Chiral Forms of 4-(2',4'-Difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic Acid (Flobufen) and Its Metabolite.Synthesis and Basic Biological Properties

1997 ◽  
Vol 62 (3) ◽  
pp. 498-509 ◽  
Author(s):  
Miroslav Kuchař ◽  
Marie Poppová ◽  
Antonín Jandera ◽  
Vladimíra Panajotovová ◽  
Hana Zůnová ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Biological Activities ◽  
Biological Properties ◽  
Optical Isomers ◽  
Clinical Testing ◽  
Chemical Parameters ◽  
Physico Chemical ◽  
Oxobutanoic Acid

4-(2',4'-Difluorobiphenyl-4-yl)-2-methyl-4-oxobutanoic acid (1, flobufen) is subjected to clinical testing in the treatment of rheumatoid arthritis. Owing to the occurrence of a centre of chirality, the compound exists in two enantiomers, and its major human metabolite, viz. 4-(2',4'-difluorobiphenyl-4-yl)-4-hydroxy-2-methylbutanoic acid isolated in the lactone form (2), possesses two chiral centres, making possible the existence of four stereoisomers. All of the optical isomers of the substances 1 and 2 were prepared. For flobufen (1), the racemate was separated into the stereoisomers by using the salts 3 with R-(+)- or S-(-)-1-phenylethylamine. The pairs of stereoisomers of 2, obtained by reduction of R-(+)-flobufen or the S-(-)-enantiomer, were separated by column chromatography. The physico-chemical parameters of the optical isomers were determined and some biological activities were evaluated in both in vitro and in vivo models.

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 Rouse model with transient intramolecular contacts on a timescale of seconds recapitulates folding and fluctuation of yeast chromosomes

2019 ◽  
Vol 47 (12) ◽  
pp. 6195-6207 ◽  
Author(s):  
Marius Socol ◽  
Renjie Wang ◽  
Daniel Jost ◽  
Pascal Carrivain ◽  
Cédric Vaillant ◽  
...  
Keyword(s):  
Structural Properties ◽  
Single Particle Tracking ◽  
Chemical Parameters ◽  
Chromosome Conformation ◽  
Formation Reaction ◽  
Rouse Model ◽  
Physico Chemical ◽  
Capture Techniques

Abstract DNA folding and dynamics along with major nuclear functions are determined by chromosome structural properties, which remain, thus far, elusive in vivo. Here, we combine polymer modeling and single particle tracking experiments to determine the physico-chemical parameters of chromatin in vitro and in living yeast. We find that the motion of reconstituted chromatin fibers can be recapitulated by the Rouse model using mechanical parameters of nucleosome arrays deduced from structural simulations. Conversely, we report that the Rouse model shows some inconsistencies to analyze the motion and structural properties inferred from yeast chromosomes determined with chromosome conformation capture techniques (specifically, Hi-C). We hence introduce the Rouse model with Transient Internal Contacts (RouseTIC), in which random association and dissociation occurs along the chromosome contour. The parametrization of this model by fitting motion and Hi-C data allows us to measure the kinetic parameters of the contact formation reaction. Chromosome contacts appear to be transient; associated to a lifetime of seconds and characterized by an attractive energy of –0.3 to –0.5 kBT. We suggest attributing this energy to the occurrence of histone tail-DNA contacts and notice that its amplitude sets chromosomes in ‘theta’ conditions, in which they are poised for compartmentalization and phase separation.

scholarly journals Biological Properties of 6-Gingerol: A Brief Review

2014 ◽  
Vol 9 (7) ◽  
pp. 1934578X1400900 ◽  
Author(s):  
Shaopeng Wang ◽  
Caihua Zhang ◽  
Guang Yang ◽  
Yanzong Yang
Keyword(s):  
Fruits And Vegetables ◽  
Biological Activities ◽  
Zingiber Officinale ◽  
Biological Properties ◽  
Anticancer Activities ◽  
Inhibition Of Angiogenesis ◽  
Underlying Mechanisms ◽  
Pharmacologically Active

