scholarly journals PREDICTION OF ACTIVITY SPECTRA OF SUBSTANCES ASSISTED PREDICTION OF BIOLOGICAL ACTIVITY SPECTRA OF POTENTIAL ANTI-ALZHEIMER’S PHYTOCONSTITUENTS

2017 ◽  
Vol 10 (16) ◽  
pp. 13
Author(s):  
Abhinav Anand ◽  
Neha Sharma ◽  
Navneet Khurana
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
The Other ◽  
Pharmacological Intervention ◽  
Input Line ◽  
In Vivo Evaluation ◽  
Other Hand ◽  
Better Than

Objective: To predict the biological activity of certain phytoconstituents for their anti-AD effects.Methods: Several phytoconstituents were selected on the basis of reported literature. The anti-AD activities of selected phytoconstituents were predicted by employing canonical simplified molecular-input line-entry system obtained from PubChem using PASS online.Results: Several phytoconstituents were predicted to have effects better than marketed drugs under some or the other out of the chosen six areas of pharmacological intervention. On the other hand, several new avenues were predicted in which the in vitro and in vivo evaluation of the phytoconstituents can be made on the basis of PASS predicted activities.Conclusion: PASS is an important tool for virtually screening the compounds of interest for the biological activities of interest. This helps the researchers to streamline the research. However, PASS has its own share of limitations amidst a multitude of merits.

In vitro insulin-mimetic activity and in vivo metallokinetic feature of oxovanadium(IV)porphyrin complexes in healthy rats

2012 ◽  
Vol 16 (01) ◽  
pp. 114-121 ◽  
Author(s):  
Tapan K. Saha ◽  
Yutaka Yoshikawa ◽  
Hirouki Yasui ◽  
Hiromu Sakurai
Keyword(s):  
The Other ◽  
Insulin Mimetic ◽  
Other Hand ◽  
Better Than

We prepared [meso-tetrakis(4-carboxylatophenyl)porphyrinato]oxovanadium(IV) tetrasodium, ([VO(tcpp)]Na4), and investigated its in vitro insulin-mimetic activity and in vivo metallokinetic feature in healthy rats. The results were compared with those of previously proposed insulin-mimetic oxovanadium(IV)porphyrin complexes and oxovanadium(IV) sulphate. The in vitro insulin-mimetic activity and bioavailability of [VO(tcpp)]Na4 were considerably better than those of [meso-tetrakis (1-methylpyridinium-4-yl)porphyrinato]oxovanadium(IV)(4+) tetraperchlorate ([VO(tmpyp)](ClO4)4) and oxovanadium(IV) sulphate. On the other hand, [VO(tcpp)]Na4 and [meso-tetrakis(4-sulfonatophenyl) porphyrinato]oxidovanadate(IV)(4-)([VO(tpps)]) showed very similar in vitro insulin-mimetic activity and in vivo metallokinetic feature in healthy rats. In particular, the order of in vitro insulin-mimetic activity of the complexes was determined to be: [VO(tcpp)]Na4 ≈ [VO(tpps)] > ([VO(tmpyp)](ClO4)4 > oxovanadium(IV) sulphate.

Oxytocin analogues with non-coded amino acid residues in position 8: [8-Neopentylglycine]oxytocin and [8-cycloleucine]oxytocin

1987 ◽  
Vol 52 (9) ◽  
pp. 2317-2325 ◽  
Author(s):  
Jan Hlaváček ◽  
Jan Pospíšek ◽  
Jiřina Slaninová ◽  
Walter Y. Chan ◽  
Victor J. Hruby
Keyword(s):  
Amino Acid ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
The Other ◽  
Amino Acid Residues ◽  
Phase Synthesis ◽  
Other Hand ◽  
Fragment Condensation

