Chebulagic Acid Research Articles

Nesfatin-1 enhances vascular smooth muscle calcification through facilitating BMP-2 osteogenic signaling

Vascular calcification (VC) arises from the accumulation of calcium salts in the intimal or tunica media layer of the aorta, contributing to higher risk of cardiovascular events and mortality. Despite this, the mechanisms driving VC remain incompletely understood. We previously described that nesfatin-1 functioned as a switch for vascular smooth muscle cells (VSMCs) plasticity in hypertension and neointimal hyperplasia. In this study, we sought to investigate the role and mechanism of nesfatin-1 in VC. The expression of nesfatin-1 was measured in calcified VSMCs and aortas, as well as in patients. Loss- and gain-of-function experiments were evaluated the roles of nesfatin-1 in VC pathogenesis. The transcription activation of nesfatin-1 was detected using a mass spectrometry. We found higher levels of nesfatin-1 in both calcified VSMCs and aortas, as well as in patients with coronary calcification. Loss-of-function and gain-of-function experiments revealed that nesfatin-1 was a key regulator of VC by facilitating the osteogenic transformation of VSMCs. Mechanistically, nesfatin-1 promoted the de-ubiquitination and stability of BMP-2 via inhibiting the E3 ligase SYTL4, and the interaction of nesfatin-1 with BMP-2 potentiated BMP-2 signaling and induced phosphorylation of Smad, followed by HDAC4 phosphorylation and nuclear exclusion. The dissociation of HDAC4 from RUNX2 elicited RUNX2 acetylation and subsequent nuclear translocation, leading to the transcription upregulation of OPN, a critical player in VC. From a small library of natural compounds, we identified that Curculigoside and Chebulagic acid reduced VC development via binding to and inhibiting nesfatin-1. Eventually, we designed a mass spectrometry-based DNA-protein interaction screening to identify that STAT3 mediated the transcription activation of nesfatin-1 in the context of VC. Overall, our study demonstrates that nesfatin-1 enhances BMP-2 signaling by inhibiting the E3 ligase SYTL4, thereby stabilizing BMP-2 and facilitating the downstream phosphorylation of SMAD1/5/9 and HDAC4. This signaling cascade leads to RUNX2 activation and the transcriptional upregulation of MSX2, driving VC. These insights position nesfatin-1 as a potential therapeutic target for preventing or treating VC, advancing our understanding of the molecular mechanisms underlying this critical cardiovascular condition.

An integrated strategy for deciphering quality markers of Terminaliae Belliricae Fructus based on a three-dimensional characteristic model

Terminalia bellirica (Gaertn.) Roxb. is an ethnomedicinal plant that has been utilized in Tibetan and traditional Chinese medicine (TCM). Nevertheless, its quality standard officially listed in the Chinese Pharmacopoeia does not include any content determination of the indicator components of Terminaliae Belliricae Fructus, which constrains the effective quality evaluation of medicinal material and related products. In this paper, a three-dimensional “content-pharmacokinetics-pharmacology” network strategy was developed to identify the quality markers (Q-markers) of Terminaliae Belliricae Fructus. in terms of “measurability”, “traceability” and “effectiveness”. Chromatographic fingerprint analysis was performed to outline its chemical contour, and identify the differential components of 17 batches of Terminaliae Belliricae Fructus. combined with multivariate statistics analysis and UPLC-QTOF-MS analysis. Serum pharmacochemistry analysis was implemented on rats, and 25 prototype components absorbed into the blood were identified. By network pharmacology analysis, a component-disease-target-pathway network was constructed, thus validating the effectiveness of the chemical components of Terminaliae Belliricae Fructus. Afterwards, the above screened candidate components were put into construction of three-dimensional "radar chart". According to the calculated regression area (RA) and coefficient of variation (CV) values, the potential Q-markers was determined, followed by “specificity” evaluation. Ultimately, ellagic acid (EA), chebulagic acid (CHA), gallic acid (GA), chebulinic acid (CA), corilagin (CO) and chebulanin (CH) were specified as the Q-markers of Terminaliae Belliricae Fructus. Owing to high content, good pharmacokinetic property, high pharmacological activities and specificity. The screened Q-markers could offer a scientific foundation for the quality control of Terminaliae Belliricae Fructus, and the proposed strategy is demonstrated to be reliable and feasible for deciphering Q-markers of TCM.

