Synthetic derivatives of pulchrol: An antiparasitic natural product

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.

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Semi-synthetic Derivatives of Heliomycin with an Antiproliferative Potency

Recent Patents on Anti-Cancer Drug Discovery ◽

10.2174/1574892813666180723150542 ◽

2018 ◽

Vol 13 ◽

Cited By ~ 1

Author(s):

A. E. Shchekotikhin ◽

Georgy Y. Nadysev ◽

Alexander S. Tikhomirov ◽

Lyubov G. Dezhenkova

Keyword(s):

Synthetic Derivatives ◽

Derivatives Of

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Semisynthesis and acaricidal activities of isoxazole and pyrazole derivatives of a natural product bisdemethoxycurcumin

Journal of Pesticide Science ◽

10.1584/jpestics.d13-027 ◽

2013 ◽

Vol 38 (4) ◽

pp. 214-219 ◽

Cited By ~ 6

Author(s):

Jinxiang Luo ◽

Wei Ding ◽

Yongqiang Zhang ◽

Zhenguo Yang ◽

Yang Li ◽

...

Keyword(s):

Natural Product ◽

Pyrazole Derivatives ◽

Derivatives Of

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Immobilized Biomolecules and Synthetic Derivatives of Biomolecules

Polymer Biomaterials in Solution, as Interfaces and as Solids ◽

10.1201/b12021-14 ◽

2014 ◽

pp. 547-676

Keyword(s):

Synthetic Derivatives ◽

Derivatives Of

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Synthetic Derivatives of Natural Alkaloid Harmine

Eurasian Chemico-Technological Journal ◽

10.18321/ectj281 ◽

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.

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

Mini-Reviews in Medicinal Chemistry ◽

10.2174/1389557521666210315162354 ◽

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.

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