scholarly journals Study on pharmacological properties and cell absorption metabolism of novel daidzein napsylates

2021 ◽  
Vol 8 (1) ◽  
pp. 201475
Author(s):  
Yanxiao Jiao ◽  
Jing Peng ◽  
Xinglin Ye ◽  
Huanan Hu ◽  
Lijun Gan ◽  
...  
Keyword(s):  
High Performance ◽  
Biological Activities ◽  
Cell Uptake ◽  
Pharmacological Properties ◽  
Uridine Diphosphate ◽  
Structure Property ◽  
Structure Property Relationships ◽  
Pharmaceutical Properties ◽  
Sulfate Conjugate

Novel daidzein napsylates (DD4 and DD5) were synthesized by microwave irradiation, according to structural modification of daidzein (DAI) using the principle of pharmacokinetic transformation. The pharmacological properties of DD4 and DD5 were evaluated via high performance liquid chromatography (HPLC) and calculated based on the drug design software C hem A xon 16.1.18. The cell uptake changes of DD4 and DD5 were investigated to analyse the structure–property relationship. The metabolisms of DD4 and DD5 were analysed by HPLC-mass spectrometry in human aortic vascular smooth muscle cells (HAVSMCs) and their possible metabolic pathways were inferred in vivo . The results showed that the solubility of DD4 and DD5 was increased by 2.79 × 10 5 and 2.16 × 10 5 times compared to that of DAI, separately, in ethyl acetate. The maximum absorption rates of DD4 and DD5 were enhanced by 4.3–4.5 times relative to DAI. Preliminary studies on metabolites of DD4 and DD5 in HAVSMCs showed that DD4 and DD5 were hydrolysed into DAI under the action of intracellular hydrolase in two ways, ester hydrolysis or ether hydrolysis. Then, DAI was combined with glucuronic acid to form daidzein monoglucuronate under the action of uridine diphosphate (UDP)-glucuronidase. Meanwhile, it was also found that metabolite M5 of DD5 could undergo glucuronidation under the action of UDP-glucuronosyltransferase and competitive sulphation under the action of sulphotransferase to produce its sulfate conjugate M7. Analysis of structure–property relationships indicated that the absorption and utilization of drugs is closely relative to the physical properties and could be improved by adjusting the liposolubility. The pharmaceutical properties were optimized comprehensively after DAI was modified by naphthalene sulphonate esterification. This indicates that this kind of derivatives may have relatively good absorption and transport characteristics and biological activities in vivo . The research on biological activities of the new derivatives (DD4 and DD5) is ongoing in our laboratory.

Tamarix articulata (T. articulata) - An Important Halophytic Medicinal Plant with Potential Pharmacological Properties

2019 ◽  
Vol 20 (4) ◽  
pp. 285-292 ◽  
Author(s):  
Abdullah M. Alnuqaydan ◽  
Bilal Rah
Keyword(s):  
Medicinal Plant ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
In Vivo Model ◽  
Drug Candidate ◽  
Phytochemical Analysis ◽  
Pharmacological Properties

Background:Tamarix Articulata (T. articulata), commonly known as Tamarisk or Athal in Arabic region, belongs to the Tamaricaece species. It is an important halophytic medicinal plant and a good source of polyphenolic phytochemical(s). In traditional medicines, T. articulata extract is commonly used, either singly or in combination with other plant extracts against different ailments since ancient times.Methods:Electronic database survey via Pubmed, Google Scholar, Researchgate, Scopus and Science Direct were used to review the scientific inputs until October 2018, by searching appropriate keywords. Literature related to pharmacological activities of T. articulata, Tamarix species, phytochemical analysis of T. articulata, biological activities of T. articulata extracts. All of these terms were used to search the scientific literature associated with T. articulata; the dosage of extract, route of administration, extract type, and in-vitro and in-vivo model.Results:Numerous reports revealed that T. articulata contains a wide spectrum of phytochemical(s), which enables it to have a wide window of biological properties. Owing to the presence of high content of phytochemical compounds like polyphenolics and flavonoids, T. articulata is a potential source of antioxidant, anti-inflammatory and antiproliferative properties. In view of these pharmacological properties, T. articulata could be a potential drug candidate to treat various clinical conditions including cancer in the near future.Conclusion:In this review, the spectrum of phytochemical(s) has been summarized for their pharmacological properties and the mechanisms of action, and the possible potential therapeutic applications of this plant against various diseases discussed.