A Review on Anticancer Properties of Chebulagic Acid from Terminalia chebula

A Review on Anticancer Properties of Chebulagic Acid from Terminalia chebula

LC-MS-Based Targeted Metabolite Profiling and Atomic Absorption Spectrophotmeter Based Mineral Analysis of Methanol Extract of Terminalia bellerica (Gaertn.) Leaves

Aim: Natural products in medicinal plants are one of the important sources for modern drug discovery. Plant-based formulations play an important role in management of numerous diseases. To discover the medical potential of natural products, it is important to understand the bioactive compounds present in medicinal plants. Hence the aim of the study is to identify the volatile compounds by LC –MS analysis and minerals by AAS assay present in the leaves of Terminalia bellerica. Study Design: This study investigates metabolites present in leaves of Terminalia bellerica have been studied by AAS and LC-MS techniques. Results: The AAS assay showed that the leaves of T. bellerica are particularly rich in iron (260 mg/kg) compared to their zinc, manganese, and copper content. Meanwhile, the LC-MS analysis identified chebulinic acid, chebulagic acid, punicafolin, myricetin, rutin, and galloyl punicalagin as being present in the highest concentrations. Conclusion: Results highlighted presence of considerable amount of iron and other minerals in methanolic extract of the leaves of T. bellerica, it may be used in the development of health supplements. The results also revealed that bioactive compounds in the methanolic extracts of T. bellerica leave used for drug design and making it safe to human health.

Targeting FAK, VEGF, and MTA1 proteins with Terminalia elliptica: a computational approach for anticancer activity.

Cancer remains a significant global health challenge, prompting exploration into alternative treatments such as those derived from natural compounds found in traditional medicine. Recent research has underscored the role of proteins like Focal Adhesion Kinase (FAK), Vascular Endothelial Growth Factor (VEGF), and Metastasis-Associated Protein 1 (MTA1) in driving cancer cell proliferation and survival. Here, we investigated the potential of a single molecule to modulate these key proteins involved in metastasis, offering a promising avenue for cancer therapy. Terminalia elliptica, commonly known as Asna, possesses a diverse range of medicinal properties, including antimicrobial, anti-inflammatory, anticancer, antidiabetic, antiaging, hepatoprotective, antioxidant, and neuroprotective activities. Our study aimed to explore the anticancer potential of Terminalia elliptica by identifying bioactive compounds capable of targeting FAK, VEGF, and MTA1 to impede cancer metastasis. Through in silico analysis, we conducted network analysis using Cytoscape to assess the significance of these bioactive compounds in the inhibition of signaling pathways driving metastasis. The utilization of these bioactives as potential candidates for targeted therapy of VEGF, FAK, and MTA1 regulated pathways was preliminarily assessed by Molecular Docking and MD Simulation. Our findings revealed that phytobioactives namely, Chebulinic Acid of Terminalia elliptica, exhibited notable binding affinity and interaction with FAK, and Chebulagic Acid with VEGF, and MTA1. This discovery holds promise as a novel therapeutic approach for combating cancer, offering potential benefits in cancer treatment and management.

