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The physicochemical and pharmaceutical properties (pH, peel force, water-vapor permeability, and stretchability) of brand-name and generic ketoprofen products were evaluated and compared. The pHs of Mohrus as a brand-name product and Teikoku as a generic product were low (about 4). Among the other generic products, Patell and Nichi- Iko had a pH of about 4.3 while Frestol, Raynanon, BMD, and Touchron showed a pH of 4.6-5.2, which was in the pH range of normal healthy skin (4.5-6.5). The adhesive force was high (≥ 1.38) for Mohrus as a brand-name product as well as for Teikoku and Patell as generic products, but it was low (≤ 0.57) for the other 5 generic products. The water-vapor permeabilities of Mohrus as a brand-name product and Teikoku and Patell as generic products were low, being less than 1/6 of those for the other 5 generic products. Among the 5 generic products, BMD showed the highest water-vapor permeability (1,330 g/m2), and the other products also showed a value ≥ 1,100 g/m2. The elongatedness of Mohrus was the lowest (15.5 cm), and that of Raynanon was the highest (24.5 cm); the difference was 9 cm. In this study, the physiochemical and pharmaceutical properties of ketoprofen tapes were clarified, which will allow pharmacists to provide products according to the needs of each patient when a brand-name product is changed to a generic one. [ABSTRACT FROM AUTHOR]

One of the significant issues in the biomechanics of the intervertebral discs is the origin of the forces on the spine in the lumbar region. This issue can be gravity and the effects of inertia, muscles, intra-abdominal pressure, fascia, and ligaments. Recently, the 3D printing technique with biocompatible metals is used to strengthen the intervertebral discs. In this study, the three-dimensional printing (3DP) technique was used to fabricate the body of the disc. The prepared disc was multi-component and coated with Hydroxyapatite (HA) bioceramic nanoparticles using the plasma spray technique. To investigate the mechanical properties, the compressive strength test, hardness test, the stress-strain diagram, and the toughness were obtained from mechanical testing. The biological behavior of the disc was investigated in the Simulated Body Fluid (SBF) after 21 days. To characterize HA and coated disc the morphology and phase structure of the surface were evaluated using Scanning Electron Microscope (SEM) and X-ray diffraction (XRD) techniques. The obtained mechanical results of three samples with a metal layer, without metal layer, and metal layer coated with HA nanoparticles were used in the mechanical simulation of the component. The artificial disk is an implant with the ability to maintain movement on the surgical surface, which reduces the side effects of vertebral connection in the destruction of adjacent components. Since the success of using an artificial disk depends on maintaining the mechanical functions of the intervertebral disc, it is useful to study the behavior of the artificial disk under different loads using Finite Element Method (FEM). In this research, the models are evaluated by comparing their behavior with experimental data and FEM data. Then, the elastic modulus and the optimal Poisson ratio were used for the two parts of the nucleus (the central part of the disk) and the annulus (the layers around the nucleus). • Three-dimensional printing technique was used to fabricate the body of the disc. • The prepared disc was multi-component and coated with Hydroxyapatite bioceramic nanoparticles. • The biological behavior of the disc was investigated in the Simulated Body Fluid for 14 and 21 days. • The models are evaluated by comparing their behavior with experimental data and FEM. • Elastic modulus and the optimal Poisson ratio are calculated for the two parts of the nucleus and the annulus. [ABSTRACT FROM AUTHOR]

In this review, the traditional uses, isolated natural substances, plant extracts and biological activities of the Swartzia genus are described. Are also presented how to obtain the crude extracts, phytochemicals separation, isolation and purification, and still equipment using spectrometric identification of these can be seen. For the literature review, were used major databases and search engines, such as: Scielo, Science Direct, Scopus, SciFinder and Web of Science. [ABSTRACT FROM AUTHOR]

