Both Cinnamomum verum J.S. Presl. and Cinnamomum cassia Blume are collectively called Cortex Cinnamonmi for their medicinal cinnamon bark. Cinnamomum verum is more popular elsewhere in the world, whereas C. cassia is a well known traditional Chinese medicine. An analysis of hydro-distilled Chinese cinnamon oil and pure cinnamaldehyde by gas chromatography/mass spectrometry revealed that cinnamaldehyde is the major component comprising 85% in the essential oil and the purity of cinnamaldehyde in use is high (> 98%). Both oil and pure cinnamaldehyde of C. cassia were equally effective in inhibiting the growth of various isolates of bacteria including Gram-positive (1 isolate, Staphylococcus aureus), and Gram-negative (7 isolates, E. coli, Enterobacter aerogenes, Proteus vulgaris, Pseudomonas aeruginosa, Vibrio cholerae, Vibrio parahaemolyticus and Samonella typhymurium), and fungi including yeasts (four species of Candida, C. albicans, C. tropicalis, C. glabrata, and C. krusei), filamentous molds (4 isolates, three Aspergillus spp. and one Fusarium sp.) and dermatophytes (three isolates, Microsporum gypseum, Trichophyton rubrum and T. mentagraphytes). Their minimum inhibition concentrations (MIC) as determined by agar dilution method varied only slightly. The MICs of both oil and cinnamaldehyde for bacteria ranged from 75 microg/ml to 600 microg/ml, for yeasts from 100 microg/ml to 450 microg/ml, for filamentous fungi from 75 microg/ml to 150 microg/ml, and for dermatophytes from 18.8 microg/ml to 37.5 microg/ml. The antimicrobial effectiveness of C. cassia oil and its major constituent is comparable and almost equivalent, which suggests that the broad-spectrum antibiotic activities of C. cassia oil are due to cinnamaldehyde. The relationship between structure and function of the main components of cinnamon oil is also discussed.

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Isodeoxyelephantopin (ESI), isolated from Elephantopus scaber L. has been reported to exert anticancer effects. In this study, we aimed to investigate whether and how cancer cells exert protective responses against ESI treatment. Confocal fluorescence microscopy showed that ESI significantly induced autophagy flux in the lung cancer cells expressing mCherry-EGFP-LC3 reporter. Treatment of the cells with ESI increased the expression levels of the autophagy markers including LC3-II, ATG3 and Beclin1 in a dose-dependent manner. Pretreatment with autophagy inhibitor 3-methyladenine (3-MA) not only attenuated the effects of ESI on autophagy, but also enhanced the effects of ESI on cell viability and apoptosis. Mechanistically, the SILAC quantitative proteomics coupled with bioinformatics analysis revealed that the ESI-regulated proteins were mainly involved in Nrf2-mediated oxidative stress response. We found that ESI induced the nuclear translocation of Nrf2 for activating the downstream target genes including HO-1 and p62 (SQSTM1). More importantly, ESI-induced p62 could competitively bind with Keap1, and releases Nrf2 to activate downstream target gene p62 as a positive feedback loop, therefore promoting autophagy. Furthermore, knockdown of Nrf2 or p62 could abrogate the ESI-induced autophagy and significantly enhanced the anticancer effect of ESI. Taken together, we demonstrated that ESI can sustain cell survival by activating protective autophagy through Nrf2-p62-keap1 feedback loop, whereas targeting this regulatory axis combined with ESI treatment may be a promising strategy for anticancer therapy.

Eight new matrine-type alkaloids, flavesines G−J (1−4), alopecurine B (5), 7,11-dehydro-oxymatrine (6), 10-oxy-5,6-dehydromatrine ( 7), and 10-oxysophoridine (8), along with nine known analogues (9−17) were isolated from the roots of Sophora f lavescens. Compounds 1−3 are the first natural matrine-type alkaloids with an open-loop ring D, while compound 4 represents an unprecedented dimerization pattern constructed from matrine and piperidine, and 5 is the first example of a matrine-type alkaloid with cleavage of the C-5−C-6 bond. The new structures were elucidated by means of spectroscopic data analysis (including NMR, MS, IR, and UV), and the absolute configurations were determined using single-crystal X-ray diffraction and ECD data. The isolated alkaloids were evaluated for their antiviral activity against hepatitis B virus, and compounds 1, 4, 5, 10, and 14 exhibited comparable antiviral potencies to matrine.

The aqueous extracts from 21 medicinal herbs traditionally used in southern mainland China were screened for antiviral activities against human herpes simplex virus type 1 (HSV-1) and human respiratory syncytial virus (RSV) using a cytopathic effect (CPE) reduction assay. Three extracts from Agrimonia pilosa, Pithecellobium clypearia and Punica granatum, respectively, showed anti-HSV-1 activity, which was possibly contributed by the polyphenolic compounds in the herbal extracts. Six of the extracts, from Blumea laciniata, Elephantopus scaber, Laggera pterodonta, Mussaenda pubescens, Schefflera octophylla and Scutellaria indica, respectively, exhibited anti-RSV activity with 50% inhibition (IC50) concentrations ranging from 12.5 to 32 microg/mL, and selective indices (SI) ranging from 11.2 to 40. In addition to polyphenolic compounds, other constituents present in these extracts may also contribute to their anti-RSV activity.

The present study found that the supercritical fluid extract of "Guangchenpi" possessed in vitro antiviral activity against respiratory syncytial virus (RSV). Bioassay-guided isolation and identification of this extract led to obtain five active polymethoxylated flavones (1-5). Cytopathic effect (CPE) reduction assay exhibited that tangeretin (2) and nobiletin (3), two major polymethoxylated flavones in the extract, possessed better anti-RSV effect comparable to the positive control ribavirin. Plaque reduction assay revealed that tangeretin dose-dependently inhibited RSV-induced plaque formation on the HEp-2 cells. This polymethoxylated flavone mainly affected the intracellular replication of RSV, and it also could inhibit RSV entry into the HEp-2 cells. Further investigations with quantitative real-time PCR and confocal and Western blot assays indicated that tangeretin downregulated the expression of RSV phosphoprotein (P protein). Results suggest the potential application of the supercritical fluid extract of "Guangchenpi" and tangeretin in the treatment and the prevention of RSV infection.

Seven new clerodane diterpenoids (1-7) were isolated from roots of Croton crassifolius, along with six known compounds. The structures were elucidated by extensive spectroscopic methods (IR, UV, HRESIMS, 1D NMR, and 2D NMR), and the structures of 1, 3, 4, and 7 were confirmed by single-crystal X-ray diffraction analyses. Compounds 1-13 were evaluated for in vitro antiviral activity against herpes simplex virus type 1 using the cytopathic effect reduction assay.