Immobilized Biomolecules and Synthetic Derivatives of Biomolecules

2014 ◽  
pp. 547-676
Keyword(s):  
Synthetic Derivatives ◽  
Derivatives Of

Synthetic derivatives of pulchrol: An antiparasitic natural product

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
P Terrazas ◽  
O Sterner
Keyword(s):  
Natural Product ◽  
Synthetic Derivatives ◽  
Derivatives Of

Synthesis, Cytotoxicity and Antioxidant Activity of New Analogs of RC-121 Synthetic Derivatives of Somatostatin

2019 ◽  
Vol 18 (10) ◽  
pp. 1417-1424 ◽  
Author(s):  
Emilia Naydenova ◽  
Diana Wesselinova ◽  
Svetlana Staykova ◽  
Ivan Goshev ◽  
Ljubomir Vezenkov
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Capacity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Colorectal Cancer Cell Line ◽  
Cervical Cancer Cell Line ◽  
Synthetic Derivatives ◽  
Derivatives Of

Background: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity. Objectives: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine). Methods: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (Human Colorectal Cancer Cell Line), MDA-MB-23 (Human Breast Cancer Cell Line), Hep G-2 (Human Hepatocellular Carcinoma Cell Line) and HeLa (cervical cancer cell line). The antioxidant capacities were tested by ORAC (Oxygen Radical Antioxidant Capacity) and HORAC (Hydroxyl Radical Averting Capacity) methods. Results: All substances expressed significantly higher antioxidant capacity by comparison with galic acid and Trolox. All substances showed considerable antioxidant capacity as well. Compound 2T (D-Phe-c(Cys-Tyr-DTrp- Dap-Tle-Cys)-Thr-NH2)had the highest antioxidant effect. The compound 4T (D-Phe-c(Cys-Tyr-D-Trp- Orn-Tle-Cys)-Thr-NH2) displayed antiproliferative effect on HeLa cells with IC50 30 µM. The peptide analog 3T (D-Phe-c(Cys-Tyr-D-Trp-Lys-Tle-Cys)-Thr-NH2) exerted the most pronounced inhibition on the cell vitality up to 53%, 56% and 65% resp. against MDA-MB-23, Hep G-2, HeLa in the higher tested concentration. Conclusion: The somatostatin analogs showed moderate influence on the vitality of different tumor cells and could be used in changing their pathology.

Semi-synthetic Derivatives of Heliomycin with an Antiproliferative Potency

2018 ◽  
Vol 13 ◽  
Author(s):  
A. E. Shchekotikhin ◽  
Georgy Y. Nadysev ◽  
Alexander S. Tikhomirov ◽  
Lyubov G. Dezhenkova
Keyword(s):  
Synthetic Derivatives ◽  
Derivatives Of

scholarly journals Synthetic Derivatives of Natural Alkaloid Harmine

2016 ◽  
Vol 11 (3) ◽  
pp. 199
Author(s):  
N.M. Ismagulova ◽  
Zh.S. Nurmaganbetov ◽  
A.Zh. Turmukhambetov ◽  
T.S. Seitembetov ◽  
S.M. Adekenov
Keyword(s):  
Indole Alkaloid ◽  
Quaternary Ammonium Salts ◽  
Ammonium Salts ◽  
Peganum Harmala ◽  
Underground Part ◽  
X Ray ◽  
Natural Alkaloid ◽  
First Time ◽  
Synthetic Derivatives ◽  
Derivatives Of

The indole alkaloid harmine was extracted from underground part of <em>Peganum harmala L.</em> With the purpose of obtaining the new biological active derivatives on base of alkaloid harmine the chemical modification was carried out. The p-toluolsulfochlorid, p-toluolsulfoacid, hydrochloric, sulfuric, nitric acids, dioxide selenium and phthalic anhydride have been chosen as modifiers. For the first time quaternary ammonium salts, derivatives of N-oxide and N (2)-oxyharminiumphthalate harmine are synthesized. The structure of the synthesized compounds is determined by methods of the spectral analysis and X-ray analysis. Antimicrobic and phagocytosis stimulating activities of isolated alkaloids and their derivatives are investigated.

