title: Cytotoxic and antimicrobial activities of aporphine alkaloids isolated from Stephania venosa (Blume) Spreng.
abstract: The cytotoxic activity of five alkaloids, namely 4,5-dioxo-dehydrocrebanine (1), dehydrocrebanine (2), crebanine (3), oxostephanine (4), and thailandine (5) isolated from the tuber and leaves of Stephania venosa (Blume) Spreng was investigated. Thailandine showed the strongest activity against lung carcinoma cells (A549) (IC50 of 0.30 µg/mL) with very low cytotoxicity against normal embryonic lung cells (MRC-5). Thailandine also demonstrated strong activity against Plasmodium falciparum, K1 strain (IC50 of 20 ng/mL), and Mycobacterium tuberculosis H(37)Ra (MIC of 6.25 µg/mL) as well as gram-positive bacteria such as Streptococcus pneumoniae and Staphylococcus aureus. Oxostephanine exhibited strong activity against breast cancer (BC) and acute lymphoblastic leukemia cells (MOLT-3) with an IC50 of 0.24 and 0.71 µg/mL, respectively, and exhibited very low cytotoxicity against MRC-5 cells. Dehydrocrebanine demonstrated strong activity against promyelocytic leukemia cells (HL-60) with an IC50 of 2.14 µg/mL whereas crebanine showed weak activity against cancer cell lines. However, both of them showed cytotoxicity against MRC-5 cells.
authors.affiliation: Chulabhorn Research Institute, Bangkok, Thailand.
authors.forename: Arthit
authors.initials: A
authors.lastname: Makarasen
authors.forename: Wandee
authors.initials: W
authors.lastname: Sirithana
authors.forename: Samang
authors.initials: S
authors.lastname: Mogkhuntod
authors.forename: Nisachon
authors.initials: N
authors.lastname: Khunnawutmanotham
authors.forename: Nitirat
authors.initials: N
authors.lastname: Chimnoi
authors.forename: Supanna
authors.initials: S
authors.lastname: Techasakul
mesh_terms: D000470:Alkaloids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000890:Anti-Infective Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001060:Aporphines / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D001232:Aspergillus fumigatus / Q000187:drug effects; D002175:Candida / Q000187:drug effects; D045744:Cell Line, Tumor; D005260:Female; D006094:Gram-Positive Bacteria / Q000187:drug effects; D018259:Herpesvirus 1, Human / Q000187:drug effects; D006801:Humans; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D010676:Phialophora / Q000187:drug effects; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D018515:Plant Leaves / Q000737:chemistry; D035281:Plant Tubers / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects; D031607:Stephania / Q000737:chemistry*; D013785:Thailand
chemical_list: D000470:Alkaloids; D000890:Anti-Infective Agents; D001060:Aporphines; D010936:Plant Extracts