Drug-peptide supramolecular hydrogel boosting transcorneal permeability and pharmacological activity via ligand-receptor interaction

SummarySynthetic peptides (TRAP or Thrombin Receptor Activating Peptide) corresponding to at least the first five aminoacids of the new N-terminal tail generated after thrombin proteolysis of its receptor are effective to mimic thrombin. We have studied two different TRAPs (SFLLR, and SFLLRN) in their effectiveness to induce the different platelet responses in comparison with thrombin. Using Indo-1/AM- labelled platelets, the maximum rise in cytoplasmic ionized calcium was lower with TRAPs than with thrombin. At threshold concentrations allowing maximal aggregation (50 μM SFLLR, 5 μM SFLLRN and 1 nM thrombin) the TRAPs-induced release reaction was about the same level as with thrombin, except when external calcium was removed by addition of 1 mM EDTA. In these conditions, the dense granule release induced by TRAPs was reduced by over 60%, that of lysosome release by 75%, compared to only 15% of reduction in the presence of thrombin. Thus calcium influx was more important for TRAPs-induced release than for thrombin-induced release. At strong concentrations giving maximal aggregation and release in the absence of secondary mediators (by pretreatment with ADP scavengers plus aspirin), SFLLRN mobilized less calcium, with a fast return towards the basal level and induced smaller lysosome release than did thrombin. The results further demonstrate the essential role of external calcium in triggering sustained and full platelet responses, and emphasize the major difference between TRAP and thrombin in mobilizing [Ca2+]j. Thus, apart from the proteolysis of the seven transmembrane receptor, another thrombin binding site or thrombin receptor interaction is required to obtain full and complete responses.

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Study of The Pharmacological Activity and Heavy Metal Content of Eichhornia Crassipes Extract

ICONIET PROCEEDING ◽

10.33555/iconiet.v2i2.17 ◽

2019 ◽

Vol 2 (2) ◽

pp. 91-95 ◽

Cited By ~ 1

Author(s):

Jimmy Jimmy ◽

Diah Indriani Widiputri ◽

Paulus Gunawan

Keyword(s):

Heavy Metal ◽

Pharmacological Activity ◽

Water Hyacinth ◽

Metal Content ◽

Eichhornia Crassipes ◽

High Light Intensity ◽

Milling Process ◽

Heavy Metal Content ◽

Solvent Ratio ◽

Negative Impacts

Eichhornia crassipes is well-known as water hyacinth. Water hyacinth grows rapidly in the nutrient-rich water and high light intensity places. The uncontrollable growth of water hyacinth has caused many negative impacts to the environment. For instance, interrupted water transport and decreased population of aquatic lives. The capacity of utilising water hyacinth is slower than water hyacinth growth and water hyacinth is still considered as a threat to theecosystem. This work was focused on the study of the pharmacological activity and heavy metal content of water hyacinth in Lake Cipondoh, Tangerang. Fresh water hyacinth was pre-treated through oven-drying and milling process. After that, each part of the plant was macerated by using multiple extraction method with 96% ethanol/water and three variations of sample-to-solvent ratios (1:30, 1:50, and 1:75 w/v). The result of the experiment showed thatwater hyacinth leaves produced an extract with lowest IC 50 (55.76 ± 6.73 ppm) compared toother parts. The most optimum solvent used to achieve this result was 96% ethanol/water (1:1 v/v). In order to obtain the lowest antioxidant activity, the sample to solvent ratio used was 1:50 and the heavy metal in the extract was very low. With this result, it was concluded that there is a promising opportunity to apply the water hyacinth growing in Lake Cipondoh, Tangerang as herbal medicine ingredient. Through this utilization, the overall number of water hyacinth in Indonesia can be reduced or at the least be controlled, so that the environmental problem caused by this plant can be minimized.