[8-Neopentylglycine]oxytocin (II) and [8-cycloleucine]oxytocin (III) were prepared by a combination of solid-phase synthesis and fragment condensation. Both analogues exhibited decreased uterotonic potency in vitro, each being about 15-30% that of oxytocin. Analogue II also displayed similarly decreased uterotonic potency in vivo and galactogogic potency. On the other hand, analogue III exhibited almost the same potency as oxytocin in the uterotonic assay in vivo and in the galactogogic assay.

scholarly journals In vitro and in vivo Evaluation of Ibuprofen Nanosuspensions for Enhanced Oral Bioavailability

2021 ◽  
Author(s):  
Mohsen Hedaya ◽  
Farzana Bandarkar ◽  
Aly Nada
Keyword(s):  
Particle Size ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
In Vivo Evaluation ◽  
Poorly Soluble ◽  
Extent Of Absorption ◽  
Better Than

Introduction: The objectives were to prepare, characterize and in vivo evaluate different ibuprofen (IBU) nanosuspensions prepared by ultra-homogenization, after oral administration to rabbits. Methods: The nanosuspensions produced by ultra-homogenization were tested and compared with a marketed IBU suspension for particle size, in vitro dissolution and in vivo absorption. Five groups of rabbits received orally 25 mg/kg of IBU nanosuspension, nanoparticles, unhomogenized suspension, marketed product and untreated suspension. A sixth group received 5 mg/kg IBU intravenously. Serial blood samples were obtained after IBU administration. Results: The formulated nanosuspensions showed significant decrease in particle size. Polyvinyl Pyrrolidone K30 (PP) was found to improve IBU aqueous solubility much better than the other tested polymers. Addition of Tween 80 (TW), in equal amount as PP (IBU: PP:TW, 1:2:2 w/w) resulted in much smaller particle size and better dissolution rate. The Cmax achieved were 14.8±1.64, 11.1±1.37, 9.01±0.761, 7.03±1.38 and 3.23±1.03 μg/ml and the tmax were 36±8.2, 39±8.2, 100±17.3, 112±15 and 105±17 min for the nanosuspension, nanoparticle, unhomogenized suspension, marketed IBU suspension and untreated IBU suspension in water, respectively. Bioavailability of the different formulations relative to the marketed suspension were the highest for nanosuspension> unhomogenized suspension> nanoparticles> untreated IBU suspension. Conclusion: IBU/PP/TW nanosuspensions showed enhanced in vitro dissolution as well as faster rate and higher extent of absorption as indicated from the higher Cmax, shorter tmax and larger AUC. The in vivo data supported the in vitro results. Nanosuspensions prepared by ultra-high-pressure-homogenization technique can be used as a good formulation strategy to enhance the rate and extent of absorption of poorly soluble drugs.

Nanostructured Ethosomal Gel Loaded with Arctostaphylos uva-ursi extract; In-vitro/In-vivo Evaluation as a Cosmeceutical Product

2021 ◽  
Vol 18 ◽  
Author(s):  
Nayla Javed ◽  
Shakeel Ijaz ◽  
Naveed Akhtar ◽  
Haji Muhammad Shoaib Khan
Keyword(s):  
Zeta Potential ◽  
Biological Activities ◽  
Skin Permeation ◽  
Radical Scavenging ◽  
Reducing Power ◽  
Potential Candidate ◽  
Skin Rejuvenation ◽  
In Vivo Evaluation

