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.

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 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 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.

Solid phase synthesis and biological activities of oxytocin carba analogues containing threonine in position 4

1985 ◽  
Vol 50 (2) ◽  
pp. 418-427 ◽  
Author(s):  
Michal Lebl ◽  
Victor J. Hruby ◽  
Jiřina Slaninová ◽  
Tomislav Barth
Keyword(s):  
Biological Activity ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Biological Activities ◽  
High Biological Activity ◽  
Phase Synthesis

Solis phase methodology was developed for the synthesis of carba-analogues of oxytocin. Two known compounds (deamino-1-carba-oxytocin (I) and deamino-6-carba-oxytocin (II)) and two new analogues ([4-threonine]deamino-1-carba-oxytocin (III) and [4-threonine]deamino-6-carba-oxytocin (IV)) were synthesized using different approaches. The latter two compounds were found to possess high biological activity in the rat uterotonic (in vitro and in vivo) and galactogogic (in vivo) assays.

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.

scholarly journals Biological Effects of Propolis on Cancer

2020 ◽  
Vol 8 (3) ◽  
pp. 573
Author(s):  
Hamide Doğan ◽  
Sibel Silici ◽  
Ahmet Ata Ozcimen
Keyword(s):  
Biological Activity ◽  
Side Effects ◽  
Biological Effects ◽  
Chemotherapeutic Agents ◽  
New Drugs ◽  
In Vivo Studies ◽  
Pharmacological Properties ◽  
Bee Colony

Propolis is a special resin and wax material collected from the leaves and shells of trees, buds and shoots of plants by honey bees (Apis mellifera L.). In recent years, many researchers have studied the chemical composition, biological activity and pharmacological properties of propolis. The colour, odour and pharmacological properties of the propolis composition also vary as the composition changes depending on the plant, region, season and bee colony. Flavonoids, aromatic acids, phenolic acids and esters are the main compounds responsible for the biological activity of propolis. A number of studies have been conducted on the use of propolis or its active ingredients in the treatment of cancer. It has been observed that the use of propolis did not cause side effects according to in-vitro and in-vivo studies. Propolis should be extracted with different compounds for use in biological assays. The most commonly used compounds for extraction are ethanol, methanol, oil and water. A number of studies have been carried out showing the antitumor effect of propolis in cell culture and animal tests. The search for new drugs derived from natural products, which may function as chemotherapeutic agents and have low side effects, has increased in recent years. Combination with antioxidant therapy may improve the side effects of chemotherapy on leukocytes, liver and kidney, thus increasing the effect of chemotherapy with dose increase.

scholarly journals Recombinant Peptide Production Platform Coupled with Site-Specific Albumin Conjugation Enables a Convenient Production of Long-Acting Therapeutic Peptide

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 364 ◽  
Author(s):  
Mijeong Bak ◽  
Junyong Park ◽  
Kiyoon Min ◽  
Jinhwan Cho ◽  
Jihyoun Seong ◽  
...  
Keyword(s):  
Half Life ◽  
Solid Phase ◽  
Biological Activities ◽  
Recombinant Peptide ◽  
Site Specific ◽  
Therapeutic Peptide ◽  
Therapeutic Peptides ◽  
Long Acting

The number of therapeutic peptides for human treatment is growing rapidly. However, their development faces two major issues: the poor yield of large peptides from conventional solid-phase synthesis, and the intrinsically short serum half-life of peptides. To address these issues, we investigated a platform for the production of a recombinant therapeutic peptide with an extended serum half-life involving the site-specific conjugation of human serum albumin (HSA). HSA has an exceptionally long serum half-life and can be used to extend the serum half-lives of therapeutic proteins and peptides. We used glucagon-like-peptide 1 (GLP-1) as a model peptide in the present study. A “clickable” non-natural amino acid—p-azido-l-phenylalanine (AzF)—was incorporated into three specific sites (V16, Y19, and F28) of a GLP-1 variant, followed by conjugation with HSA through strain-promoted azide–alkyne cycloaddition. All three HSA-conjugated GLP-1 variants (GLP1_16HSA, GLP1_19HSA, and GLP1_28HSA) exhibited comparable serum half-lives in vivo. However, the three GLP1_HSA variants had different in vitro biological activities and in vivo glucose-lowering effects, demonstrating the importance of site-specific HSA conjugation. The platform described herein could be used to develop other therapeutic peptides with extended serum half-lives.

scholarly journals The pharmacological potentials of Musa paradisiaca Linn.

