Article by Disease | Synthesis, Cytotoxicity and Antioxidant Activity of New Analogs of RC-121 Synthetic Derivatives of Somatostatin

Bentham Oncology Collection| Oncology | Cervical Cancer

 

 

 

Abstract:

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.

 

Read out more at: http://www.eurekaselect.com/node/161359/article

EDITOR’S CHOICE – Vigna unguiculata Trypsin Inhibitor – Current Enzyme Inhibition

Journal: Current Enzyme Inhibition

Author(s): Romana Parveen, Tooba Naz Shamsi, Sumbul Afreen, Mudsser Azam, Tasneem Fatma, Qazi Mohd. Rizwanul Haque, Sadaf Fatima*

Graphical Abstract:

 

Abstract:

Background: Trypsin Inhibitors are one of the most promising and investigated subject for their role in pharmacognostical and pharmacological studies.

Aim: The paper describes purification and characterization of trypsin inhibitor obtained from blackeyed cowpea (Vigna unguiculata).

Methods: The purification procedure of Vigna unguiculata trypsin inhibitor (VUTI) includes homogenization followed by ammonium sulphate precipitation. The protein thus precipitated was further dialysed and purified by ion exchange chromatography and gel permeation chromatography. The molecular weight was determined by SDS-PAGE. The protein thus purified was characterized biochemically to demonstrate curative potential as strong antioxidant, anti-inflammatory and antimicrobial agent.

Results: The 15 kDa VUTI obtained showed IC50 values 490 µg/ml compared to standard which was 254µg/ml in 1, 1-diphenyl-2-picrylhydrazyl (DPPH) assay. Also, the highest ferric reducing antioxidant power (FRAP) results confirmed the highest FRAP value of 0.405 mM at 1000 µg/ml and the lowest value of 0.113 mM at 100 μg/ml which were quite comparable to ascorbic acid (standard). Anti-inflammatory activity of VUTI was depicted by the method of inhibition of albumin denaturation where, VUTI showed high IC50 value of 696.46 µg/ml. Also, VUTI showed good antibacterial potential by inhibiting all tested bacterial strains with maximum inhibition against Bacillus subtilis (99.62%) and minimum against Staphylococcus aureus (34.62%). The results were quite comparable with standard drug ampicillin (5 mg/ml). Unfortunately, VUTI failed to show any activity against fungi.

Conclusion: Thus, the results obtained depict that VUTI additionally be a wonderful candidate for development of novel antibacterial drugs, and it can also be used to reduce the deletorious effects of free radicals.

Read more here: http://www.eurekaselect.com/153396/article

TESTIMONIAL BY FEDERICA POLLASTRO!

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