Background: Arctostaphylos uva-ursi (AUU) being rich in polyphenols and arbutin is known to have promising biological activities and can be a potential candidate as a cosmaceutical. Ethosomes encourage the formation of lamellar-shaped vesicles with improved solubility and entrapment of many drugs including plant extracts. Objective: The objective of this work was to develop an optimized nanostructured ethosomal gel formulation loaded with AUU extract and evaluated for skin rejuvenation and depigmentation. Methods: AUU extract was tested for phenolic and flavonoid content, radical scavenging potential, reducing power activity, and in-vitro SPF (sun protection factor) estimation. AUU loaded 12 formulations were prepared and characterized by SEM (scanning electron microscopy), vesicular size, zeta potential, and entrapment efficiency (%EE). The optimized formulation was subjected to non-invasive in-vivo investigations after incorporating it into the gel system and ensuring its stability and skin permeation. Results: Ethosomal vesicles were spherical in shape and Zeta size, zeta potential, PDI (polydispersity index), % EE and in-vitro skin permeation of optimized formulation (F3) were found to be 114.7nm, -18.9mV, 0.492, 97.51±0.023%, and 79.88±0.013% respectively. AUU loaded ethosomal gel formulation was stable physicochemically and exhibited non-Newtonian behavior rheologically. Moreover, it significantly reduced skin erythema, melanin as well as sebum level and improved skin hydration and elasticity. Conclusion: A stable AUU based ethosomal gel formulation could be a better vehicle for phytoextracts than conventional formulations for cosmeceutical applications such as for skin rejuvenation and depigmentation etc.

scholarly journals Biological activities of recombinant chicken leptin C4S analog compared with unmodified leptins

2000 ◽  
Vol 279 (1) ◽  
pp. E116-E123 ◽  
Author(s):  
S. Dridi ◽  
N. Raver ◽  
E. E. Gussakovsky ◽  
M. Derouet ◽  
M. Picard ◽  
...  
Keyword(s):  
Biological Activity ◽  
Food Intake ◽  
Leptin Receptor ◽  
Biological Activities ◽  
Wild Type ◽  
Escherichia Coli Cells ◽  
Prokaryotic Expression Vector ◽  
Long Form

The chicken leptin sequence, in contrast to mammalian leptins, contains an unpaired Cys at position 3 of the original cDNA ( AF012727 ). The presence of an extra Cys may confer a different structure and affect the leptin's biological activity. To address this, we studied the effects of wild-type and mutated (C4S) chicken leptins in vitro and in vivo and compared them with mammalian leptin prepared from ovine leptin cDNA. The prokaryotic expression vector pMON, encoding full-size A(−1) chicken leptin ( AF012727 ), was mutated using a mutagenesis kit, yielding the C4S analog. Escherichia coli cells transformed with this vector overexpressed large amounts of chicken leptin C4S upon induction with nalidixic acid. The expressed protein, found in the inclusion bodies, was refolded and purified to homogeneity on a Q-Sepharose column, yielding three electrophoretically pure fractions, eluted from the column by 100, 125, and 150 mM NaCl, respectively. All three fractions showed a single band of the expected molecular mass (16 kDa) and were composed of >95% monomeric protein. Proper refolding was evidenced by comparing the circular dichroism spectrum of the analog with spectra of nonmutated chicken and ovine leptins. The biological activity of the C4S analog was evidenced by its ability to stimulate proliferation of leptin-sensitive BAF/3 cells transfected with a long form of human leptin receptor construct similar to its nonmutated counterpart, indicating that Cys4 plays no role in leptin activity. The in vitro activity of both wild-type and mutated chicken leptins was ∼10-fold lower than that of ovine leptin. After intravenous or intraperitoneal injections, C4S analog and the nonmutated chicken and ovine leptins all lowered the food intake of starved 9-day-old broiler or 5-wk-old layer male chickens by 11–34%. Monitoring food behavior revealed that the attenuated food intake resulted not from a decreased number of approaches to the feeders but from a decrease in the average time spent eating during each approach.

scholarly journals Interplay between MPIase, YidC, and PMF during Sec-independent insertion of membrane proteins

2021 ◽  
Vol 5 (1) ◽  
pp. e202101162
Author(s):  
Yuta Endo ◽  
Yuko Shimizu ◽  
Hanako Nishikawa ◽  
Katsuhiro Sawasato ◽  
Ken-ichi Nishiyama
Keyword(s):  
Membrane Proteins ◽  
Molecular Basis ◽  
Terminal Region ◽  
Integral Membrane Proteins ◽  
The Other ◽  
Other Hand ◽  
Model Protein

