Evaluation of Picralima nitida hypoglycemic activity, toxicity and analytical standards

Background: Traditional knowledge has been a legacy of the past to the present. Barks of Ficus hispida Linn. and leaves of Ficus pomifera Wall. (Moraceae) have been used traditionally for the treatment of diabetes in North-east India and many other places. As many drugs have been developed from traditional plants, the authors have taken up the plants for the study of hypoglycemic activity. Objective: To investigate the hypoglycemic activities of the triterpenoids isolated from the plants and their antioxidant activities. Methods: The bioactive compounds were determined by biochemical analysis, antioxidant activity using DPPH method. Hypoglycemic activity was detected using glucose tolerance test in normal rats and alloxan induced diabetic rats with Gliclazide as standard. Results: The biochemicals and trace elements were present in appreciable amounts. Triterpenoids, (1-5), from F. pomifera and 19-hydroxyphlogacantholide (6), 3-O-[ß-D-glucopyranosyl-(1’→2’)-α- L-rhamnopyranosyl-phlogacanthoside] (7) and galanolactone (8) along with stigmasterol (9), stigmasta- 5,22-dien-7-on-3ß-ol (10), 5-(decahydro-1,1,4a-trimethyl-6-methylene-5-yl)-3-methylpent-2- enal (11), stigmasterol glucoside (12) and stigmast-4-en-3-one (13) from F. hispida Linn., respectively, were isolated. The different extracts of the barks and leaves of these plants along with the isolated compounds had antioxidant and hyploglycemic activities. Conclusions: The five triterpenoids (1-5) were isolated from the methanol extract of the leaves of F. pomifera, and compounds (6-13) were isolated from the chloroform extract of the barks of F. hispida. Methanol extract of the leaves of F. pomifera and the chloroform extract of the barks of F. hispida; compounds (1-13) isolated from these two plants reduced DPPH free radicals in a concentrationdependent manner. It was also observed that the methanol and chloroform extracts of the plants, F. pomifera and F. hispida respectively, and the compounds (1, 6 & 7) exhibited anti-diabetic properties and also caused a highly significant reduction in the blood glucose levels of normal rats.

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Development and Validation of a UHPLC-qTOF MS Method for the Determination of Sorbitol-Based Nuclear Clarifying Agents in Food Simulants after Migration from Food Contact Materials

Applied Sciences ◽

10.3390/app11093789 ◽

2021 ◽

Vol 11 (9) ◽

pp. 3789

Author(s):

Emmanouil D. Tsochatzis ◽

Georgios Theodoridis ◽

Helen G. Gika

Keyword(s):

A Posteriori ◽

Contact Materials ◽

Food Contact ◽

Food Simulants ◽

Target Analytes ◽

Commission Regulation ◽

Development And Validation ◽

Migration Testing ◽

Analytical Standards

Nuclear clarifying agents (NCAs) are a class of substances frequently used as additives in the production of polymers to improve their physical properties. Some are EU regulated under Commission Regulation (EU) no. 10/2011 can be used as additives in the production of food contact plastics. However, limited analytical methods for their analysis are currently available, in part due to poor solubility in most common organic solvents and lack of analytical standards of known purity. In this work, a simple and sensitive method was developed to analyze 4 EU-regulated sorbitol-based nucleating agents in food simulants, following solubility studies to establish effective solvents. The method was shown to be accurate and precise and can be used with official food simulant D1 (50% v/v ethanol/H2O). Application to other ethanolic simulants is also possible, but due to solubility issues, a posteriori conversion of those simulants into simulant D1 is required. Finally, the method was applied to quantify the target analytes in simulants after migration testing with polypropylene (PP) beverage cups.

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Pyrrolidinyl Synthetic Cathinones α-PHP and 4F-α-PVP Metabolite Profiling Using Human Hepatocyte Incubations

International Journal of Molecular Sciences ◽

10.3390/ijms22010230 ◽

2020 ◽

Vol 22 (1) ◽

pp. 230

Author(s):

Jeremy Carlier ◽

Xingxing Diao ◽

Raffaele Giorgetti ◽

Francesco P. Busardò ◽

Marilyn A. Huestis

Keyword(s):

