NEWS OF THE WEEK
NIH GRANT SUCCESS RATE IMPROVES
A
plications that resulted in National Institutes of Health grants for individual researchers— R01s and their equivalent—showed a slight uptick in 2014, according to NIH data released this month. The success rate, a gauge of the difficulty of getting an NIH grant, will be watched closely to see if a more positive trend for researchers has emerged.—ANDREA
FUNDING: Individual investigator
awards rebound slightly
WIDENER
7,028
32%
7,063 Awarded
32% Success rate
2001 21,967
6,965
32%
6,799
2003 24,634
31%
7,430
2004 27,461
30% 6,991
2005 28,423
25%
6,463
2006 29,097
23%
6,037
2007 27,325
21% 24%
6,456
2008 26,648
6,116
23%
2009 26,675
5,924
22%
2010 27,850 NOTE: All data are for R01 or equivalent awards: R23, R29, and R37. Actual dollars awarded without adjustment for inflation. SOURCE: NIH Data Book
$262,347
1999 21,944 2000 Year 22,088 Total applications 2002 22,212
2011
6,217
28,781
22%
5,380
2012 29,626
19% 18%
5,436
2013 28,044
4,902
2014 27,502
5,163
NEW CLASS OF BIOACTIVES NATURAL PRODUCTS: Triterpenoids
with unprecedented ring system are stout immunosuppressants
W
FTER YEARS of decline, the percentage of ap-
HETHER THEY’RE picking apart an ancient
Chinese herbal medicine or a backwoods home remedy from the southern Appalachians, chemists are interested in identifying bioactive Phainanoid F, molecules in various cures and determining how they with its spirocyclic work. Now and again the scientists come across somegroups highlighted in red, is the most thing interesting. powerful of the A research team led OCH3 O newly discovO by Jian-Min Yue of the ered immunoO OCH3 Shanghai Institute of MaO suppressants. O teria Medica of the ChiH OH nese Academy of Sciences has uncovered H six new compounds, called phainanoids A–F, notable for a never-before-seen ring system. The researchers found that the bioactive molecules have H O the potential to knock down the body’s immune system, O H which could help prevent organ transplant rejection and OH immunity-associated disorders such as multiple scleroO sis (J. Am. Chem. Soc. 2014, DOI: 10.1021/ja511813g). Phainanoid F CEN.ACS.ORG
6
17% 19%
$6,737,855,769
282,591 Average award
7,616,683,058 Total funding
$304,110
$8,513,561,502
324,325
9,362,950,132
340,974
10,101,683,116
352,214
10,555,849,413
361,611
10,685,232,289
361,307
10,522,350,609
362,970
10,427,770,948
373,804
10,429,497,662
391,281
10,725,000,910
403,691
11,125,330,616
408,594
10,975,655,055
419,321
11,021,860,936
405,874
10,174,867,296
431,177
10,359,458,392
Yue and coworkers came across the phainanoids while studying Phyllanthus hainanensis, a chemically uncharacterized member of a group of some 700 flowering plants scattered throughout tropical regions. Some Phyllanthus species are used in traditional Chinese medicine and Ayurvedic medicine in India for treating infections, diabetes, and hepatitis B. The right side of the phainanoid ring system is structurally similar to a rare group of dichapetalin-type triterpenoids that contain a spirocyclic lactone. The left side, however, is unprecedented in containing a second spirocyclic group—a benzofurancyclobutanone. After characterizing the phainanoids by spectroscopic and chemical methods, including X-ray crystallography, the Shanghai researchers tested the compounds for their ability to impede proliferation of white blood cells (lymphocytes) from mice. They found that the immunosuppressive properties exceed those of cyclosporin A, a drug often given to transplant patients and people with rheumatoid arthritis. “The nanomolar values effective against both T and B cells are certainly impressive and unexpected,” notes A. Douglas Kinghorn, editor-in-chief of the Journal of Natural Products and a professor at Ohio State University, whose research group studies Phyllanthus anticancer compounds. “It does seem as if compounds from plants in the genus Phyllanthus do have potential in modulating the immune system in humans.”—STEVE RITTER
JANUARY 12, 2015