Product development and characterization of a lipid-based Ayurvedic polyherbal formulation: Kalyanaka Ghrita

BackgroundKalyanaka Ghrita (KG) is polyherbal oleaginous medicament consisting of extracts from twenty-eight different plants, indicated for management of psychosomatic disorders like Unmada (Schizophrenia), Apasmara (Epilepsy) and numerous other ailments. ObjectiveTo develop and validate standard manufacturing procedure of KG by following Ayurvedic principles in three batches to ensure process uniformity and standards. Materials and methodsThree batches of KG were prepared by adopting principles of Ashtanga Hrudya and Ayurvedic Formulary of India to ensure consistency in manufacturing process. Observations during process such as temperature, duration were recorded. KG was subjected to chief desired characteristics, organoleptic (color, odour, taste, texture, touch), physicochemical (acid value, peroxide value, iodine value, saponification value, loss on drying, refractive index, specific gravity, mineral oil, rancidity test, viscosity) as per pharmacopeial standard. Chromatographic screening and fingerprinting of KG were conducted through GCMS whereas quantification of curcumin and chebulagic acid biomarkers were assessed through HPLC. ResultsAverage yield of KG was 83.41%, with average intermittent heating duration of 20.35 h subsequently divided into three days. Temperature throughout preparation ranged from 66 °C to 101 °C. KG was pale olive in colour, exhibiting pleasant taste, characteristic smell, and soft texture. Organoleptic and physicochemical characters were comparable for three batches of KG while safety parameters were found within permissible limits. ConclusionPharmaceutical standardization of Kalyanaka Ghrita is necessary for establishing biological and chemical profile of formulations. Present study recommends use of coarse powdered ingredients for optimal yield during pharmaceutical process, and heating up to Madhyama Paka stage calibrated over three days with average temperature of 85 °C. The data obtained from this study may contribute to future research and development activities, serving as a basis for manufacturing standards of KG.

Revealing the potential hypoglycaemic ingredients of Terminalia chebula Retz. by spectrum–effect relationship combining molecular docking and experimental validation

Terminalia chebula Retz. is commonly used in the treatment of diabetes, but its specific ingredients and hypoglycaemic mechanisms remain unclear. In this study, spectrum-effect relationships between common peaks of fingerprint and DPPH, ABTS, PTP1B, α-glucosidase, were used to screen six compounds as the potential hypoglycemic ingredients. Molecular docking studies were conducted on chebulagic acid, chebulinic acid and punicalagin, which were identified by reference standard, revealing the potent in teractions between these bioactive substances and the PTP1B, α-glucosidase protein. Additionally, the cellular level results showed that punicalagin displayed stronger inhibition of PTP1B and α-glucosidase, with IC50 values of 0.0236 and 0.335 μg/mL, respectively, while improving glucose consumption and intracellular glycogen content of insult-resistant L6 muscle cell, and the hypoglycemic effect was achieved by activating the PI3K/AKT signaling pathway. This study demonstrated that T. chebula has the potential to become a hypoglycemic functional food, and offers a strategy for characterization hypoglycemic ingredients.

Identification of Potential Inhibitors from Medicinal Plant-based Phytochemicals for the Influential C4 Target of Diabetic Retinopathy by Molecular Docking Studies.

Diabetic retinopathy is the major cause of vision failure in diabetic patients, and the current treatment involves the practice of glucocorticoids or VEGF antagonists that are "off-label". A few small organic molecules against DR were discovered many years ago. Nutraceuticals are naturally available functional foods that endorse different health benefits, including vitamins, antioxidants, minerals, fatty acids, and amino acids that can defer the development of some diseases. Numerous studies reported that nutraceuticals encourage multiple therapeutic benefits and provide protection against various diseases. In diabetes, nutraceuticals contribute to improving insulin sensitivity, metabolism regulation, and lower hyperglycemia. The major aim of this study is to discover the most active drug from natural or plant sources. In this work, 42 phytochemical constituents from 4 kinds of plants were docked with the C4 target of diabetic retinopathy by an in silico molecular docking study. According to the binding energy, all the phytoconstituents possessed good to high attraction towards the target, and 6 phytochemicals, such as terchebulin, punicalagin, chebulagic acid, casuarinin, punicalin, and pedunculagin, disclosed superior binding energy towards the target than standard ruboxistaurin via the interactions of conventional hydrogen bonding, pi-alkyl interactions, etc. Molecular dynamic simulation studies further established the stability of the phytoconstituents, and ADMET studies proved the safety profile of these phytoconstituents. Hence, the current study suggested that the phytochemicals from various herbs inhibit the C4 target of diabetic retinopathy and can be utilized as lead compounds to develop analogs or repurposed for the treatment of DR.