Integral membrane proteins with the N-out topology are inserted into membranes usually in YidC- and PMF-dependent manners. The molecular basis of the various dependencies on insertion factors is not fully understood. A model protein, Pf3-Lep, is inserted independently of both YidC and PMF, whereas the V15D mutant requires both YidC and PMF in vivo. We analyzed the mechanisms that determine the insertion factor dependency in vitro. Glycolipid MPIase was required for insertion of both proteins because MPIase depletion caused a significant defect in insertion. On the other hand, YidC depletion and PMF dissipation had no effects on Pf3-Lep insertion, whereas V15D insertion was reduced. We reconstituted (proteo)liposomes containing MPIase, YidC, and/or F0F1-ATPase. MPIase was essential for insertion of both proteins. YidC and PMF stimulated Pf3-Lep insertion as the synthesis level increased. V15D insertion was stimulated by both YidC and PMF irrespective of the synthesis level. These results indicate that charges in the N-terminal region and the synthesis level are the determinants of YidC and PMF dependencies with the interplay between MPIase, YidC, and PMF.

scholarly journals In vitro Multiplication of Iraca palm (Carludovica palmata Ruíz & Pavón)

2020 ◽  
Vol 73 (1) ◽  
pp. 9039-9046
Author(s):  
Rodrigo Alberto Hoyos Sanchez ◽  
Diego Chicaíza Finley ◽  
Juan Carlos Zambrano Arteaga
Keyword(s):  
Root Formation ◽  
The Other ◽  
Naphthaleneacetic Acid ◽  
Multiplication Rate ◽  
In Vitro Multiplication ◽  
Commercial Interest ◽  
Other Hand ◽  
Number Of Shoots

Carludovica palmata Ruíz & Pavón is a plant that belongs to the Cyclanthaceae family. Its commercial interest is related to the production of fibers for the manufacture of handicrafts, mainly the Panama hat, so it is important to study its propagation. This investigation aimed to determine the effect of 6-benzylaminopurine (BAP) in the formation of new shoots and 1-naphthaleneacetic acid (NAA) in the formation of roots, as well as the adaptation in greenhouse conditions of Carludovica palmata Ruíz & Pavón. In order to find the optimal multiplication rate, 0.5 cm length explants were planted in glass jars with 15 mL of semisolid MS with different concentrations of BAP and cultured under in vitro conditions for 90 days. The multiplication parameters in this stage were number of shoots per explant (NSE), length of shoots (LS), and length of roots (LR) as multiplication parameters. In a similar procedure, the number of roots per explant (NRE), length of roots (LR), and length of plantlets (LP) was determined using different concentrations of NAA. Finally, different substrates were evaluated for the adaptation of plantlets of C. palmata produced in vitro, under greenhouse conditions for 80 days. The highest multiplication rate (17±3 shoots per explant) was obtained with 2.0 mg L-1 of BAP. Root formation occurred efficiently in all treatments, without significant statistical differences between them. On the other hand, the use of substrate soil-t15 was the best treatment for the growth of C. palmata under greenhouse conditions. From the results obtained, it is concluded that C. palmata can be efficiently multiplied under in vitro conditions and did not present problems during the in vivo rooting process.

CORTICOID PRODUCTION IN VITRO AS A TEST OF ADRENOCORTICAL FUNCTION IN RATS

1960 ◽  
Vol XXXIII (I) ◽  
pp. 59-66 ◽  
Author(s):  
J. van der Vies
Keyword(s):  
Adrenal Cortex ◽  
Adrenal Function ◽  
The Other ◽  
Adrenocortical Function ◽  
Experimental Conditions ◽  
Adrenal System ◽  
Other Hand ◽  
Stimulation Of

ABSTRACT Adrenal function in rats under various experimental conditions was studied by incubating the adrenals in vitro and determining the corticosteroid output during one hour. This in vitro corticoid production was reduced after hypophysectomy, hypothalamus-lesioning and treatment with hydrocortisone or with Nembutal and morphine. On the other hand, an increased production was observed following stimulation of the pituitary-adrenal system by exogenous histamine or corticotrophin. From these experiments it is concluded that the corticoid production in vitro reflects the activity of the adrenal cortex in vivo and hence can be used for the study of the latter function.