Numerous studies have revealed that regular consumption of certain fruits and vegetables can reduce the risk of many diseases. The rhizome of Zingiber officinale (ginger) is consumed worldwide as a spice and herbal medicine. It contains pungent phenolic substances collectively known as gingerols. 6-Gingerol is the major pharmacologically-active component of ginger. It is known to exhibit a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation. 6-Gingerol has been found to possess anticancer activities via its effect on a variety of biological pathways involved in apoptosis, cell cycle regulation, cytotoxic activity, and inhibition of angiogenesis. Thus, due to its efficacy and regulation of multiple targets, as well as its safety for human use, 6-gingerol has received considerable interest as a potential therapeutic agent for the prevention and/or treatment of various diseases. Taken together, this review summarizes the various in vitro and in vivo pharmacological aspects of 6-gingerol and the underlying mechanisms.

scholarly journals Propolis: A Complex Natural Product with a Plethora of Biological Activities That Can Be Explored for Drug Development

2015 ◽  
Vol 2015 ◽  
pp. 1-29 ◽  
Author(s):  
Ricardo Silva-Carvalho ◽  
Fátima Baltazar ◽  
Cristina Almeida-Aguiar
Keyword(s):  
Chemical Composition ◽  
Biological Activities ◽  
Clinical Effectiveness ◽  
Biological Properties ◽  
New Drugs ◽  
Published Data ◽  
Alternative Source ◽  
Scientific Attention

The health industry has always used natural products as a rich, promising, and alternative source of drugs that are used in the health system. Propolis, a natural resinous product known for centuries, is a complex product obtained by honey bees from substances collected from parts of different plants, buds, and exudates in different geographic areas. Propolis has been attracting scientific attention since it has many biological and pharmacological properties, which are related to its chemical composition. Severalin vitroandin vivostudies have been performed to characterize and understand the diverse bioactivities of propolis and its isolated compounds, as well as to evaluate and validate its potential. Yet, there is a lack of information concerning clinical effectiveness. The goal of this review is to discuss the potential of propolis for the development of new drugs by presenting published data concerning the chemical composition and the biological properties of this natural compound from different geographic origins.

scholarly journals Characterization of Andean Blueberry in Bioactive Compounds, Evaluation of Biological Properties and in vitro Bioaccessibility

2020 ◽  
Author(s):  
Nieves Baenas ◽  
Jenny Ruales ◽  
Diego A. Moreno ◽  
Daniel Alejandro Barrio ◽  
Carla M. Stinco ◽  
...  
Keyword(s):  
Antioxidant Capacity ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
In Vitro Digestion ◽  
Biological Properties ◽  
Wide Range ◽  
Zebrafish Embryogenesis

Andean blueberries are wild berries grown and consumed in Ecuador which contain high values of bioactive compounds, mainly anthocyanins, with powerful antioxidant activity. The aim of this study was to evaluate the profile and contents of (poly)phenols and carotenoids in Andean blueberry by HPLC-DAD-MSn and determine a wide range of its biological activities. The antioxidant capacity of this fruit was evaluated in vitro by three different methods and in vivo using the zebrafish animal model, also the toxicity effect was determined by the zebrafish embryogenesis test. Besides, the antimicrobial activity and the capacity of Andean blueberry to produce hemagglutination in blood cells were evaluated. Finally, the bioaccessibility of (poly)phenols and related antioxidant capacity were determined in the different phases of an in vitro digestion. The global results indicated no toxicity of Andean blueberry, weakly bacteriostatic activity, and high contents of anthocyanins and antioxidant capacity, which were partially bioaccesible in vitro (~ 50 % at the final intestinal step), contributing to the knowledge of its health benefits for consumers and its potential use in the food and pharmaceutical industry as functional ingredient.