Changes in phenolic compounds of Phyllanthus emblica juice during different storage temperature and pH conditions.

The aim of this experiment was to investigate the effect of storage temperature and pH on phenolic compounds of Phyllanthus emblica juice. Juice was stored at different temperatures and pH for 15 days and sampled on 2-day intervals. The browning index (BI, ABS420 nm), pH, centrifugal precipitation rate (CPR), and phenolic compounds were evaluated. The results showed 4°C and pH 2.5 could effectively inhibit browning and slow down pH drop of P. emblica juice. The result of orthogonal partial least square-discriminant analysis showed P. emblica juice stored at 4°C and pH 2.5 still had a similar phenolic composition, but at 20°C, 37°C, and pH 3.5, the score plots were concentrated only in the first 3 days. Additionally, gallic acid (GA) and ellagic acid (EA) were screened out to be the differential compounds for browning of P. emblica juice. The contents of GA, epigallocatechin (EGC), corilagin (CL), gallocatechin gallate (GCG), chebulagic acid (CA), 1,2,3,4,6-O-galloyl-d-glucose (PGG), and EA were more stable at 4°C and pH 2.5. Overall, during storage at 4°C and pH 2.5, it could inhibit the increase of GA and EA and decrease of CL, GCG, CA, and PGG, whereas EGC did not show significant difference between storage conditions. The CPR was higher at 4°C, while pH 2.5 could reduce the CPR. In conclusion, in order to maintain stability of phenolic compounds and extended storage period, the P. emblica juice could be stored at low temperature and adjust the pH to increase the stability of juice system.

Inhibition of SARS-CoV-2-Induced NLRP3 Inflammasome-Mediated Lung Cell Inflammation by Triphala-Loaded Nanoparticle Targeting Spike Glycoprotein S1.

The COVID-19 pandemic, caused by SARS-CoV-2, poses a significant global health threat. The spike glycoprotein S1 of the SARS-CoV-2 virus is known to induce the production of pro-inflammatory mediators, contributing to hyperinflammation in COVID-19 patients. Triphala, an ancient Ayurvedic remedy composed of dried fruits from three plant species-Emblica officinalis (Family Euphorbiaceae), Terminalia bellerica (Family Combretaceae), and Terminalia chebula (Family Combretaceae)-shows promise in addressing inflammation. However, the limited water solubility of its ethanolic extract impedes its bioavailability. In this study, we aimed to develop nanoparticles loaded with Triphala extract, termed "nanotriphala", as a drug delivery system. Additionally, we investigated the in vitro anti-inflammatory properties of nanotriphala and its major compounds, namely gallic acid, chebulagic acid, and chebulinic acid, in lung epithelial cells (A549) induced by CoV2-SP. The nanotriphala formulation was prepared using the solvent displacement method. The encapsulation efficiency of Triphala in nanotriphala was determined to be 87.96 ± 2.60% based on total phenolic content. In terms of in vitro release, nanotriphala exhibited a biphasic release profile with zero-order kinetics over 0-8 h. A549 cells were treated with nanotriphala or its active compounds and then induced with 100 ng/mL of spike S1 subunit (CoV2-SP). The results demonstrate that chebulagic acid and chebulinic acid are the active compounds in nanotriphala, which significantly reduced cytokine release (IL-6, IL-1β, and IL-18) and suppressed the expression of inflammatory genes (IL-6, IL-1β, IL-18, and NLRP3) (p < 0.05). Mechanistically, nanotriphala and its active compounds notably attenuated the expression of inflammasome machinery proteins (NLRP3, ASC, and Caspase-1) (p < 0.05). In conclusion, the nanoparticle formulation of Triphala enhances its stability and exhibits anti-inflammatory properties against CoV2-SP-induction. This was achieved by suppressing inflammatory mediators and the NLRP3 inflammasome machinery. Thus, nanotriphala holds promise as a supportive preventive anti-inflammatory therapy for COVID-19-related chronic inflammation.

