Honokiol: A naturally occurring lignan with pleiotropic bioactivities / 中国天然药物

Honokiol is the dominant biphenolic compound isolated from the Magnolia tree, and has long been considered as the active constituent of the traditional Chinese herb, 'Houpo', which is widely used to treat symptoms due to 'stagnation of qi'. Pharmacological studies have shown that honokiol possesses a wide range of bioactivities without obvious toxicity. Honokiol protects the liver, kidneys, nervous system, and cardiovascular system through reducing oxidative stress and relieving inflammation. Moreover, honokiol shows anti-diabetic property through enhancing insulin sensitivity, and anti-obese property through promoting browning of adipocytes. In vivo and in vitro studies indicated that honokiol functions as an anti-cancer agent through multiple mechanisms: inhibiting angiogenesis, promoting cell apoptosis, and regulating cell cycle. A variety of therapeutic effects of honokiol may be associated with its physiochemical properties, which make honokiol readily cross the blood brain barrier and the blood-cerebrospinal fluid barrier, with high bioavailability. In the future, more clinical researches on honokiol are needed to fully authenticate its therapeutic values.

14-Deoxygarcinol, a polyisoprenylated benzophenone from Garcinia cambogia, ameliorates inflammatory responses in adipose tissue via suppressing NLRP 3 inflammasome / 中国药理学与毒理学杂志

OBJECTIVE Interleukin (IL)-1β, one of the principal inflammatory cytokines mainly secreted by mono?cytes and macrophages, is produced by cleavage of the inactive pro-IL-1βprecursor by caspase-1 via the NLRP3 inflam?masome complex. The fruits of Garcinia cambogia (Clusiaceae) are widely developed as health products for anti-obese purpose. 14-deoxygarcinol (DOG) is a polyisoprenylated benzophenone from the fruits of G. cambogia, which showed potent anti-inflammatory effect in our previous study. The objective of this study was to explore the anti-inflammatory mechanism of DOG and its roles in alleviating adipose tissue inflammation and insulin resistance. METHODS The anti-inflammatory effect of DOG was evaluated on LPS plus nigericin-induced THP-1 macrophages. The expression of NLRP3 inflammasome complex proteins was analyzed by Western blotting, immunofluorescence staining and co-immu?noprecipitation. The pro-inflammatory cytokines levels were determined by ELISA kits. RESULTS DOG increased the expression of Sirtuin 2 (SIRT2) deacetylase and enhanced its deacetylating activity to suppress the NLRP3 inflamma?some activation and IL-1βsecretion in THP-1 macrophages. Moreover, DOG attenuated macrophage conditioned medium-induced inflammatory responses in adipocytes and blocked THP-1 macrophages migration towards 3T3-L1 adipocytes. CONCLUSION DOG attenuated the inflammatory crosstalk between macrophages and adipocytes through SIRT2-mediated NLRP3 inflammasome inhibition, which might be used for the treatment of adipose tissue inflammation-related metabolic disorders.

Nagilactone E increases PD-L1 expression through activation of c-Jun in lung cancer cells / 中国天然药物

Nagilactone E (NLE), a natural product with anticancer activities, is isolated from Podocarpus nagi. In this study, we reported that NLE increased programmed death ligand 1 (PD-L1) expressions at both protein and mRNA levels in human lung cancer cells, and enhanced its localization on the cell membrane. Mechanistically, NLE increased the phosphorylation and expression of c-Jun, and promoted the localization of c-Jun in the nucleus, while silencing of c-Jun by small interfering RNA (siRNA) reduced NLE-induced PD-L1. Further study showed that NLE activated the c-Jun N-terminal kinases (JNK), the upstream of c-Jun, and its inhibitor SP600125 reversed the NLE-increased PD-L1. Moreover, NLE-induced PD-L1 increased the binding intensity of PD-1 on the cell surface. In summary, NLE upregulates the expression of PD-L1 in lung cancer cells through the activation of JNK-c-Jun axis, which has the potential to combine with the PD-1/PD-L1 antibody therapies in lung cancer.