Advances on Quinazoline Based Congeners for Anticancer Potential

2021 ◽  
Vol 25 ◽  
Author(s):  
Parul Grover ◽  
Monika Bhardwaj ◽  
Garima Kapoor ◽  
Lovekesh Mehta ◽  
Roma Ghai ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Biological Properties ◽  
Anticancer Compounds ◽  
In Vivo Models ◽  
Appropriate Treatment

: The heterocyclic compounds have a great significance in medicinal chemistry because they have extensive biological activities. Cancer is globally the leading cause of death and it is a challenge to develop an appropriate treatment for the management of cancer. Continuous efforts are being made to find a suitable medicinal agent for cancer therapy. Nitrogen-containing heterocycles have received noteworthy attention due to their wide and distinctive pharmacological activities. One of the most important nitrogen-containing heterocycles in medicinal chemistry is ‘quinazoline’ that possesses a wide spectrum of biological properties. This scaffold is an important pharmacophore and is considered a privileged structure. The various substituted quinazolines displayed anticancer activity against different types of cancer. This review highlights the recent advances in quinazoline based molecules as anticancer agents. Several in-vitro and in-vivo models used along with the results are also included. A subpart briefing natural quinazoline containing anticancer compounds is also incorporated in the review.

scholarly journals Synthesis, characterization, biological activities, and catalytic applications of alcoholic extract of saffron (Crocus sativus) flower stigma-based gold nanoparticles

2021 ◽  
Vol 10 (1) ◽  
pp. 230-245
Author(s):  
Fahad A. Alhumaydhi ◽  
Ibrahim Khan ◽  
Abdur Rauf ◽  
Muhammad Nasimullah Qureshi ◽  
Abdullah S. M. Aljohani ◽  
...  
Keyword(s):  
Gold Nanoparticles ◽  
Biological Activities ◽  
Inhibitory Effect ◽  
Biological Properties ◽  
Crocus Sativus ◽  
Alcoholic Extract ◽  
X Ray ◽  
Vis Spectroscopy

Abstract Currently, nanotechnology is gaining massive attention compared to conventional methods as the biosynthesis of plant-based nanoparticles is considered safe, effective, and ecofriendly. Therefore, keeping in view the importance of nanotechnology, the present study was designed to synthesize, characterize, and evaluate the biological effectiveness of saffron stigma-based gold nanoparticles (SS-AuNPs) for their in vitro and in vivo biological properties. These gold nanoparticles were characterized by UV–Vis spectroscopy, Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), energy-dispersive X-ray spectroscopy (EDX), and X-ray diffraction (XRD). The highest antibacterial effect was observed by the saffron extract against Escherichia coli (22 mm). SS-AuNPs significantly inhibited the activity of enzyme urease (54.98%) and CA-II (64.29%). However, the nonsignificant inhibitory effect was observed in the case of α-chymotrypsin. Maximum analgesic (84.98%) and antiinflammatory (88.98%) effects were observed for SS-AuNPs (10 mg/kg). Similarly, SS-AuNPs demonstrated a significant (P < 0.01) sedative effect at all tested doses.

scholarly journals Underutilised fruits: a review of phytochemistry and biological properties

2018 ◽  
Vol 1 ◽  
Author(s):  
Ahmad Hasan Salahuddin Mirfat ◽  
Ismail Amin ◽  
Kassim Nur Kartinee ◽  
Hamid Muhajir ◽  
Mat Ali Mohd Shukri
Keyword(s):  
Current Knowledge ◽  
Biological Activities ◽  
Sustainable Use ◽  
Biological Properties ◽  
Fruit Species ◽  
Health Promoting ◽  
Health Significance ◽  
Canarium Odontophyllum

Underutilised fruits are not only important sources of food and nutrition, but also secure household income especially for rural and farm communities. However, some of the underutilised fruits have not received much attention as compared to commercial fruits. This could be due to their lack of knowledge of their potential values. Hence, information about their health promoting properties is critical to increase the value of underutilised fruit species to enhance their preservation and sustainable use in strengthening food, nutrition, health and livelihood security. This article aims to provide a comprehensive review on the phytochemical properties and biological activities of underutilised fruit species grown in Malaysia focussing on health promoting aspects. With regard to phytochemistry, only 21 species of underutilised fruits have been identified and quantified. Phytochemical investigations of various parts of the fruits have revealed the presence of over 100 phytochemicals which are phenolics, terpenoids, carotenoids and other miscellaneous compounds. About 51 underutilised fruit species have been explored for interesting biological activities (antioxidant, antimicrobial, anticholinesterase, cytotoxicity, antiatherosclerotic, antihyperlipidemia, antidiabetic, cytoprotective, cardioprotective and antiplatelet activities) supporting their diverse traditional uses. Different parts of the fruits have been analysed mainly in vitro and barely in vivo, with pulp being the most dominant. Of all the underutilised fruits studied, Mangifera species and Canarium odontophyllum have been the major focus for researchers. The gaps obtained from this review create further research opportunities to add to the current knowledge of health promoting properties of underutilised fruits in Malaysia. More studies are needed to confirm the health significance and explain their mechanisms of action in order to fully understand the real potential of this underutilised fruit species.

