Evaluation of cholinesterase inhibitory activity and cytotoxicity of synthetic derivatives of di- and triterpene metabolites from Pinus silvestris and Dipterocarpus alatus resins

A variety of new and earlier synthesized lupane, oleanane, ursane and dammarane triterpenoids have been investigated for their inhibitory activity against α-glucosidase. 2,3-Indole-21β-acetyl-20β,28-epoxy-18α,19βH-ursane and 3-oxo-3A-homo-3a-aza-20( S)-hydroxydammar-24(25)-ene were synthesized for the first time. The compounds 3, 4, 8–11 and 14 demonstrated strong in vitro inhibitory activity towards α-glucosidase with IC50 values of 37.5–115.1 μM. 3-Deoxy-3a-homo-3a-aza-28-cinnamoyloxy-20(29)-lupene, with an IC50 of 6.67 μM was 60-fold more active than the market drug acarbose.

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Synthetic derivatives of pulchrol: An antiparasitic natural product

Planta Medica ◽

10.1055/s-0036-1596772 ◽

2016 ◽

Vol 81 (S 01) ◽

pp. S1-S381

Author(s):

P Terrazas ◽

O Sterner

Keyword(s):

Natural Product ◽

Synthetic Derivatives ◽

Derivatives Of

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Synthesis, Biological Evaluation and the Rationalisation of the Inhibitory Activity of a Range of Sulfonate Derivatives of Estrone (E1) in the Design of Reversible Inhibitors of Estrone Sulfatase (ES)

Letters in Drug Design & Discovery ◽

10.2174/1570180811666140226235116 ◽

2014 ◽

Vol 11 (8) ◽

pp. 985-992 ◽

Cited By ~ 1

Author(s):

Mohsen Akbarzadeh ◽

Timothy Cartledge ◽

Sabbir Ahmed

Keyword(s):

Inhibitory Activity ◽

Biological Evaluation ◽

Reversible Inhibitors ◽

Estrone Sulfatase ◽

Derivatives Of

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

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520618666180417164344 ◽

2019 ◽

Vol 18 (10) ◽

pp. 1417-1424 ◽

Cited By ~ 2

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.

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