T20 (generic name: Enfuvirtide, brand name: Fuzeon) is the only FDA-approved HIV fusion inhibitor that is being used for treatment of HIV/AIDS patients who have failed to respond to current antiretroviral drugs. However, it rapidly induces drug resistance in vitro and in vivo. On the basis of the structural and functional information of anti-HIV peptides from a previous study, we designed an HIV fusion inhibitor named CP32M, a 32-mer synthetic peptide that is highly effective in inhibiting infection by a wide range of primary HIV-1 isolates from multiple genotypes with R5-or dual-tropic (R5X4) phenotype, including a group O virus (BCF02) that is resistant to T20 and C34 (another anti-HIV peptide). Strikingly, CP32M is exceptionally potent (at low picomolar level) against infection by a panel of HIV-1 mutants highly resistant to T20 and C34. These findings suggest that CP32M can be further developed as an antiviral therapeutic against multidrug resistant HIV-1.drug-resistance ͉ gp41 ͉ peptide ͉ six-helix bundle

Radix Bupleuri is a traditional Chinese medicine harvested from two Bupleurum species (B. chinense and B. scorzonerifolium). It is widely used and is sourced from different regions of China. 1H NMR spectroscopy and multivariate data analysis were applied to 67 Radix Bupleuri samples to discriminate the two species, and explore the influences of habitat and culture method on the quality of Radix Bupleuri based on their metabolomics profiles. Metabolites responsible for the differences between the two species were higher levels of arginine, citric acid, sucrose, saikosaponin b1/b2 analogs, volatile oil with an (E)-2-olefin aldehyde fragment, and fatty acids in B. scoreonerifolium, and more saikosaponin a/c/d analogs in B. chinense. The variances of two cultivation areas were observed due to the higher amount of saikosaponins a/c/d in samples from Shaanxi and lipidsin samples from Shanxi. No obvious difference was detected between cultivars and wild type. 1HNMR metabolomics can simultaneously detect saikosaponins and hydrocarbon aldehydes, and also differentiate the two main saikosaponin skeletons, making it a suitable tool for the species discrimination and quality evaluation of Radix Bupleuri.

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A high-performance liquid chromatographic (HPLC) method was established to analyze 36 Chaihu (Radix Bupleuri) samples collected from three species (Bupleurum chinense DC., B. scorzonerifolium Willd. and B. smithii Wolff.). Addition of trifluoroacetic acid into the mobile phase resulted in fingerprint chromatograms with stable baselines. There were thirty-two characteristic peaks in the standard fingerprint of B. chinense DC. Different recognition pattern methods, including similarity analysis (SA), hierarchical cluster analysis (HCA), principal component analysis (PCA) and partial least squares-discrimination analysis (PLS-DA) were utilized to analyze the 36 samples based on the contents of chemical constituents. Consistent results from SA, HCA and PCA analysis illustrated the rationalisation for why B. smithii Wolff. was not quoted in the Chinese Pharmacopoeia and classified samples were in agreement with their species. PLS-DA loading plots showed the chemical markers which had the most influences on the separation among different species. However, SA, HCA and PCA could not differentiate between wild and cultivated B. chinense DC. as well as between samples from different provinces. HPLC fingerprint in combination with chemometric techniques provided a very flexible and reliable method for homogeneity evaluation and quality assessment of traditional Chinese medicine.