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Monoamine transporter and receptor interaction profiles of novel phenethylamine derivatives

10.26226/morressier.5785edc5d462b80296c9921e ◽

2016 ◽

Author(s):

Dino Luethi

Keyword(s):

Receptor Interaction ◽

Monoamine Transporter

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Pharmacognostical and pharmacological activity of Justicia gendarussa burm.f.: a comprehensive review

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11i3.2475 ◽

2020 ◽

Vol 11 (3) ◽

pp. 3384-3390

Author(s):

Ashish ◽

Anjali ◽

Dixit Praveen K ◽

Nagarajan K ◽

Sahoo Jagannath

Keyword(s):

Pharmacological Activity ◽

Chemical Constituents ◽

Biological Action ◽

Andaman Islands ◽

Comprehensive Review ◽

Medicinal Value ◽

Anti Oxidant ◽

Phytochemical Constituents ◽

Pharmacologically Active ◽

Different Parts

Justicia gendarussa Burm .f. (family Acanthaceae) which is also known as willow-leaves and commonly known as Nili-Nirgundi, it is very commonly found nearby to China and its availability is very common in larger parts of India and Andaman islands. Traditionally it is used to treat various sorts of disorders such as wound healing, anti-inflammatory, anti-oxidant, antiproliferative, anti-arthritic etc. Justicia gendarussa is one of the crucial herbs which has been used in the Ayurveda. Majorly leaves parts of the plant shows the pharmacological activity but the root of the plant Justicia gendarussa is also have the important medicinal values. A large variety of pharmacologically active constituents i.e., alkaloids, flavonoids, saponin, carbohydrates, steroids, triterpenoids, carotenoids, aminoacids, tannins, phenolics, coumarines and anthaquinones are also present in this plant and they makes the plant pharmacologically important. The activity of the plant is also dependent on the solvent which is used for the extraction the various vital chemical constituents. The different- different parts of the plants having the different medicinal values also differ in the chemical values. This review is not only focused on the essential phytochemical constituents which is available in the plant but it also explains their necessary medicinal value to shows the essential biological action and phytopharmacological actions of various parts of the plant.

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An ayurvedic tablet formulation for ulcer protection

International Research Journal of Pharmaceutical and Applied Sciences ◽

10.26452/irjpas.v10i4.1374 ◽

2020 ◽

Vol 10 (4) ◽

pp. 35-38

Author(s):

Shiva Kumar K ◽

Purushothaman M ◽

Soujanya H ◽

Jagadeeshwari S

Keyword(s):

Pharmacological Activity ◽

The Body ◽

Gastric Ulcers ◽

Antiulcer Activity ◽

Herbal Drugs ◽

Human Beings ◽

Synthetic Drugs ◽

Scientific Investigations ◽

System A ◽

The World

Gastric ulcers or the peptic ulcer is the primary disease that affects the gastrointestinal system. A large extent of the population in the world are suffering from the disease, and the age group of people those who suffer from ulcers are 20-55years. Herbs are known to the human beings that are useful in the treatment of diseases, and there are a lot of scientific investigations that prove the pharmacological activity of herbal drugs. Practitioners have been using the herbal material to treat the ulcers successfully, and the same had been reported scientifically. Numerous publications have been made that proves the antiulcer activity of the plants around the world. The tablets were investigated for the antiulcer activity in two doses 200 and 400mg/kg in albino Wistar rats in the artificial ulcer those are induced by the ethanol. The prepared tablets showed a better activity compared to the standard synthetic drug and the marketed ayurvedic formulation. The tablets showed a dose-dependent activity in ulcer prevention and treatment. Many synthetic drugs are available for the ulcer treatment, and the drugs pose the other problems in the body by showing the side effects and some other reactions. This limits the use of synthetic drugs to treat ulcers effectively. Herbs are known to the human beings that are useful in the treatment of diseases, and there are a lot of scientific investigations that prove the pharmacological activity of herbal drugs.

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Faculty Opinions recommendation of The GAAA tetraloop-receptor interaction contributes differentially to folding thermodynamics and kinetics for the P4-P6 RNA domain.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1009837.136558 ◽

2002 ◽

Author(s):

Samuel Butcher

Keyword(s):

Receptor Interaction ◽

Thermodynamics And Kinetics ◽

Folding Thermodynamics

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