This paper reports the changes in various physical properties associated with the derivatization of sulfamethoxazole. The properties studied include moisture content, crystallanity, particle size distribution, porosity, flow, compressibility and compactability. It was found that the derivatives, salicylidene-sulfamethoxazole-Zn(II) • H2O and salicylidene-sulfamethoxazole-Cu(II) • H2O are crystalline substances. The moisture content was found to be highest in salicylidene-sulfamethoxazole-Zn(II) • H2O followed by salicylidene-sulfamethoxazole-Cu(II) • H2O and sulfamethoxazole. The copper complex contained only chemically bonded water, whereas the zinc complex contained both bonded and absorbed water, which affected the strength of the tablets prepared from the three materials accordingly. The particle size decreased on derivatization and complexation with metal ions and the trend was: sulfamethoxazole > salicylidene-sulfamethoxazole-Cu(II) • H2O > salicylidene-sulfamethoxazole-Zn(II) • H2O. This trend was represented by better compactability shown by salicylidene-sulfamethoxazole-Cu(II) • H2O and salicylidene-sulfamethoxazole-Zn(II) • H2O as compared with sulfamethoxazole. Salicylidene-sulfamethoxazole-Zn(II) • H2O had the highest porosity followed by salicylidene-sulfamethoxazole-Cu(II) • H2O, and sulfamethoxazole; this resulted in better compressibility behavior of the complexes. Thus it was observed that salicylidene-sulfamethoxazole-Cu(II) • H2O and salicylidene-sulfamethoxazole-Zn(II) • H2O formed stronger compacts. The values of angle of repose and flow rate show better flow properties for salicylidene-sulfamethoxazole-Cu(II) • H2O as compared with sulfamethoxazole and salicylidene-sulfamethoxazole-Zn(II) • H2O. It was concluded that derivatization substantially changed the pharmaceutical properties, which have important role to play in formulation of solid dosage form. [ABSTRACT FROM AUTHOR]

An appendix is presented which discusses the new route of synthesis on Estetrol (E4) reported by the Good Manufacturing Practice (GMP).

Ajuga bracteosa Wall. ex Benth. is an endangered medicinal herb traditionally used against different ailments. The present study aimed to create new insight into the fundamental mechanisms of genetic transformation and the biological activities of this plant. We transformed the A. bracteosa plant with rol genes of Agrobacterium rhizogenes and raised the regenerants from the hairy roots. These transgenic regenerants were screened for in vitro antioxidant activities, a range of in vivo assays, elemental analysis, polyphenol content, and different phytochemicals found through HPLC. Among 18 polyphenolic standards, kaempferol was most abundant in all transgenic lines. Furthermore, transgenic line 3 (ABRL3) showed maximum phenolics and flavonoids content among all tested plant extracts. ABRL3 also demonstrated the highest total antioxidant capacity (8.16 ± 1 μg AAE/mg), total reducing power, (6.60 ± 1.17 μg AAE/mg), DPPH activity (IC50 = 59.5 ± 0.8 μg/mL), hydroxyl ion scavenging (IC50 = 122.5 ± 0.90 μg/mL), and iron-chelating power (IC50 = 154.8 ± 2 μg/mL). Moreover, transformed plant extracts produced significant analgesic, anti-inflammatory, anticoagulant, and antidepressant activities in BALB/c mice models. In conclusion, transgenic regenerants of A. bracteosa pose better antioxidant and pharmacological properties under the effect of rol genes as compared to wild-type plants. [ABSTRACT FROM AUTHOR]

The synthesis of new compounds with antimicrobial and antiviral properties is a central objective today in the context of the COVID-19 pandemic. Benzimidazole and pyrazole compounds have remarkable biological properties, such as antimicrobial, antiviral, antitumor, analgesic, anti-inflammatory, anti-Alzheimer's, antiulcer, antidiabetic. Moreover, recent literature mentions the syntheses and antimicrobial properties of some benzimidazole–pyrazole hybrids, as well as other biological properties thereof. In this review, we aim to review the methods of synthesis of these hybrids, the antimicrobial activities of the compounds, their correlation with various groups present on the molecule, as well as their pharmaceutical properties. [ABSTRACT FROM AUTHOR]

Medicinal mushrooms have important health benefits and exhibit a broad spectrum of pharmacological activities, including antiallergic, antibacterial, antifungal, anti-inflammatory, antioxidative, antiviral, cytotoxic, immunomodulating, antidepressive, antihyperlipidemic, antidiabetic, digestive, hepatoprotective, neuroprotective, nephroprotective, osteoprotective, and hypotensive activities. The growing interest in mycotherapy requires a strong commitment from the scientific community to expand clinical trials and to propose supplements of safe origin and genetic purity. Bioactive compounds of selected medicinal mushrooms and their effects and mechanisms in in vitro and in vivo clinical studies are reported in this review. Besides, we analyzed the therapeutic use and pharmacological activities of mushrooms. [ABSTRACT FROM AUTHOR]

