Pyrazolopyrimidines in ‘all-natural’ products for erectile dysfunction treatment: the unreliable quality of dietary supplements

Schramek, Nicholas; Wollein, Uwe; Eisenreich, Wolfgang

doi:10.1080/19440049.2014.992980

Cited by 10 publications

(3 citation statements)

References 26 publications

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“…A few researchers have been concluded that pyrazolo[4,3‐ d ]pyrimidine is an anti‐diabetic agent, While Pfizer reported pyrazolo[4,3‐ d ]pyrimidine derivative as PDE−V inhibitor . Moreover, some of the commercially available drugs for the treatment of type‐2 diabetes mellitus belong to the class of dipeptidyl peptidase inhibitors‐4 namely, Anagliptin, Vildagliptin and Saxagliptin.…”

Section: Introductionmentioning

confidence: 99%

Novel Pyrazolo[3,4‐d]pyrimidine‐Containing Amide Derivatives: Synthesis, Molecular Docking, In Vitro and In Vivo Antidiabetic Activity

et al. 2019

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A new series of Pyrazolo [3,4-d]pyrimidine containing amide derivatives (8 a-l) were designed, synthesized, and evaluated for their in vitro α-amylase inhibitory activity. The IC 50 values of the target compounds ranged from 1.60 � 0.48 to 2.04 � 1.20 μM as compared to the standard acarbose 1.73 � 0.05 μM. All the Pyrazolo[3,4-d]pyrimidine amide derivatives displayed good inhibitory activities, while seven analogs (8 d, 8 f, 8 g, 8 h, 8 i, 8 j and 8 k) exhibited more or less equipotent activity with IC 50 values 1.77 � 2.84, 1.65 � 0.45, 1.66 � 2.24, 1.73 � 0.37, 1.60 � 0.48, 1.75 � 0.36 and 1.64 � 0.03 μM respectively. Further, the most potent α-amylase inhibitors 8 d and 8 k were also screened for their in vivo antidiabetic activity against alloxan induced diabetic rat model at the dose of 25 and 50 mg/kg. Oral administration of these tested compounds significantly reduced the fasting blood glucose levels in dose dependent manner. The hypoglycemic effects of these compounds were more evident at 3 h and 5 h after administration of tested compounds which was similar to the effect displayed by the positive control. In addition, the binding energies calculated from the docking studies with the α-amylase enzyme (PDB ID: 1HNY) and biological activities indicate that the compounds containing nitro moiety on the phenyl group contributed significantly towards the antidiabetic activity.[a] Dr.

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Section: Introductionmentioning

confidence: 99%

Novel Pyrazolo[3,4‐d]pyrimidine‐Containing Amide Derivatives: Synthesis, Molecular Docking, In Vitro and In Vivo Antidiabetic Activity

et al. 2019

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“…Schramek et al [77] screened multiple identical samples of herbal supplements for PDE-5is using LC-DAD and LC-MS. They found 14 compounds with the same pyrazolopyrimidine structure similar to sildenafil.…”

Section: Hyphenated Techniquesmentioning

confidence: 99%

Chemical Adulterants in Herbal Medicinal Products: A Review

et al. 2016

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Many herbal medicinal products have been found to contain synthetic prescription drugs as chemical adulterants. This has become evident by the number of toxicity cases and adverse reactions reported in which casualties were reported via analytical techniques that detected the presence of chemical adulterants in them, which could be responsible for their toxicity. The adulteration of herbal medicinal products with synthetic drugs continues to be a serious problem for regulatory agencies. This review provides up to date information on cases of toxicity, major chemical adulterants in herbal medicinal products, and current analytical techniques used for their detection.

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“…However, for some unscrupulous manufacturers, the deliberate addition of chemical ingredients into health foods and CTPMs is a profit-driven practice aiming to intensify the claimed natural health benefits of the products [ 2 ]. Over the past few years, many types of illegal adulterants are being detected in various forms of health foods and CTPMs without labeling, which can lead to potentially serious public health consequences [ 3 – 11 ].…”

Section: Introductionmentioning

confidence: 99%

Simultaneous analysis of 23 illegal adulterated aphrodisiac chemical ingredients in health foods and Chinese traditional patent medicines by ultrahigh performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry

Wang

Zheng

et al. 2018

Journal of Food and Drug Analysis

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This paper presents an application of ultra high-performance liquid-chromatography-quadrupole-TOF high resolution mass spectrometry (UHPLC-Q-TOF HRMS) for simultaneous analysis of 23 illegal adulterated aphrodisiac type chemical ingredients in health foods and Chinese Traditional Patent Medicines (CTPMs). The mass spectrometer was operated in Information Dependent Acquisition (IDA) mode, which provides crucial information for the elemental composition analysis, structure elucidation and quantitative analysis simultaneously. Quantitative analysis was performed using the peak areas of the precursor ions in the XICs. The method validation included assessment of selectivity, sensitivity, calibration curve, accuracy, precision, recovery, matrix effect and stability. The results show good linear relationship with the concentrations of the analytes over wide concentration ranges (e.g., 0.05-10 μg/g for sildenafil) as all the fitting coefficients of determination r are >0.9984. The detection limits (LODs) were in the range of 0.002-0.1 μg/g. The recoveries were able to reach 82.5-103.6%, while the matrix effects ranged from 87.7 to 109.3%. The intra- and inter-day accuracies were in the range of 82.3-113.8%, while the intra- and inter-day precision ranged from 0.4 to 13.6%. Among 40 batches of health foods and 32 batches of CTPMs (including 28 capsules, 32 tablets, 10 liquid and 2 pills) samples, 28 batches of heath foods were positive. The detected chemical ingredients involved sildenafil, tadalafil, aildenafil and sulfoaildenafil. This method can be used for the screening, identification and quantification of illegal adulterated aphrodisiac chemical ingredients in health foods and CTPMs. Moreover, the LC-Q-TOF MS is very useful to structural elucidation of unknown compound.

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Pyrazolopyrimidines in ‘all-natural’ products for erectile dysfunction treatment: the unreliable quality of dietary supplements

Cited by 10 publications

References 26 publications

Novel Pyrazolo[3,4‐d]pyrimidine‐Containing Amide Derivatives: Synthesis, Molecular Docking, In Vitro and In Vivo Antidiabetic Activity

Novel Pyrazolo[3,4‐d]pyrimidine‐Containing Amide Derivatives: Synthesis, Molecular Docking, In Vitro and In Vivo Antidiabetic Activity

Chemical Adulterants in Herbal Medicinal Products: A Review

Simultaneous analysis of 23 illegal adulterated aphrodisiac chemical ingredients in health foods and Chinese traditional patent medicines by ultrahigh performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry

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