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. 2021 Apr 19;11(4):603. doi: 10.3390/biom11040603

Table 4.

Pharmacological activities of podophyllotoxin and its derivatives.

Activity Podophyllotoxin Derivative Mechanism Conclusion Ref.
Cytotoxic activity Cleistantoxin Activity was checked against MCF-7, MCF-7R, KBand HT29 cancer cell lines Cleistantoxin showed strong cytotoxic activity [146]
Antibacterial activity New precursors of podophyllotoxin were synthesized, and screened to check their antibacterial activity Activity was checked against Klebsiella pneumoniae, Streptococcus faecalis, Citrobacter sp., Pseudomonas aeruginosa, Escherchia coli, Salmonella typhi and Shigella sonnei Ethyl-2-(3′-methyl-4′-methoxybenzoyl)-3-(4″ methoxyphenol)-cyclopropane-1-carboxylic acid and Ethyl-2-(3′-methyl-4′-methoxybenzyol-3-1 3″, 4″-dimethoxyphenyl)-cyclopropane-carboxylic acid, both of them showed significant antibacterial activity [147]
Antitumour activity VP 16-213 (NSC-141540) Activity was checked against L1210 ascites tumour in N/D mice In 24 hours, divided treatment after every 3 hours, resulted in significant cure, hence, VP 16-213 is a cell cycle specific drug [148]
Insecticidal activity 20 podophyllotoxin analogues were tested Activity was checked against fifth-instar larvae of Brontispa longissima in vivo Among 20 analogues Deoxypodophyllotoxin showed more protential for insecticidal activity than a commercial insecticide (toosendanin) [149]
Antineoplastic activity New hybrids of podophyllotoxin and indirubin Activity was checked against human leukemia cancer cells as a multifunctional anti-MDR agent Podophyllotoxin-indirubin hybrid (Da-1) showed potential to overcome drug resistance. It is a novel hybrid havingpotent antiproliferative activity [150]
Cyclolignans, derived from podophyllotoxin Activity was checked againstA-549 human lung carcinoma, P-388 murine leukemia and HT-29 colon carcinoma A number of substances were active in assay at concentrations below 1 pM; deoxypodophyllotoxin being the most potent compound in all cases [151]