Search Results (6)

Background: This study encapsulates an in-depth correlation analysis for the biological activities (cytotoxicity, antimicrobial, and α-amylase inhibition) vs. the phytochemical classes (flavonoids “FV” and alkaloid “AL”) present in fenugreek seed extract. Methodology: Cell cultures for different cell lines were used to assess the cytotoxicity and selectivity (IC₅₀ value), agar diffusion assay was used to determine the MIC and MBC for different bacteria and fungi, whereas α-amylase inhibition was studied to evaluate the antidiabetic potential for the forty-five different origins of fenugreek seed extracts. An in-house analysis for the phytochemical classes of flavonoids (rutin, RT; quercetin, QT; luteolin, LT; kaempferol, KF) and alkaloid (trigonelline, TG) was performed for the seed extracts. Results: A lower IC₅₀ value (14.7 ± 1.46 µg/mL) was recorded for the IR3M extract against the HT29, MCF7 (13.03 ± 1.95 µg/mL), and MRC5 (14.58 ± 2.92 µg/mL) cell line. The extract with the lower IC₅₀ value (8.17 ± 0.73 µg/mL) against HepG2 was IR2M. For the antimicrobial activity, a lower MIC value (6.3 mg/mL) was observed for E2C, E2M, E3C, and I3H extracts against SF and for the E1M, Y3C, IR2H, IR3H, and IR3C extracts against SA. The lowest MBC value (12.5 mg/mL) was seen for E2C, E2M, E3C, and I3H against SF as well as for the extracts E1M, Y3C, IR2H, IR3H, and IR3C against SA. The extracts of Q1H (49.07 ± 2.45 µg/mL) and Y3C (43.65 ± 2.97 µg/mL) exhibited IC₅₀ values comparable to the standard drugs tested for α-amylase inhibition. The statistical models were of Pearson’s correlation. Principal component analysis (PCA) and a paired t-test established a strong positive correlation for the FV (QT, KF, LT) and alkaloid (TG) (p < 0.05) in the biological activities (cytotoxicity, antimicrobial, and α-amylase inhibition), thereby suggesting a substantial role for these phytochemical classes in the traditional and medicinal uses of fenugreek seeds. Conclusions: The FV and alkaloid are the key to impart the biological properties to the fenugreek seeds, hence their presence is utmost in the fenugreek seeds. This research work may be used as marker to help authenticate the fenugreek seeds for the quality variation in the major phytochemical classes. Full article

Animal production requires efficiency, safety and environmental sustainability. Bioactive compounds from tropical plants could modulate ruminal fermentation, providing an alternative method to antibiotic treatment and addressing concerns about antibiotic resistance. In this study, the aim was to determine the effects of Tithonia diversifolia extract (TDE) on performance, intake, digestibility and blood parameters [i.e., glucose, blood urea nitrogen (BUN), aspartate aminotransferase (AST), alanine aminotransferase (ALT)] in crossbreed sheep. The main biocompounds of the TDE include caffeic acid (CA), quercetin (QCT), luteolin (LT) and apigenin (AP). Experiment 1: An in vitro dry matter digestibility (IVDMD) study was conducted to determine the optimal inclusion levels. The IVDM values were 73.09a, 82.03b, 81.01b, 73.20a and 74.51a for the control, 5, 10, 15 and 20 g/kg for the DM treatments, respectively (R-Sq adj = 0.857). The levels of 5 and 10 g were selected for the in vivo experiment. Experiment 2: Twenty-eight male crossbred hair lambs were assigned to four treatments (n = 7): control, 20 mg monensin/day, 5 g TDE/day and 10 g TDE/day groups. No differences in animal performance were observed, including body weight and feed conversion (p > 0.05). The TDE at 10 g/day improved NDF digestibility) (61.32%) and reduced the ruminal acetate to propionate ratio. The total digestible nutrients (TDN) were higher in 10 g TDE treatment with 66.41% and the lowest acetate production (67.82%) (p = 0.042), and propionate production (21.07%) were observed. The TDE were safe at 5 g and 10 g/day for liver function and exhibited lower BUN levels suggesting an improvement in protein metabolism. TDE extract at 10 g/day (TDE10), showed improvements in total tract digestibility of NDF and reduced the ruminal acetate to propionate ratio. However, due to TDE10 reducing the DM intake, the improvements in digestibility and ruminal fermentation were not reflected in growth performance improvements. Full article