Investigating Antibacterial Activities of Phytochemicals from Terminalia chebula and Terminalia bellirica fruit extract: An in vitro and in silico Study

This study aims to investigate the antibacterial activities of phytochemicals derived from Terminalia chebula (T. Chebula) and Terminalia bellirica (T. bellirica) through a combined approach of in vitro and in silico analyses. T. chebula and T. bellirica are medicinal plants widely recognized for their therapeutic properties and have been traditionally used to treat various infectious diseases. The potential antibacterial properties of these plants have drawn significant interest in recent years. In the in vitro phase of the study, crude extracts of dried fruit of T. chebula and T. bellirica are prepared and subjected to various antibacterial assays against a panel of clinically significant bacterial strains. It has been found that both extracts were effective against Staphylococcus aureus but had no inhibitory effect on Escherichia coli and Salmonella typhi at the tested concentrations. Furthermore, the study incorporated an in silico analysis to predict the interactions between the active phytochemical constituents and Staphylococcus aureus targets. Molecular docking was employed to examine the binding affinity and mode of interaction of these phytochemicals with the active site of protein DNA Gyrase of Staphylococcus aureus (3U2D). Most of the phytochemicals posed the highest binding affinity than inbuilt ligands. The protein interacted effectively with phytochemicals through various types of interactions including hydrogen bonding, electrostatic interactions, carbon-hydrogen bonding, metal-ion coordination and hydrophobic interactions. These interactions suggest potential binding mechanisms and provide important information about the potential biological activities of these phytochemicals. From ADME and toxicity analysis, phytochemicals "Syringic acid," "Ellagic acid" and "Punicalagin" from Terminalia chebula and "Ellagic acid," "Chebulagic acid" and "Terchebin" from Terminalia bellirica emerged as potential druggable candidates with relatively low toxicity concerns.

Recent Insights into the Antimicrobial Properties of Phyllanthus emblica L.: A Comprehensive Review of Wonder Berry.

Phyllanthus emblica L., or Amla, is known for its therapeutic properties and has been used as a medicinal plant. It is rich in vitamin C and other bioactive phytochemicals like polyphenols, gallic acid, chebulagic acid, leutolin, quercetin, etc. Different parts of this plant are used to treat various viral, bacterial, and fungal diseases. This review article summarizes the recent literature relevant to the antiviral, antibacterial, and antifungal effects of P. emblica. A variety of bacteria (Staphylococcus aureus, Bacillus subtillus, Enterococcus faecalis, Salmonella typhi, and Escherichia, etc.), fungi (Alternaria alternate Botroyodiplodia theobromae, Colletotrichum corcori, Curvularia lunata, Fusarium exquisite, Fusarium solanii, Aspergillus niger, Candida albicans, Colletotrichum gleosparoitis, and Macrophomina phaseolina) and viruses, like Influenza A virus strain H3N2, hepatitis B, Human Immunodeficiency virus type-1 (HIV-1), Simplex virus type 1 (HSV-1) and type 2 (HSV-2) have experimented. Different techniques were used based on the way of identification. 'For example, disc diffusion, dilution methods, sound diffusion, Immuno-peroxidase monolayer assay, serum HBV and HBsAg assay, enzyme immunoassay, etc. The present review analyzed and summarized the antimicrobial activities of P. emblica and possible mechanisms of action to provide future directions in translating these findings clinically.

Study on Quality Characteristic of Chebulae Fructus and Its Adulterants and Degradation Pathway of Hydrolyzable Tannins.

