cholesterol. Ratio influenced size, charge, PDI, DLC, EE, and Y. The results were 225.5 ± 5.83 nm, negatively charged, 0.38, 16.2 ± 0.87%, 64.8 ± 3.49%, and 87.3 ± 3.09%, respectively. Additionally, the release of encapsulated ME was pH sensitive because 85% of the ME can be released at a pH of 5.5 within seven days and decrease to 70% at a pH of 7.4. The maximum swelling ratios of patches with 0.5% and 1% Ca2+ crosslinking were 867 wt% and 1,025 wt%, respectively, after 30 min. These results suggested that a medium dose (15 mg) of niosomal ME incorporated in a hydrogel film provided better bacterial inhibition, cell migration, and cell adhesion in an in vitro model. Additionally, no toxicity was observed in the fibroblasts and red blood cells. Therefore, given the above-mentioned advantages, this product can be a promising candidate for wound dressing applications.
ABSTRACT
Natural polymer-based hydrogel films possess considerable potential for use in biomedical applications and are excellent for wound healing. The purpose of this research was to use ionic crosslinking to improve the mechanical characteristics, absorption of fluid in the wound, and drug release behavior of Cassia alata L. (CA) extract loaded niosomes (CANs) that were incorporated in an alginate-pectin film (A/P). Then, chemically crosslinked A/P hydrogels were obtained by immersing them in different concentrations of calcium chloride (CaCl2) (0.5-1% w/v) for 15-120 s. The degree of crosslinking was controlled by both contact time and CaCl2 concentration. The optimal crosslinking conditions were 1% CaCl2 for 15 seconds. In this study, the following features of the hydrogel films were investigated: physical properties, morphological characteristics, drug loading, in vitro drug release, antibacterial activity, wound healing activity, cytocompatibility profiles, and hemocompatibility. The crosslinked hydrogel films maintained their physical integrity during use, with the 1% film attaining the best results in the shortest period (15 sec). Then, in vitro drug release from the films was examined. Crosslinking was observed to prolong the release of the CA extract from the hydrogel film. Finally, a cell viability experiment was conducted to evaluate the cytotoxicity profile. The A/P composite film exhibited excellent wound dressing qualities and good mechanical properties in preformulation testing. The in vitro drug release profile indicated that the A/P created a regulated drug release profile, and the cell viability experiment revealed that the film was nontoxic and hemocompatible. A/P composite films can be produced using CAN extract as a possible wound dressing. However, further studies in animals and humans are required to determine both safety and effectiveness.