Anticancer carbazole alkaloids and coumarins from Clausena plants: A review / 中国天然药物

Pharmaceutical research has focused on the discovery and development of anticancer drugs. Clinical application of chemotherapy drugs is limited due to their severe side effects. In this regard, new naturally occurring anticancer drugs have gained increasing attention because of their potential effectiveness and safety. Fruits and vegetables are promising sources of anticancer remedy. Clausena (family Rutaceae) is a genus of flowering plants and includes several kinds of edible fruits and vegetables. Phytochemical and pharmacological studies show that carbazole alkaloids and coumarins from Clausena plants exhibit anticancer activity. This review summarizes research progresses made in the anticancer properties of plants belonging to Clausena; in particular, compounds with direct cytotoxicity, cell cycle arrest, apoptosis induction, and immune potentiation effects are discussed. This review reveals the potential use of plants from Clausena in preventing and treating cancer and provides a basis for development of relevant therapeutic agents.

Chemical constituents from roots of Breynia fruticosa / 中草药

Objective: To study the chemical constituents from the roots of Breynia fruticosa. Methods: The compounds were isolated by comprehensive column chromatography, and the structures were elucidated by spectral methods. Results: Thirteen compounds were isolated and elucidated, including four triterpenoids, friedelin (1), friedelinol (2), lupenone (3), and glochidiol (4); three steroids, including β-sitosterol (5), stigmastane-3β, 6β-diol (6), and β-sitosterylglucoside-6'-octadecanoate (7); two cerebrosides, including 1-O-β-D-glucopyranosyl-(2S, 3R, 4E, 8Z)-2-[(2-hydroxyoctadecanoyl) amido]-4, 8-octadecadiene-1, 3-diol (8) and 1-O-β-D-glucopyranosyl-(2S, 3S, 4R, 8Z)-2-[(2R)-2-hydroxypentacosanoylamino]-8-octadecene-1, 3, 4-triol (9); and four other compounds, including (-)-epicatchin (10), ε-caprolactone (11), aviculin (12), and vanillin (13). Conclusion: Compounds 3, 4, 6-9, and 11 are isolated from the plant of Breynia J. R. et G. Forst. nom. cons. for the first time, and compound 11 is isolated from the natural product for the first time.

Deep inferior epigastric perforator (DIEP) free flap in immediate breast reconstruction / 中华整形外科杂志

<p><b>OBJECTIVE</b>In order to facilitate psychological rehabilitation of the women who underwent modified radical mastectomy for breast cancer, the DIEP free flap was used for immediate breast reconstruction in a series of patients. We present a review of the surgical outcomes.</p><p><b>METHODS</b>From December 2001 to January 2003, unilateral breast reconstruction was performed in 12 patients using the DIEP free flap at the same time of modified radical mastectomy in our department. The recipient vessels were the thoracodorsal artery and vein or the internal mammary artery and its venae concomitants.</p><p><b>RESULTS</b>Of the 12 DIEP flaps, 1 was vascularized by a single perforator, 3 were vascularized by two perforators, 6 by three perforators, 1 by four an 1 by five perforators. One flap failed totally, likely due to previous multiple lower abdominal operations. The eleven reconstructed breasts achieved almost the same size and shape as the healthy sides. The time of patient getting out of bed ranged from 3 to 7 days and the mean hospital stay was 8.8 days. All patients were satisfied with the outcome. No complications were observed in the abdominal wall, including weakness, abdominal bulge or hernia.</p><p><b>CONCLUSION</b>Immediate breast reconstruction facilitates the psychological rehabilitation and helps to avoid the dressing inconveniences resulted from total mastectomy. Free DIEP flap is a new and reliable technique for immediate breast reconstruction with autologous tissue. This flap offers the patients the same advantages as the TRAM flap and avoids its most important disadvantage of potential abdominal wall weakness, by preserving the continuity of the rectus abdominis muscle. The donor site morbidity is thus reduced and recovery is faster. The more complex nature of this procedure leads to increased operating time and requires more demanding surgical skills.</p>