Chebulae Fructus (CF) is known as one of the richest sources of hydrolyzable tannins (HTs). In this study, ultra-performance liquid chromatography coupled with a photodiode array detector method was established for simultaneous determination of the 12 common phenolcarboxylic and tannic constituents (PTCs). Using this method, quantitative analysis was accomplished in CF and other four adulterants, including Terminaliae Belliricae Fructus, Phyllanthi Fructus, Chebulae Fructus Immaturus, and Canarii Fructus. Based on a quantitative analysis of the focused compounds, discrimination of CF and other four adulterants was successfully accomplished by hierarchical cluster analysis and principal component analysis. Additionally, the total contents of the 12 compounds that we focused on in this study were unveiled as 148.86 mg/g, 96.14 mg/g, and 18.64 mg/g in exocarp, mesocarp, and endocarp and seed of CF, respectively, and PTCs were witnessed to be the most abundant in the exocarp of CF. Noticeably, the HTs (chebulagic acid, chebulanin acid, chebulinic acid, and punicalagin) were observed to be ultimately degraded to chebulic acid, gallic acid, and ellagic acid during sunlight-drying of the fresh fruits. As a result, our study indicated that CF and its adulterants could be distinguished by the observed 12 PTCs, which were mainly distributed in the exocarp of the fruits. The HTs were prone to degrade into the three simple phenolcarboxylic acids during drying or processing, allowing us to obtain a more comprehensive understanding of the PTCs, with great significance in the improved quality of CF and related products.

A study on exosome based delivery of Terminalia chebula Retz. fruit extract in hepatocellular carcinoma

Terminalia chebula Retz. is an extensively used plant for the treatment of numerous ailments in Ayurveda. The major phytochemicals found in this plant are tannins, phenols which possess anti-inflammatory, anti-oxidative, anti-carcinogenic, and anti-mutagenic effect. In the present study, we focused on identification of drug like candidates and exosomes mediated drug delivery system for cancer treatment. We have investigated phenolic content, anti-inflammatory potential, and anti-oxidative capacity of hydro-alcoholic Terminalia chebula Retz. fruit extract (TCE) which was found higher when compared to the standards. HPLC and GC-MS analysis have revealed the presence of 73 compounds in TCE and three of them were further exploited for the development of novel safer and potent anticancer drug. Using computational approach the potential inhibitory effects and binding of 3 phytochemicals (i.e., chebulagic acid, chebulinic acid and corilagin) obtained from TCE against 8 structural and functional target proteins (i.e., IL-6, NFκβ, LRP-6, BCL-XL, MEK1, Aurora kinase, EGFR, and α1β2) that are crucially involved in carcinogenesis were studied. Chebulagic acid has showed good docking score with almost all the protein considered in this study. We have observed higher binding affinity of chebulagic acid for the target proteins as evidenced from the more negative value of the binding energy compared to other ligands i.e. chebulinic acid and corilagin by docking analysis. Chebulagic acid forms five and four hydrogen bonds with amino acids in the active site of the IL-6 and NFκβ target protein, with the least binding energy of −10.79 and −10.26 respectively and hence considered as an excellently docked conformation. Exosome mediated TCE delivery was investigated in HuH-7 cell line. The in-vitro cytotoxic study by MTT assay and apoptotic study in HuH-7 cell lines have revealed that TCE has anti-proliferative activity in malignancy like hepatocellular carcinoma, however TCE loaded in exosomes (Ex-TCE) showed better results due to increased intracellular delivery of TCE.

Consequences of Gamma Irradiation on Triphala’s Phytochemical Compositions, Microbial Burden and Antioxidant Properties