scholarly journals In vivo efficacy and metabolism of the antimalarial cycleanine and improved in vitro antiplasmodial activity of novel semisynthetic analogues

2020 ◽  
Author(s):  
Fidelia Ijeoma Uche ◽  
Xiaozhen Guo ◽  
Jude Okokon ◽  
Imran Ullah ◽  
Paul Horrocks ◽  
...  
Keyword(s):  
Metabolic Pathways ◽  
High Performance ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Antiplasmodial Activity ◽  
Survival Times ◽  
Antiproliferative Effects ◽  
Future Evaluation

Bisbenzylisoquinoline (BBIQ) alkaloids are a diverse group of natural products that demonstrate a range of biological activities. In this study, the in vitro antiplasmodial activity of three BBIQ alkaloids (cycleanine (1), isochondodendrine (2) and 2′-norcocsuline (3)) isolated from the Triclisia subcordata Oliv. medicinal plant traditionally used for the treatment of malaria in Nigeria are studied alongside two semi-synthetic analogues (4 and 5) of cycleanine. The antiproliferative effects against a chloroquine-resistant Plasmodium falciparum strain were determined using a SYBR Green 1 fluorescence assay. The in vivo antimalarial activity of cycleanine (1) is then investigated in suppressive, prophylactic and curative murine malaria models after infection with a chloroquine-sensitive Plasmodium berghei strain. BBIQ alkaloids (1–5) exerted in vitro antiplasmodial activities with IC50 at low micromolar concentrations with the two semi-synthetic cycleanine analogues showing an improved potency and selectivity than cycleanine. At oral doses of 25 and 50mg/kg body weight of infected mice, cycleanine suppressed the levels of parasitaemia, and increased mean survival times significantly compared to the control groups. The metabolites and metabolic pathways of cycleanine (1) were also studied using high performance liquid chromatography electrospray ionization tandem mass spectrometry. Twelve novel metabolites were detected in rats after intragastic administration of cycleanine. The metabolic pathways of cycleanine were demonstrated to involve hydroxylation, dehydrogenation, and demethylation. Overall, these in vitro and in vivo results provide a basis for the future evaluation of cycleanine and its analogues as leads for further development.

Structure–property relationships of high-performance polyethylene fibres

1989 ◽  
Vol 116 (1) ◽  
pp. 179-195 ◽  
Author(s):  
A. Schaper ◽  
D. Zenke ◽  
E. Schulz ◽  
R. Hirte ◽  
M. Taege
Keyword(s):  
High Performance ◽  
Structure Property ◽  
Structure Property Relationships

scholarly journals Selective Modulation of Follicle-Stimulating Hormone Signaling Pathways with Enhancing Equine Chorionic Gonadotropin/Antibody Immune Complexes

Endocrinology ◽  
2010 ◽  
Vol 151 (6) ◽  
pp. 2788-2799 ◽  
Author(s):  
Vanessa Wehbi ◽  
Jérémy Decourtye ◽  
Vincent Piketty ◽  
Guillaume Durand ◽  
Eric Reiter ◽  
...  
Keyword(s):  
Chorionic Gonadotropin ◽  
Biological Activities ◽  
Target Cells ◽  
Pharmacological Properties ◽  
Dairy Goats ◽  
Glycoprotein Hormone ◽  
Guanine Nucleotide Binding Protein ◽  
Equine Chorionic Gonadotropin ◽  
The Impact

