Bioactivity guided isolation of anticancer constituents from leaves of Alnus sieboldiana (Betulaceae).
The leaves of the Japanese Alnus sieboldiana have been extracted with n-hexane and then with methanol. A bioactivity-guided approach based on MTT assay for growth inhibition and quantitative real-time PCR for TNF-α inhibitory activity was taken to identify the active compounds in EtOAc soluble fraction of the methanol extract. From this active fraction, seven compounds have been isolated and four compounds (pinosylvin, galangin, quercetin and methyl gallate) have been examined for their dose-response effect on the viability of A549 cells and on TNF-α inhibitory activity. Based on MTT assay, all of the four examined compounds inhibit growth of human lung cancer cells. Among four tested compounds only galangin (3,5,7-trihydroxyflavone) significantly inhibited TNF-α gene expression in A549 cells (IC₅₀ = 94 μM). Taken together, this finding suggests that galangin may be useful in cancer prevention.
Laboratory of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Tokushima Bunri University, 180 Yamaschiro-cho, Tokushima 770-8514, Japan.
A
A
Ludwiczuk
A
A
Saha
T
T
Kuzuhara
Y
Y
Asakawa
D029661:Alnus / Q000737:chemistry*; D016588:Anticarcinogenic Agents / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use; D000972:Antineoplastic Agents, Phytogenic / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D005419:Flavonoids / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use*; D005707:Gallic Acid / Q000031:analogs & derivatives / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D018515:Plant Leaves; D011794:Quercetin / Q000302:isolation & purification / Q000494:pharmacology; D013267:Stilbenes / Q000302:isolation & purification / Q000494:pharmacology; D014409:Tumor Necrosis Factor-alpha / Q000037:antagonists & inhibitors*; D000094162:Phytoalexins
D016588:Anticarcinogenic Agents; D000972:Antineoplastic Agents, Phytogenic; D005419:Flavonoids; D005707:Gallic Acid; D010936:Plant Extracts; D011794:Quercetin; D013267:Stilbenes; D014409:Tumor Necrosis Factor-alpha; C037032:galangin; C052082:methyl gallate; C049032:pinosylvin; D000094162:Phytoalexins