Metabolite Profiling ◽

Human Liver ◽

Liver Microsomes ◽

Drug Market ◽

Metabolite Profile ◽

Illegal Drug ◽

Human Hepatocyte ◽

Synthetic Cathinones ◽

Metabolic Fate ◽

Analytical Standards

For more than ten years, new synthetic cathinones (SCs) mimicking the effects of controlled cocaine-like stimulants have flooded the illegal drug market, causing numerous intoxications and fatalities. There are often no data on the pharmacokinetics of these substances when they first emerge onto the market. However, the detection of SC metabolites is often critical in order to prove consumption in clinical and forensic settings. In this research, the metabolite profile of two pyrrolidinyl SCs, α-pyrrolidinohexaphenone (α-PHP) and 4′′-fluoro-α-pyrrolidinovalerophenone (4F-α-PVP), were characterized to identify optimal intake markers. Experiments were conducted using pooled human hepatocyte incubations followed by liquid chromatography–high-resolution tandem mass spectrometry and data-mining software. We suggest α-PHP dihydroxy-pyrrolidinyl, α-PHP hexanol, α-PHP 2′-keto-pyrrolidinyl-hexanol, and α-PHP 2′-keto-pyrrolidinyl as markers of α-PHP use, and 4F-α-PVP dihydroxy-pyrrolidinyl, 4F-α-PVP hexanol, 4F-α-PVP 2′-keto-pyrrolidinyl-hexanol, and 4F-α-PVP 2′-keto-pyrrolidinyl as markers of 4F-α-PVP use. These results represent the first data available on 4F-α-PVP metabolism. The metabolic fate of α-PHP was previously studied using human liver microsomes and urine samples from α-PHP users. We identified an additional major metabolite (α-PHP dihydroxy-pyrrolidinyl) that might be crucial for documenting exposure to α-PHP. Further experiments with suitable analytical standards, which are yet to be synthesized, and authentic specimens should be conducted to confirm these results.

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Current Trends and Challenges for Rapid SMART Diagnostics at Point-of-Site Testing for Marine Toxins

Sensors ◽

10.3390/s21072499 ◽

2021 ◽

Vol 21 (7) ◽

pp. 2499

Author(s):

Michael Dillon ◽

Maja A. Zaczek-Moczydlowska ◽

Christine Edwards ◽

Andrew D. Turner ◽

Peter I. Miller ◽

...

Keyword(s):

Method Development ◽

Regulatory Control ◽

Detection Methods ◽

Control Individual ◽

Mouse Bioassay ◽

Future Market ◽

Site Testing ◽

Wide Range ◽

Development And Validation ◽

Analytical Standards

In the past twenty years marine biotoxin analysis in routine regulatory monitoring has advanced significantly in Europe (EU) and other regions from the use of the mouse bioassay (MBA) towards the high-end analytical techniques such as high-performance liquid chromatography (HPLC) with tandem mass spectrometry (MS). Previously, acceptance of these advanced methods, in progressing away from the MBA, was hindered by a lack of commercial certified analytical standards for method development and validation. This has now been addressed whereby the availability of a wide range of analytical standards from several companies in the EU, North America and Asia has enhanced the development and validation of methods to the required regulatory standards. However, the cost of the high-end analytical equipment, lengthy procedures and the need for qualified personnel to perform analysis can still be a challenge for routine monitoring laboratories. In developing regions, aquaculture production is increasing and alternative inexpensive Sensitive, Measurable, Accurate and Real-Time (SMART) rapid point-of-site testing (POST) methods suitable for novice end users that can be validated and internationally accepted remain an objective for both regulators and the industry. The range of commercial testing kits on the market for marine toxin analysis remains limited and even more so those meeting the requirements for use in regulatory control. Individual assays include enzyme-linked immunosorbent assays (ELISA) and lateral flow membrane-based immunoassays (LFIA) for EU-regulated toxins, such as okadaic acid (OA) and dinophysistoxins (DTXs), saxitoxin (STX) and its analogues and domoic acid (DA) in the form of three separate tests offering varying costs and benefits for the industry. It can be observed from the literature that not only are developments and improvements ongoing for these assays, but there are also novel assays being developed using upcoming state-of-the-art biosensor technology. This review focuses on both currently available methods and recent advances in innovative methods for marine biotoxin testing and the end-user practicalities that need to be observed. Furthermore, it highlights trends that are influencing assay developments such as multiplexing capabilities and rapid POST, indicating potential detection methods that will shape the future market.

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Exploring Secondary Metabolite Profiles of Stachybotrys spp. by LC-MS/MS

Toxins ◽

10.3390/toxins11030133 ◽

2019 ◽

Vol 11 (3) ◽

pp. 133 ◽

Cited By ~ 3

Author(s):

Annika Jagels ◽

Viktoria Lindemann ◽

Sebastian Ulrich ◽

Christoph Gottschalk ◽

Benedikt Cramer ◽

...

Keyword(s):

Secondary Metabolites ◽

Future Research ◽

Structural Modifications ◽

Metabolite Profiles ◽

The Individual ◽

First Time ◽

Analytical Standards ◽

Respective Species

The genus Stachybotrys produces a broad diversity of secondary metabolites, including macrocyclic trichothecenes, atranones, and phenylspirodrimanes. Although the class of the phenylspirodrimanes is the major one and consists of a multitude of metabolites bearing various structural modifications, few investigations have been carried out. Thus, the presented study deals with the quantitative determination of several secondary metabolites produced by distinct Stachybotrys species for comparison of their metabolite profiles. For that purpose, 15 of the primarily produced secondary metabolites were isolated from fungal cultures and structurally characterized in order to be used as analytical standards for the development of an LC-MS/MS multimethod. The developed method was applied to the analysis of micro-scale extracts from 5 different Stachybotrys strains, which were cultured on different media. In that process, spontaneous dialdehyde/lactone isomerization was observed for some of the isolated secondary metabolites, and novel stachybotrychromenes were quantitatively investigated for the first time. The metabolite profiles of Stachybotrys species are considerably influenced by time of growth and substrate availability, as well as the individual biosynthetic potential of the respective species. Regarding the reported adverse effects associated with Stachybotrys growth in building environments, combinatory effects of the investigated secondary metabolites should be addressed and the role of the phenylspirodrimanes re-evaluated in future research.

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