Therapeutic Journey of Andrographis paniculata (Burm.f.) Nees from Natural to Synthetic and Nanoformulations

2021 ◽  
Vol 21 ◽  
Author(s):  
Sharuti Mehta ◽  
Anil Kumar Sharma ◽  
Rajesh K. Singh
Keyword(s):  
Biological Activities ◽  
Andrographis Paniculata ◽  
Herbaceous Plant ◽  
Target Tissue ◽  
Active Components ◽  
Essential Information ◽  
Compound Plant ◽  
Therapeutic Activities ◽  
Synthetic Derivatives ◽  
Derivatives Of

: Andrographis paniculata (Burm.f.) Nees (Acanthaceae) is a herbaceous plant and commonly called 'King of Bitters'. It has gained attraction as a potential hepatoprotective agent and a natural molecule with various biological activities viz. anticancer, immunomodulatory, anti-inflammatory, antibacterial, neuroprotective, and so on. The andrographolide is one of the main diterpenoids responsible for the drug's bitter taste and various therapeutic activities. The poor cellular permeability, solubility and short biological half-life of its pure components limit its distribution to the target tissue. To conquer this obstacle, various researchers worldwide have been working on designing the synthetic derivatives of its active components and nanoformulations to improve the drug's efficiency and selectivity to develop more active leads for biomedical applications. This article discussed the recent research on synthetic derivatives, including their possible therapeutic applications and structure-activity relationship (SAR). Additionally, this article also presents the essential information concerning the various nanoformulations developed to increase the delivery of pure compound/plant extract to the target site, thereby improving the drug's efficacy for multiple ailments.

scholarly journals Current Research on the Safety of Pyrethroids Used as Insecticides

Medicina ◽  
2018 ◽  
Vol 54 (4) ◽  
pp. 61 ◽  
Author(s):  
Agnieszka Chrustek ◽  
Iga Hołyńska-Iwan ◽  
Inga Dziembowska ◽  
Joanna Bogusiewicz ◽  
Marcin Wróblewski ◽  
...  
Keyword(s):  
Sodium Channels ◽  
Hepatic Metabolism ◽  
The Body ◽  
Lower Body ◽  
Lipid Levels ◽  
Skin Contact ◽  
Comprehensive Information ◽  
Synthetic Derivatives ◽  
Derivatives Of ◽  
Absorption Level

Pyrethroids are synthetic derivatives of natural pyrethrins extracted from Chrysanthemum cinerariaefolium. They are 2250 times more toxic to insects than to vertebrates due to insects’ smaller size, lower body temperature and more sensitive sodium channels. In particular, three pyrethroid compounds, namely deltamethrin, permethrin, and alpha-cypermethrin, are commonly used as insecticides and are recommended for in-home insect control because they are considered to be relatively non-toxic to humans in all stages of life. However, recent data show that they are not completely harmless to human health as they may enter the body through skin contact, by inhalation and food or water, and absorption level depending on the type of food. Permethrin seems to have an adverse effect on fertility, the immune system, cardiovascular and hepatic metabolism as well as enzymatic activity. Deltamethrin induces inflammation, nephro- and hepatotoxicity and influences the activity of antioxidant enzymes in tissues. Alpha-cypermethrin may impair immunity and act to increase glucose and lipid levels in blood. The aim of the review is to provide comprehensive information on potential hazards associated to human exposure to deltamethrin, permethrin and alpha-cypermethrin. The results of presented studies prove that the insecticides must be used with great caution.

Inhibitory Effect of Retinoic Acid on Proliferation, Maturation and Tryptase Level in Human Leukemic Mast Cells (HMC-1)

2003 ◽  
Vol 16 (1) ◽  
pp. 43-47 ◽  
Author(s):  
M.G. Alexandrakis ◽  
D.S. Kyriakou ◽  
D. Seretakis ◽  
W. Boucher ◽  
R. Letourneau ◽  
...  
Keyword(s):  
Mast Cell ◽  
Retinoic Acid ◽  
Mast Cells ◽  
Allergic Inflammation ◽  
Inhibitory Effect ◽  
Control Group ◽  
Tryptase Level ◽  
Synthetic Derivatives ◽  
Derivatives Of ◽  
Inhibit Cell Proliferation

Mast cells play an important role in allergic inflammation by releasing histamine, tryptase and several inflammatory cytokines. Human leukemic mast cells (HMC-1) have been used to study mast cell mediators and their role in inflammatory mechanisms. HMC-1 contain and release several inflammatory mediators, of which the proteolytic enzyme tryptase is most characteristic. Retinoids, including retinoic acid, are naturally occurring and synthetic derivatives of vitamin A. All-trans-retinoic (ATRA) acid had been previously reported to inhibit cell proliferation, differentiation and apoptosis. In the present study, we investigated the effect of ATRA on the proliferation and secretion of tryptase in HMC-1. HMC-1 were treated with ATRA at 10-4M, 10-5M or 10-6M for 3,4 or 5 days in culture. Control HMC-1 were treated with equal amount of culture medium only. ATRA decreased the number of HMC-1 as compared to the control group. The same treatment for 3, 4 or 5 days also decreased intracellular tryptase levels. These results indicate that ATRA significantly inhibits both proliferation and growth as shown by the decreased intracellular tryptase levels in HMC-1. ATRA may be a useful agent in the treatment of mast cell proliferative disorders.

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