Heptazoline

Heptazoline exerts antiproliferative effects on human melanoma cells by inducing apoptosis, cell cycle arrest and targeting MAPK signalling pathway.[Pubmed:34269001]

J BUON. 2021 May-Jun;26(3):1184.

The Editors of JBUON issue an Expression of Concern to 'Heptazoline exerts antiproliferative effects on human melanoma cells by inducing apoptosis, cell cycle arrest and targeting MAPK signalling pathway', by Wei Zhou, Ling Zhou, Min Wang, Zeming Liu, Danyang Chen, Liang Guo; JBUON 2020;25(1):479-484; PMID: 32277672. Following the publication of the above article, readers drew to our attention that part of the data was possibly unreliable. We sent emails to the authors with a request to provide the raw data to prove the originality, but received no reply. Therefore, as we continue to work through the issues raised, we advise readers to interpret the information presented in the article with due caution. We thank the readers for bringing this matter to our attention. We apologize for any inconvenience it may cause.

Heptazoline exerts antiproliferative effects on human melanoma cells by inducing apoptosis, cell cycle arrest and targeting MAPK signalling pathway.[Pubmed:32277672]

J BUON. 2020 Jan-Feb;25(1):479-484.

PURPOSE: Melanoma is one of the prevalent types of cancer and ranks 6th major cause of cancer associated mortality. In this study the anticancer effects of the carbazole alkaloid Heptazoline were investigated against a panel of melanoma cells. METHODS: The normal BJ-5TA and melanoma cell lines MEL-CLS-1M MEL-CLS-2, MEL-CLS-3 were used in this study. MTT and colony formation assays were used to determine the proliferation rate of melanoma cells Aciridine orange (AO)/ ethidium bromide (EB) and annexin V/propidium iodide (PI) staining were used to check the apoptotic cell death. Cell cycle analysis was performed by flow cytometry and protein expression was checked by western blotting. RESULTS: Heptazoline inhibited the growth of all the melanoma cell lines, exhibiting an IC50 of 15 to 40 microM against the melanoma cells. However, the normal skin cells had IC50 125 microM. The anticancer effects were found to be due to induction of apoptotic cell death which was associated with the upregulation of Bax, cleaved caspase 3, 9 and PARP and downregulation of Bcl-2. Furthermore, Heptazoline also triggered the G0/G1 arrest of melanoma cells. The effects of Heptazoline on the MAPK signalling pathway revealed that this molecule could inhibit the expression of p-p38 concentration-dependently. CONCLUSION: Taken together, Heptazoline may prove a lead molecule in the development of systemic therapy of melanoma.

Antibacterial Activity of Coumarins and Carbazole Alkaloid from Roots of Clausena anisata.[Pubmed:30863444]

Adv Pharmacol Sci. 2019 Feb 3;2019:5419854.

Clausena anisata is one of the medicinal plants used traditionally for treatment of parasitic infections, irritation (boils, ringworm, and eczema), flatworm infestations, influenza, abdominal cramps, and constipation. Phytochemical screening test of dichloromethane/methanol (1 : 1) roots extract revealed the presence of flavonoids, phytosterols, coumarins, phenols, alkaloids, tannins, terpenoids, and free reducing sugars and the absence of saponins. Silica gel column chromatographic separation of the dichloromethane/methanol (1 : 1) extract afforded a carbazole alkaloid derivative of Heptazoline (1) and three coumarins (2-4), including the known coumarins imperatorin (3) and chalepin (4). Structures of the compounds were elucidated by spectroscopic techniques (IR, (1)H NMR, (13)C NMR, and DEPT-135). Antibacterial activity of the crude extracts and isolated compounds was screened using agar diffusion method against strains of Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, and Bacillus substilis. The results of antibacterial test revealed derivative of heptaphylline (1) and imperatorin (3) exhibited comparable antibacterial activity against S. aureus and B. substilis (14 and 13 mm zone of inhibition, respectively) to that of ciprofloxacin (15 mm zone of inhibition) at a concentration of 20 microg/mL. Chalepin (4) revealed more antibacterial activity against B. substilis (16 mm zone of inhibition) compared to ciprofloxacin (15 mm).

Heptazoline (CAS 32042-35-6) is a natural product offered by BioCrick for research applications. Customers can buy or order Heptazoline from BioCrick, a supplier and manufacturer of research chemicals, with product specifications, purity, packaging, and pricing information available upon request.