Persisting mild hypothermia suppresses hypoxia-inducible factor-1α protein synthesis and hypoxia-inducible factor-1-mediated gene expression

2010 ◽  
Vol 298 (3) ◽  
pp. R661-R671 ◽  
Author(s):  
Tomoharu Tanaka ◽  
Takuhiko Wakamatsu ◽  
Hiroki Daijo ◽  
Seiko Oda ◽  
Shinichi Kai ◽  
...  
Keyword(s):  
Gene Expression ◽  
Low Temperature ◽  
Hypoxia Inducible Factor ◽  
The Body ◽  
The Other ◽  
Adaptation To Hypoxia ◽  
Hypoxia Inducible Factor 1 ◽  
Other Hand

The transcription factor hypoxia-inducible factor-1 (HIF-1) plays an essential role in regulating gene expression in response to hypoxia-ischemia. Ischemia causes the tissue not only to be hypoxic but also to be hypothermic because of the hypoperfusion under certain circumstances. On the other hand, the induced hypothermia is one of the most common therapeutic modalities to extend tolerance to hypoxia. Although hypoxia elicits a variety of cellular and systemic responses at different organizational levels in the body, little is known about how hypoxia-induced responses are affected by low temperature. We examined the influence of mild hypothermic conditions (28–32°C) on HIF-1 in both in vitro and in vivo settings. In vitro experiments adopting cultured cells elucidated that hypoxia-induced HIF-1 activation was resistant to 4-h exposure to the low temperature. In contrast, exposure to the low temperature as long as 24 h suppressed HIF-1 activation and the subsequent upregulation of HIF-1 target genes such as VEGF or GLUT-1. HIF-1α protein stability in the cell was not affected by hypothermic treatment. Furthermore, intracellular ATP content was reduced under 1% O2 conditions but was not largely affected by hypothermic treatment. The evidence indicates that reduction of oxygen consumption is not largely involved in suppression of HIF-1. In addition, we demonstrated that HIF-1 DNA-binding activity and HIF-1-dependent gene expressions induced under 10% O2 atmosphere in mouse brain were not influenced by treatment under 3-h hypothermic temperature but were inhibited under 5-h treatment. On the other hand, we indicated that warming ischemic legs of mice for 24 h preserved HIF-1 activity. In this report we describe for the first time that persisting low temperature significantly reduced HIF-1α neosynthesis under hypoxic conditions, leading to a decrease in gene expression for adaptation to hypoxia in both in vitro and in vivo settings.

MODEL STUDIES IN VITRO WITH LONG-ACTING HORMONAL PREPARATIONS

1970 ◽  
Vol 64 (4) ◽  
pp. 656-669 ◽  
Author(s):  
J. van der Vies
Keyword(s):  
Biological Activity ◽  
Active Component ◽  
Biological Activities ◽  
Pharmacological Properties ◽  
Model Studies ◽  
Rate Of Absorption ◽  
Long Acting ◽  
Hydrolysis Of

ABSTRACT Since the biological activities of long-acting hormonal preparations, containing steroids or esters of steroids dissolved in arachis oil, depend very much on the rate of absorption from the intramuscular depot, an in vitro model for the latter has been developed. In this model the solution of the drug in oil is applied to a strip of filter paper and the spot eluted with a stream of hog plasma. Using this model, results were obtained which correlated with the observed rates of resorption in vivo. This demonstrates that the physical process underlying parenteral resorption depends on the distribution of the steroid between oil and plasma. As far as these esters of steroids are concerned, the steroid moiety of which is the ultimate active component, the hydrolysis of the ester by the esterase of the transporting plasma is another important factor. This has been studied in an in vitro system. The results obtained with both models proved valuable in understanding the pharmacological properties of a number of anabolic, androgenic and progestational steroids and steroid esters and also in explaining the differences in biological activity between closely related preparations.

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