2021 ◽  
Vol 8 (4) ◽  
Author(s):  
Ridwan Adesola
Keyword(s):  
Traditional Medicine ◽  
Biological Activities ◽  
Scientific Information ◽  
Model Studies ◽  
Musa Paradisiaca ◽  
In Vivo Animal Model ◽  
Review Reports ◽  
Musa Species

Musa paradisiaca Linn. (Plantain or cooking banana) is among the major crops that are being cultivated by farmers and serve as the main food crop for both animals and humans in some parts of the world. It shows several beneficial properties. In traditional medicine, the fruits in addition to the other parts of the plant such as the stalk, peel, pulp and leaf are used to treat different diseases in humans. This review presents the scientific information on the pharmacological potentials, possible nutritional values and phytochemicals of this Musa species. It is a source of carbohydrate that can easily be digestible and also provides vital vitamins like vitamin B complex, vitamin C and a lot of minerals like potassium (K), calcium (Ca) and magnesium (Mg) etc. Most of the in vitro studies, in vivo (animal model) studies and clinical trials, propose that innumerable banana and plantain parts have been utilized in traditional medicine for the treatment of countless non-communicable diseases like diabetes, cancer, hypertension, atherosclerosis, ulcers, urolithiasis and Alzheimer’s infection. Also, this review reports the phytocompounds isolated through the use of different solvents for extraction of the plant’s parts. A comprehensive assessment of the biological activities of different extracts is included and possible mechanisms and phytochemicals involved have been correlated.

BIOLOGICAL ACTIVITY OF SYNTHETIC HUMAN CORTICOTROPHIN WITH REVISED AMINO ACID SEQUENCE

1974 ◽  
Vol 75 (1) ◽  
pp. 24-32 ◽  
Author(s):  
Lotte Schenkel-Hulliger ◽  
René Maier ◽  
Pierre L. Barthe ◽  
Pierre A. Desaulles ◽  
Andrée Jarret ◽  
...  
Keyword(s):  
Biological Activity ◽  
Amino Acid ◽  
Amino Acid Sequence ◽  
Lipolytic Activity ◽  
Biological Activities ◽  
Test Systems

ABSTRACT The corticotrophic, melanotrophic and lipolytic activity of synthetic human corticotrophin of revised structure has been evaluated and compared with that of synthetic porcine ACTH (uncorrected structure). The amino acid sequence of the two peptides differs at 3 sites in the 25 to 31 region. The two peptides exihibit identical biological activities in in vitro and in vivo test systems in the rat.

scholarly journals Ebselen and Analogues: Pharmacological Properties and Synthetic Strategies for Their Preparation

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4230
Author(s):  
Claudio Santi ◽  
Cecilia Scimmi ◽  
Luca Sancineto
Keyword(s):  
Clinical Trials ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Review Article ◽  
Pharmacological Properties ◽  
Specific Topic ◽  
The Subject ◽  
Synthetic Approaches

Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities. It was the subject of several clinical trials and it is currently in clinical evaluation for the treatment of COVID-19 patients. Given our interest in the synthesis and pharmacological evaluation of selenorganic derivatives with this review, we aimed to collect all the papers focused on the biological evaluation of ebselen and its close analogues, covering the timeline between 2016 and most of 2021. Our analysis evidences that, even if it lacks specificity when tested in vitro, being able to bind to every reactive cysteine, it proved to be always well tolerated in vivo, exerting no sign of toxicity whatever the administered doses. Besides, looking at the literature, we realized that no review article dealing with the synthetic approaches for the construction of the benzo[d][1,2]-selenazol-3(2H)-one scaffold is available; thus, a section of the present review article is completely devoted to this specific topic.

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