scholarly journals Cartwright's method as a physico-chemical marker of antimonium crudum biological effect

2021 ◽  
Vol 17 (2) ◽  
pp. 14-14
Author(s):  
Hannah MG Mota ◽  
Ana Carla Aparicio ◽  
Larissa Helen Silva Oliveira ◽  
Renata Rossettini Palombo Pedro ◽  
Sandra AG Pinto ◽  
...  
Keyword(s):  
Biological Effects ◽  
Electric Signal ◽  
Chemical Marker ◽  
Chemical Parameters ◽  
Monocyte Migration ◽  
Physico Chemical ◽  
Methylene Violet ◽  
One Way Anova

Mice bearing Leishmania (L) amazonensis infection and treated with Antimonium crudum (AC) 30cH presented significant reduction of the monocyte migration to the site of infection with clinical improvement. In vitro, the treatment of infected macrophages with AC 30cH produced inhibition of the parasite-induced peaks of CCL2 (a chemokine for monocytes migration) and inhibition of lysosome activity, explaining the results obtained previously in vivo. In the following studies, physical-chemical parameters of the remedy and respective controls were evaluated, to search for a correlation with the former described biological effects. The study of polarity changes in different water-based dilutions of AC using Cartwright´s method, revealed dilution-dependent variations in the absorbance of three solvatochromic dyes ET 33, BDN and methylene Violet (MV), used as “probes” to evaluate the dipole features of the medicine. The electrical activity of the homeopathic preparations appears to be dilution-dependent and related to their biological effects. Further experiments were performed using samples of the supernatant of infected macrophages after 96 hours of incubation with AC in different dilutions. These samples were processed using the same procedures as used for the original medicines and were analyzed by MV method. All tested potencies presented a sharp increase of absorbance at 580 nm, in relation to all controls (supernatant from untreated cells and cells treated with succussed water), as performed by one-way ANOVA, being F = 176.208; p = 0.001 and ?2 = 0.988. This results strongly suggest that biological systems could amplify the electric signal and the following changes in the medium polarity.

scholarly journals Some biological activities of pigments extracted from Micrococcus roseus (PTCC 1411) and Rhodotorula glutinis (PTCC 5257)

2016 ◽  
Vol 29 (4) ◽  
pp. 684-695 ◽  
Author(s):  
Hossein Rostami ◽  
Hassan Hamedi ◽  
Mahmoud Yolmeh
Keyword(s):  
Antioxidant Activity ◽  
Biological Activities ◽  
Rhodotorula Glutinis ◽  
Biological Properties ◽  
Gram Positive Bacteria ◽  
Synthetic Pigments ◽  
Micrococcus Roseus ◽  
Higher Sensitivity

The importance of replacing synthetic pigments with natural types is increasing day by day in the food industry due to the harmful effects of some synthetic pigments. Microorganisms are a major source of natural pigments, which nowadays have attracted the attention of researchers. In this study, carotenoid pigments were produced by Micrococcus roseus and Rhodotorula glutinis, and some of their biological properties such as antimicrobial, antioxidant, anticancer, and anti-inflammatory activities were evaluated. Given the results, bacteria, especially gram-positive bacteria, had higher sensitivity to the pigments extracted from M. roseus (PEM) and R. glutinis (PER) compared to molds so that Bacillus cereus and Alternaria citri had the highest and the lowest sensitivity, respectively. PER showed a higher antioxidant activity compared with PEM in the various methods of measuring antioxidant activity. In vitro and in vivo anti-tumor-promoting activities of PER were measured significantly more than PEM ( P <0.05). Both pigment extracts remarkably inhibited the 12- O-tetradecanoylphorbol-13-acetate (TPA)-induced inflammation, so that ID50 (50% inhibitory dose) of PEM and PER were 0.22 and 0.09 mg/ear, respectively.

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