Four azoimine quinoline derivatives namely (1Z)-N'-(4-fluorophenyl)-2-oxo-N-quinolin-8-ylpropanehydrazonamide (H 2 L-F) ,(1Z)-2-oxo-N′-phenyl-N-quinolin-8-ylpropane hydrazonamide (H 2 L-H) ,(1Z)-N'-(4-nitrophenyl)-2-oxo-N-quinolin-8-ylpropane hydrazonamide (H 2 L-NO 2) and (1Z)-N'-(4-bromophenyl)-2-oxo-N-quinolin-8-ylpropane hydrazonamide (H 2 L-Br) were synthesized and evaluated for their biological activities. At very low concentrations, the four compounds showed a greater antioxidant potential than that of ascorbic acid. The results of the antimicrobial screening indicate that all derivatives have a variable activity against the investigated species, bacteria and fungi. The anti-inflammatory activity of the compounds was found to be in the range of 55–80%. The binding interaction of these molecules with DNA and bovine serum albumin (BSA) was investigated by UV–visible and cyclic voltammetry. The DNA binding study revealed that all the compounds are strongly bound to DNA via intercalation in a spontaneous manner. It was also found that the investigated azoimine quinolines are interacted to BSA with a static quenching process. The choice of these molecules was based on simple synthesis processes, better yield, moderate toxicity, and low cost. Image 1 • New azoimine quinoline H 2 L-F derivative was synthesized. • All compounds could be considered as potential antioxidants. • H 2 L-Br and H 2 L-F show the best anti-inflammatory activity. • The compounds are efficient DNA binders. • Compounds are interacted to BSA with a static quenching process. [ABSTRACT FROM AUTHOR]

The identification of molecules that can modulate RNA or protein function and the subsequent chemical and structural optimization to refine such molecules into drugs is a key activity in drug discovery. Here, we explored the extent to which chemical and structural differences in antisense oligonucleotides, designed as gapmers and capable of recruiting RNase H for target RNA cleavage, can affect their functional properties. To facilitate structure-activity learning, we analyzed two sets of iso-sequential locked nucleic acid (LNA)-modified gapmers, where we systematically varied the number and positions of LNA modifications in the flanks. In total, we evaluated 768 different and architecturally diverse gapmers in HeLa cells for target knockdown activity and cytotoxic potential and found widespread differences in both of these properties. Binding affinity between gapmer and RNA target, as well as the presence of certain short sequence motifs in the gap region, can explain these differences, and we propose statistical and machine-learning models that can be used to predict region-specific, optimal LNA-modification architectures. Once accessible regions in the target of interest have been identified, our results show how to refine and optimize LNA gapmers with improved pharmacological profiles targeting such regions., (Copyright © 2019 The Author(s). Published by Elsevier Inc. All rights reserved.)

In the title compound, C18H15NO3, the isoxazole moiety adopts a shallow envelope conformation, with the C atom bearing the OH group displaced by 0.148 (1) Å from the mean plane through the other four atoms. The mean plane of this ring (all atoms) subtends dihedral angles of 87.19 (6) and 15.51 (7)° with the benzo-furan ring system (r.m.s. deviation = 0.007 Å) and the 4-methylphenyl ring, respectively. In the crystal, mol-ecules are linked by O-H⋯N hydrogen bonds, generating [001] C(5) chains, with adjacent mol-ecules in the chain related by c-glide symmetry. Weak C-H⋯O inter-actions link the chains into a three-dimensional network.

In the title compound, C17H15NO2S, the two C atoms linking the S and carbonyl C atoms of the seven-membered thia-zepine ring are disordered over two sites, with occupancies of 0.511 (4) and 0.489 (4); both disorder components adopt distorted twist-boat conformations. In the crystal, N-H⋯O and C-H⋯O hydrogen bonds link inverted-related mol-ecules into dimers, incorporating R 1 (2)(6) and R 2 (2)(8) ring motifs; the acceptor carbonyl O atom is bifurcated. These dimers are further linked by C-H⋯O hydrogen bonds, forming supra-molecular tapes running along the a axis.