The global spread of the metabolic syndrome, oncological and viral diseases forces researchers to pay increased attention to the secondary metabolites of marine hydrobionts, which often have a high therapeutic potential in the treatment of these pathologies and are effective components of functional food. The flavone luteolin (LT), as one of the most widely distributed and studied plant metabolites, is distinguished by a diverse spectrum of biological activity and a pleiotropic nature of the mechanism of action at the molecular, cellular and organismal levels. However, there is still practically no information on the spectrum of biological activity of its sulfated derivatives, which are widely represented in seagrasses of the genus Zostera. In the present work, a comparative study of the pharmacological properties of LT and its 7,3′-disulfate was carried out with a brief analysis of the special role of sulfation in the pharmacological activity of flavonoids. Full article

Luteolin (LT), present in most plants, has potent anti-inflammatory properties both in vitro and in vivo. Furthermore, some of its derivatives, such as luteolin-7-O-glucoside, also exhibit anti-inflammatory activity. However, the molecular mechanisms underlying luteolin-3′-O-phosphate (LTP)-mediated immune regulation are not fully understood. In this paper, we compared the anti-inflammatory properties of LT and LTP and analyzed their molecular mechanisms of action; we obtained LTP via the biorenovation of LT. We investigated the anti-inflammatory activities of LT and LTP in macrophage RAW 264.7 cells. We confirmed from previously reported literature that LT inhibits the production of nitric oxide and prostaglandin E₂, as well as the expression of inducible NO synthetase and cyclooxygenase-2. In addition, expressions of inflammatory genes and mediators, such as tumor necrosis factor-α, interleukin-6, and interleukin-1β, were suppressed. LTP showed anti-inflammatory activity similar to LT, but better anti-inflammatory activity in all the experiments, while also inhibiting mitogen-activated protein kinase and nuclear factor-kappa B more effectively than LT. At a concentration of 10 μM, LTP showed differences of 2.1 to 44.5% in the activity compared to LT; it also showed higher anti-inflammatory activity. Our findings suggest that LTP has stronger anti-inflammatory activity than LT. Full article

In the present study, luteolin (LT)-loaded nanosized vesicles (LT-NVs) were prepared by a solvent evaporation–hydration method using phospholipid and edge activator. The formulation was optimized using three factors at a three-level Box–Behnken design. The formulated LT-NVs were prepared using the three independent variables phospholipid (A), edge activator (B) and sonication time (C). The effect of used variables was assessed on the vesicle size (Y₁) and encapsulation efficiency (Y₂). The selection of optimum composition (LT-NVopt) was based on the point prediction method of the software. The prepared LT-NVopt showed the particle size of 189.92 ± 3.25 nm with an encapsulation efficiency of 92.43 ± 4.12% with PDI and zeta potential value of 0.32 and −21 mV, respectively. The formulation LT-NVopt was further converted into Carbopol 934 gel (1% w/v) to enhance skin retention. LT-NVoptG was further characterized for viscosity, spreadability, drug content, drug release, drug permeation and antioxidant, antimicrobial and cytotoxicity assessment. The evaluation result revealed optimum pH, viscosity, spreadability and good drug content. There was enhanced LT release (60.81 ± 2.87%), as well as LT permeation (128.21 ± 3.56 µg/cm²/h), which was found in comparison to the pure LT. The antioxidant and antimicrobial study results revealed significantly (p ˂ 0.05) better antioxidant potential and antimicrobial activity against the tested organisms. Finally, the samples were evaluated for cytotoxicity assessment using skin cancer cell line and results revealed a significant difference in the viability % at the tested concentration. LT-NVoptG showed a significantly lower IC₅₀ value than the pure LT. From the study, it can be concluded that the prepared LT-NVoptG was found to be an alternative to the synthetic drug as well as conventional delivery systems. Full article

The aim of this study was to determine aldose reductase (AR) inhibitory activity and 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity of compounds from Agrimonia pilosa Ledeb (AP). We isolated agrimoniin (AM), four flavonoid glucosides and two flavonoid glucuronides from the n-butanol fraction of AP 50% methanol extract. In addition to isolated compounds, the AR-inhibitory activity and the DPPH free radical scavenging activity of catechin, 5-flavonoids, and 4-flavonoid glucosides (known components of AP) against rat lens AR (RLAR) and DPPH assay were measured. AM showed IC₅₀ values of 1.6 and 13.0 μM against RLAR and DPPH scavenging activity, respectively. Additionally, AM, luteolin-7-O-glucuronide (LGN), quercitrin (QU), luteolin (LT) and afzelin (AZ) showed high inhibitory activity against AR and were first observed to decrease sorbitol accumulation in the rat lens under high-sorbitol conditions ex vivo with inhibitory values of 47.6%, 91.8%, 76.9%, 91.8% and 93.2%, respectively. Inhibition of recombinant human AR by AM, LGN and AZ exhibited a noncompetitive inhibition pattern. Based on our results, AP and its constituents may play partial roles in RLAR and oxidative radical inhibition. Our results suggest that AM, LGN, QU, LT and AZ may potentially be used as natural drugs for treating diabetic complications. Full article