The injection of equine chorionic gonadotropin (eCG) in dairy goats induces the production of anti-eCG antibodies (Abs) in some females. We have previously shown that Abs negatively modulate the LH and FSH-like bioactivities of eCG, in most cases, compromising fertility in treated females. Surprisingly, we found out that some anti-eCG Abs improved fertility and prolificity of the treated females, in vivo. These Abs, when complexed with eCG, enhanced LH and FSH ability to induce steroidogenesis on specific target cells, in vitro. In the present study, we analyzed the impact of three eCG/anti-eCG Ab-enhancing complexes on two transduction mechanisms triggered by the FSH receptor: guanine nucleotide-binding protein αS-subunit/cAMP/protein kinase A (PKA) and β-arrestin-dependent pathways, respectively. In all cases, significant enhancing effects were observed on ERK phosphorylation compared with eCG alone. However, cAMP production and PKA activation induced by eCG could be differently modulated by Abs. By using a pharmacological inhibitor of PKA and small interfering RNA-mediated knock-down of endogenous β-arrestin 1 and 2, we demonstrated that signaling bias was induced and was clearly dependent on the complexed Ab. Together, our data show that eCG/anti-eCG Ab-enhancing complexes can differentially modulate cAMP/PKA and β-arrestin pathways as a function of the complexed Ab. We hypothesize that enhancing Abs may change the eCG conformation, the immune complex acquiring new “biased” pharmacological properties ultimately leading to the physiological effects observed in vivo. The modulation of ligand pharmacological properties by Abs opens promising research avenues towards the optimization of glycoprotein hormone biological activities and, more generally, the development of new therapeutics.

scholarly journals Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

2019 ◽  
Vol 20 (17) ◽  
pp. 4238 ◽  
Author(s):  
Yaqi Ren ◽  
Chunlan Wang ◽  
Jiakun Xu ◽  
Shuaiyu Wang
Keyword(s):  
Furan Ring ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Coffee Beans ◽  
Anti Cancer ◽  
Underlying Mechanisms ◽  
Target Alternative ◽  
Anti Inflammation

Cafestol and kahweol are natural diterpenes extracted from coffee beans. In addition to the effect of raising serum lipid, in vitro and in vivo experimental results have revealed that the two diterpenes demonstrate multiple potential pharmacological actions such as anti-inflammation, hepatoprotective, anti-cancer, anti-diabetic, and anti-osteoclastogenesis activities. The most relevant mechanisms involved are down-regulating inflammation mediators, increasing glutathione (GSH), inducing apoptosis of tumor cells and anti-angiogenesis. Cafestol and kahweol show similar biological activities but not exactly the same, which might due to the presence of one conjugated double bond on the furan ring of the latter. This review aims to summarize the pharmacological properties and the underlying mechanisms of cafestol-type diterpenoids, which show their potential as functional food and multi-target alternative medicine.

scholarly journals Fused Filament Fabrication of PEEK: A Review of Process-Structure-Property Relationships

Polymers ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 1665 ◽  
Author(s):  
Ali Reza Zanjanijam ◽  
Ian Major ◽  
John G. Lyons ◽  
Ugo Lafont ◽  
Declan M. Devine
Keyword(s):  
High Performance ◽  
Space Station ◽  
Weight Ratio ◽  
High Strength ◽  
Structure Property ◽  
Fused Filament Fabrication ◽  
Space Applications ◽  
Structure Property Relationships ◽  
Complex Design ◽  
Process Structure