Triphala, a renowned polyherbal blend comprising three fruits, Phyllanthus emblica Linn., Terminalia chebula Retz., and Terminalia bellirica (Gaertn.) Roxb., in equal proportions, holds a rich historical lineage in both Ayurvedic and Thai traditional medicine. Triphala has been reputed as the indigenous medicine in the Thailand National List of Essential Drugs: List of Herbal Medicinal Products which has been widely used as a natural remedy for relieving cough and phlegm. However, the inherent challenge of microbial contamination in herbal remedies necessitates effective interventions. Gamma () irradiation emerges as a pivotal method to mitigate the microbial burden in medicinal plants, albeit with potential repercussions on their chemical composition and biological properties. This study investigated the impact of -irradiation doses of 5, 10, and 25 kGy exposed to Triphala and the microbial contamination along with antioxidant activity, total phenolic content (TPC), gallic acid (GA), and chebulagic acid (CA) contents. The TPC and antioxidant activity of non-irradiated and irradiated Triphala were determined by using the Folin-Ciocalteu method and DPPH assay, while the GA and CA contents were quantified by HPLC analysis. The results demonstrated the efficacy of radiation doses (5-25 kGy) in diminishing microbial loads without significantly altering TPC or DPPH scavenging activity. Intriguingly, irradiation at 5 and 10 kGy, resulted in a notable increase in GA contents and CA contents (p&lt; 0.05). Thus, the -irradiation emerges as a promising avenue for preserving Triphala quality and antioxidant properties amidst microbial contamination challenges.

In-vitro colonic fermentation of Kakadu plum (Terminalia ferdinandiana) fruit powder: Microbial biotransformation of phenolic compounds and cytotoxicity

Kakadu plum (Terminalia ferdinandiana) (KP) is an indigenous fruit used as a functional ingredient in powdered form. Three KP doses (1, 2.5 and 5 g) were digested in a dynamic in vitro gut digestion model over 48 h. Faecal water digests from the colonic reactors were assessed for total soluble polyphenols (TSP), ferric reducing antioxidant power (FRAP), phenolic metabolites and short-chain fatty acids (SCFAs). Effects of digests on cell viability were tested against Caco-2 intestinal and HepG2 hepatic cells. All doses of KP fermentation produced castalagin, corilagin, chebulagic acid, chebulinic acid, and gallic acid. TSP and FRAP significantly increased in 5 g KP digests at 0 and 48 h of fermentation. SCFA concentrations significantly increased after 48 h. Cytotoxic effects of 2.5 and 5 g KP digests diminished significantly after 12 h. Overall, colonic fermentation increased antioxidant activity and polyphenolic metabolites of 5 g KP powder for 48 h.

Effect of ultrasonication on the quality of amla pulp (Emblica officinalis): Optimization and comparison with the thermal processing

Amla pulp was treated with ultrasonication technique under the different set of designed conditions in order to optimize the ultrasonic conditions. A two factor four level Taguchi design was adopted to study the effect of ultrasonic intensity (180 – 717 W/cm2) and treatment time (4 – 16 min) on the ascorbic acid, naringin, total phenolic content, titratable acidity, total soluble solids, browning index, polymethylesterase and polyphenol oxidase activity of amla pulp. The optimal conditions were determined as ultrasonic intensity, 359 W/cm2 and treatment time, 12 min on the basis of S/N ratio analysis. Optimized ultrasonicated pulp was compared with the thermally treated pulp (90 °C/ 5 s) to observe the effect on quality parameters. Enzymatic activity reduced to a lower level at optimal ultrasonic processing conditions. Total phenolic content increased after ultrasonication treatment. LCMS of the optimized sample depicted the presence of compounds like ascorbic acid, corilagin, gallic acid, kaempferol, chebulagic acid and many more. Thermal treatment showed lower retention of bioactives and there were notable losses in ascorbic acid and total phenolic content. Browning index was also higher than control and ultrasonicated pulp sample. Microstructure of ultrasonicated sample showed damage to cells but thermal treated sample exhibited major cell damage.

Comprehensive assessment of the extraction of Phyllanthus emblica L. based on the G1-Entropy Method and Response Surface Methodology

