ABSTRACT
A novel monoterpenoid indole alkaloid, melognine (1) possessing an unprecedented skeleton with a 6/6/5/5/6/6 hexatomic rearranged ring system was isolated from the stems of Melodinus fusiformis. The structure with absolute configuration of 1 was established by extensive spectroscopic analyses and quantum ECD calculations. Melognine showed significant cytotoxicity on human breast cancer BT549 cells with an IC50 value of 1.49 µM by MTT assay. Further mechanism of action study indicated that melognine demonstrated the ability to induce apoptosis by activation of caspase-3 and p53, and downregulation of Bcl-2 in BT549 cells.
Subject(s)
Apocynaceae , Apoptosis/drug effects , Secologanin Tryptamine Alkaloids , Apocynaceae/chemistry , Cell Line, Tumor , Humans , Molecular Structure , Monoterpenes/isolation & purification , Monoterpenes/pharmacology , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Plant Stems/chemistry , Secologanin Tryptamine Alkaloids/isolation & purification , Secologanin Tryptamine Alkaloids/pharmacologyABSTRACT
Two new butenolides, balanolides A (1) and B (1), were isolated from the aerial parts of the parasitic plant Balanophora fungosa. Their structures were established by comprehensive spectroscopic analysis and quantum chemical ECD calculation. The new butenolides were evaluated for their inhibitory effects against nitric oxide (NO) production in LPS-induced RAW 264.7 macrophage cells. Compounds 1 and 2 displayed moderate anti-inflammatory activity with IC50values of 11.8 and 12.9 µM, respectively.
Subject(s)
4-Butyrolactone/analogs & derivatives , Anti-Inflammatory Agents/pharmacology , Balanophoraceae/chemistry , 4-Butyrolactone/pharmacology , Animals , Lipopolysaccharides/pharmacology , Macrophages/drug effects , Mice , Nitric Oxide/biosynthesis , Plant Extracts/chemistry , RAW 264.7 CellsABSTRACT
Four new aspidosperma-type alkaloids, melosuavines J-M (1-4) were isolated from the leaves of Melodinus suaveolens. Their structures with absolute configurations were elucidated by extensive HRESIMS and NMR spectroscopic analysis, as well as ECD calculations and Mosher's method. Their cytotoxic activities against four human cancer cell lines were also evaluated.
Subject(s)
Alkaloids/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Apocynaceae/chemistry , Plant Leaves/chemistry , Alkaloids/isolation & purification , Antineoplastic Agents, Phytogenic/isolation & purification , Cell Line, Tumor , China , Humans , Molecular Structure , Phytochemicals/isolation & purification , Phytochemicals/pharmacologyABSTRACT
Tanshinone IIA (Tan IIA) is a pharmacologically lipophilic active constituent isolated from the roots and rhizomes of the Chinese medicinal herb Salvia miltiorrhiza Bunge (Danshen). Tan IIA is currently used in China and other neighboring countries to treat patients with cardiovascular system, diabetes, apoplexy, arthritis, sepsis, and other diseases. Recently, it was reported that tan IIA could have a wide range of antitumor effects on several human tumor cell lines, but the research of the mechanism of tan IIA is relatively scattered in cancer. This review aimed to summarize the recent advances in the anticancer effects of tan IIA and to provide a novel perspective on clinical use of tan IIA.
ABSTRACT
A new bisindole alkaloid, melosuavine I (1) possessing an aspidosperma-aspidosperma dimeric skeleton, was isolated from the leaves of Melodinus suaveolens. The structure with absolute configuration of 1 was elucidated by a combination of MS, NMR and computational methods. MTT assays indicated that 1 exhibited significant cytotoxicity on human breast cancer BT549 cells with an IC50 value of 0.89⯵M. Further study showed that 1 inhibited BT549 cell proliferation by inducing apoptosis through activation of caspase 3 and p53, and down-regulation of Bcl-2.