Poly (ether ether ketone) (PEEK) is a high-performance engineering thermoplastic polymer with potential for use in a variety of metal replacement applications due to its high strength to weight ratio. This combination of properties makes it an ideal material for use in the production of bespoke replacement parts for out-of-earth manufacturing purposes, in particular on the International Space Station (ISS). Additive manufacturing (AM) may be employed for the production of these parts, as it has enabled new fabrication pathways for articles with complex design considerations. However, AM of PEEK via fused filament fabrication (FFF) encounters significant challenges, mostly stemming from the semi crystalline nature of PEEK and its associated high melting temperature. This makes PEEK highly susceptible to changes in processing conditions which leads to a large reported variation in the literature on the final performance of PEEK. This has limited the adaption of FFF printing of PEEK in space applications where quality assurance and reproducibility are paramount. In recent years, several research studies have examined the effect of printing parameters on the performance of the 3D-printed PEEK parts. The aim of the current review is to provide comprehensive information in relation to the process-structure-property relationships in FFF 3D-printing of PEEK to provide a clear baseline to the research community and assesses its potential for space applications, including out-of-earth manufacturing.

QSPR Prediction of Retention Times of Methylxanthines and Cotinine by Bioplastic Evolution

2018 ◽  
Vol 3 (1) ◽  
pp. 74-87 ◽  
Author(s):  
Francisco Torrens ◽  
Gloria Castellano
Keyword(s):  
High Performance ◽  
Formation Enthalpy ◽  
Fractal Dimensions ◽  
High Performance Liquid Chromatographic ◽  
Chromatographic Retention ◽  
Structure Property ◽  
Structure Property Relationships ◽  
Prediction Of Retention ◽  
Acquired Characters ◽  
Liquid Chromatographic

High-performance liquid-chromatographic retention times of methylxanthines and cotinine in human plasma and urine are modelled by structure–property relationships. Bioplastic evolution is an evolutionary perspective conjugating the effect of acquired characters, and relations that emerge among the principles of evolutionary indeterminacy, morphological determination and natural selection. It is applied to design co-ordination index, which is used to characterize retentions of methylxanthines, etc. Parameters used to calculate co-ordination index are formation enthalpy, molecular weight and surface area. Morphological and co-ordination indices provide strong correlations. Effect of different types of features like thermodynamic, fractal, etc., are analyzed. The molar formation enthalpy, fractal dimensions, etc. distinguished methylxanthines and cotinine in linear fits. Different behaviour depends on number of C+N+O atoms.

scholarly journals Simultaneous Measurement of Tadehaginoside and its Principal Metabolite in Rats by HPLC–MS/MS and its Application in Pharmacokinetics and Tissue Distribution Study

2021 ◽  
Author(s):  
Cai-Yun Zhang ◽  
Ya-Ting Lu ◽  
Yin-Feng Tan ◽  
Lin Dong ◽  
Zhi-Heng Su ◽  
...  
Keyword(s):  
Tissue Distribution ◽  
High Performance ◽  
Biological Activities ◽  
Intragastric Administration ◽  
Distribution Study ◽  
Chromatography Tandem Mass Spectrometry ◽  
Liquid Chromatography Tandem Mass ◽  
Tissue Distribution Study

Abstract Background Tadehaginoside, an active ingredient isolated from Tadehagi triquetrum L., exhibited various biological activities. However, the pharmacokinetics and tissue-distribution which affects tadehaginoside’s therapeutic actions and application remain elusive.MethodsTo clarify the metabolism of tadehaginoside in vivo, a high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was established to detect the level of tadehaginoside in plasma and eleven tat tissues (brain, heart, liver, spleen, lungs, kidneys, stomach, small intestine, skeletal muscle, body fat, and testes). Besides, this validated method was also successfully applied to the quantitative determination of its metabolite, p-hydroxycinnamic acid (HYD) in plasma. The pharmacokinetic and tissue-distribution of tadehaginoside were investigated by this developed method. ResultsThe pharmacokinetic study indicated that tadehaginoside in plasma of rats with intragastric administration showed relatively low concentration may be due to the formation of its metabolite, and the quick absorption of tadehaginoside was detected following intravenous administration. Tissue-distribution study indicated that kidney and spleen were the major distribution organs for tadehaginoside in rats. ConclusionsThese results could provide clues for exploring the bioactivity of tadehaginoside based on its pharmacokinetic characteristics.

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