In this study, the G1-Entropy method was employed together with a response surface methodology (RSM) approach to establish a multi-index-based system for evaluating and optimizing the extraction of bioactive compounds from Phyllanthus emblica L. Seven chemical classes' contents were evaluated, including TPC (total phenolic content), TC (tannin content), DEY (dry extract yield), GA (gallic acid), CO (corilagin), CA (chebulagic acid), and EA (ellagic acid). The resultant extracts were also assessed for their antioxidant activity, as measured based on their DPPH radical, ABTS+, and hydroxyl radical scavenging activity levels and their capacity to reduce iron ions. The inhibition of fluorescent AGEs generation was also assessed in BSA-Fru and MGO-BSA model assays to gauge the anti-glycation activity of these extracts. In total, a comprehensive score was derived based on 13 indices and corresponding weight values, with these scores then being used to determine the extraction conditions that yielded the best outcome. Through this strategy, the ideal extraction processing parameters were found to include an ethanol concentration of 56%, a liquid-solid ratio of 8 mL/g, and an extraction duration of 100 min. Using these optimized conditions yielded a predicted comprehensive score (Y) of 94.91, while the response value based on three independent variables from the validation experiments performed using these conditions was 92.03. These results highlight the promise of leveraging Phyllanthus emblica as a resource for use in the cosmetic, food, biochemical, and pharmaceutical industries.

Formulation Development of Directly Compressible Tablets Incorporating Trisamo Extract With Synergistic Antioxidant Activity.

This work investigates the synergistic antioxidant activity of the compositions of Trisamo (TSM) herbal formula containing the dried fruits of Terminalia chebula, Terminalia arjuna, and Terminalia bellirica. An augmented simplex lattice design was utilized to investigate the synergistic antioxidant activity, finding an equal mass ratio among the three herbal drugs to exhibit optimal synergistic antioxidant activity, with a combination index of less than 0.8. The optimal TSM extract was used to prepare directly compressible tablets employing a Box-Behnken design response surface methodology, optimizing compressional force (500, 1000, and 1500 psi), sodium starch glycolate (0%, 2%, and 4%), and magnesium stearate (0.5%, 1.0%, and 1.5%). Optimal parameters were a compressional force of 1000 psi, 2% sodium starch glycolate, and 0.5% magnesium stearate. The TSM extract tablet had a weight of 600.06 mg, a diameter of 12.78 mm, a thickness of 4.12 mm, a hardness of 6.85 kP, a friability of 0.30%, and a disintegration time of 1.81 min. Computer model predictions were verified with a low percentage error (≤ 10.00%). After 6 h, phenolic compounds were dissolved to an extent of approximately 40%-80%, including gallic acid (57.11%), corilagin (38.64%), chebulagic acid (58.49%), and chebulinic acid (81.44%). Stability data revealed that the phenolic compounds were retained for 3 months compared to the initial time point, with gallic acid at 81.43% and 100.27%, corilagin at 94.81% and 87.85%, chebulagic acid at 92.22% and 69.83%, and chebulinic acid at 107.00% and 85.54% at 30°C/75% RH and 45°C/75% RH, respectively. The summation of these four compounds did not change significantly when stored under either set of conditions. In summary, mixture design and response surface design were successfully utilized in the optimization of TSM extract tablets with synergistic antioxidant activity.

Laxilignans A-C from the leaves of Terminalia laxiflora Engl. and their α-glucosidase inhibitory activity

Three previously undescribed dibenzylbutane lignans, laxilignans A−C, together with fifteen known compounds were isolated and characterized from the leaves of Terminalia laxiflora Engl. The structures of laxilignans A−C were elucidated by extensive 1D and 2D NMR analyses, together with mass spectrometry. The inhibitory activity of the isolated compounds against α-glucosidase enzyme, obtained from Saccharomyces cerevisiae, was evaluated in comparison to acarbose (IC50 = 16.42 ± 0.14 µM). The results revealed that corilagin, chebulagic acid, laxilignan A, termilignan B, termitomenin C, arjunglucoside II, and laxilignan B possess α-glucosidase inhibitory potential, with IC50 values in the range of 1.61 ± 0.05 – 403.5 ± 29.5 μM, respectively. The results of the molecular docking revealed that the two laxilignans A and B showed comparable binding affinities to those of acarbose with the binding sites of the human α-glucosidase enzyme. These findings suggest that dibenzylbutane lignans may act as promising lead compounds for the development of α-glucosidase inhibitors.