Abstract
One new cyclic hexapeptide named rubipodanin A (1), which is the first identified natural N-desmonomethyl Rubiaceae-type cyclopeptide, together with six known Rubiaceae-type cyclopeptides (2-7) were obtained using the TLC cyclopeptide protosite detection method with ninhydrin from the roots and rhizomes of Rubia podantha. The cyclopeptide structures were elucidated by extensive spectroscopic analysis, including 1D-NMR, 2D-NMR, IR, UV and MS. The solution conformation and biological activities of 1 and RA-V (4) were evaluated, and the results demonstrated that the N9-methyl group plays a vital role in the maintenance of the conformation and bioactivity.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Cell Line
-
Cell Proliferation / drug effects
-
Cell Survival / drug effects
-
HEK293 Cells
-
HeLa Cells
-
Humans
-
Molecular Structure
-
Peptides, Cyclic / chemistry*
-
Peptides, Cyclic / pharmacology
-
Plant Extracts / chemistry*
-
Plant Extracts / pharmacology
-
Plant Roots / chemistry*
-
Rubia / chemistry*
Substances
-
Peptides, Cyclic
-
Plant Extracts
Grants and funding
This work was supported by the National Basic Research Program of China (2013CB127505), the Foundation of Chinese Academy of Sciences (Hundred Talents Program, XDA09030301-4), the National Natural Science Foundation of China (U1032602, 91013002, 31470428), the National New Drug Innovation Major Project of China (2011ZX09307-002-02), and the Natural Science Foundation of Yunnan Province (2012GA003).