A new dihydroflavone and a new polyacetylene glucoside from Bidens parviflora.

A new dihydroflavone, 2(S)-isookanin-4'-methoxy-8-O-ß-D-glucopyranoside (1), and a new polyacetylene glucoside, (10S)-tridecane-2E-ene-4,6,8-triyne-1-ol-10-O-ß-D-glucopyranoside (2), along with seven known compounds (3-9), were isolated from the herb of Bidens parviflora Willd. The structures of all the extracted compounds were elucidated by HR-ESI-MS, 1 D and 2 D NMR spectra, as well as circular dichroism (CD).

CDC6 is a possible biomarker for hepatocellular carcinoma.

OBJECTIVE: Research has proven that the expression of CDC6 is tightly related to tumorigenesis and progression of various tumors. However, the effects of CDC6 in hepatocellular carcinoma remain uncertain. The main purpose of this research is to explore this relationship. METHODS: We assessed the expression levels of CDC6 in a serious of cancers from GEPIA database. The expression of CDC6 in hepatocellular carcinoma tissue and normal liver tissue was compared, and further assessed by immunohistochemical staining. Graphpad software was performed for data analysis, and t-test and χ2 analysis were used to investigate the role of CDC6 in hepatocellular carcinoma. RESULTS: The expression level of CDC6 was significantly higher in malignant carcinoid, melanoma, urothelial tumor, and hepatocellular carcinoma in the GEPIA online database. It was related to clinical progression of hepatocellular carcinoma. We found that the expression of CDC6 was correlated with tumor size (P=0.018) and the number of tumor nodes (P=0.003), but not with age, gender and AFP value (P>0.05). CONCLUSIONS: The expression level of CDC6 in hepatocellular carcinoma is related tightly to clinical findings. Detecting the expression of CDC6 might provide a new biomarker for patients with hepatocellular carcinoma.

Identification of kinesin family member 3B (KIF3B) as a molecular target for gastric cancer.

Gastric cancer (GC) is the fourth most common malignancy worldwide, with 80% mortality rate in over 70% countries. Recently, targeted therapy for GC has great clinical prospects, and it is still badly needed to find novel molecular targets to control the progression and development of GC. Kinesin family member 3B (KIF3B) is known as a microtubule motor kinesin and one of the most ubiquitously expressed KIFs. KIF3B participates in multiple cellular processes such as mitosis and spermatogenesis, and the possible role of KIF3B on tumor progression has been widely revealed. KIF3B affects the progression and metastasis of multiple types of tumors, such as pancreatic cancer, prostate cancer, and hepatocellular carcinoma; however, its potential impact on GC is still unknown. Herein, we explored the possible role of KIF3B on the progression of GC and noticed that KIF3B was high expression in tumor tissues from GC patients. KIF3B was also significantly correlated with clinical pathological characteristics such as tumor size (P = .014*) and recurrence (P = .044*). We further revealed that KIF3B depleted GC cells exhibited impaired proliferation capacity in vitro. Similarly, KIF3B depletion suppressed tumor growth of GC cells in mice. In conclusion, we identified KIF3B as a promising therapeutic target for the treatment of GC.

Ingredients from Litsea garrettii as Potential Preventive Agents against Oxidative Insult and Inflammatory Response.

Oxidative stress and inflammation undoubtedly contribute to the pathogenesis of many human diseases. The nuclear transcription factor erythroid 2-related factor (Nrf2) and the nuclear factor κB (NF-κB) play central roles in regulation of oxidative stress and inflammation and thus are targets for developing agents against oxidative stress- and inflammation-related diseases. Our previous study indicated that the EtOH extract of Litsea garrettii protected human bronchial epithelial cells against oxidative insult via the activation of Nrf2. In the present study, a systemic phytochemical investigation of L. garrettii led to the isolation of twenty-one chemical ingredients, which were further evaluated for their inhibitions on oxidative stress and inflammation using NAD(P)H:quinone reductase (QR) assay and nitric oxide (NO) production assay. Of these ingredients, 3-methoxy-5-pentyl-phenol (MPP, 5) was identified as an Nrf2 activator and an NF-κB inhibitor. Further studies demonstrated the following: (i) MPP upregulated the protein levels of Nrf2, NAD(P)H:quinone oxidoreductase 1 (NQO1), and glutamate-cysteine ligase regulatory subunit (GCLM); enhanced the nuclear translocation and stabilization of Nrf2; and inhibited arsenic [As(III)]-induced oxidative insult in normal human lung epithelial Beas-2B cells. And (ii) MPP suppressed the nuclear translocation of NF-κB p65 subunit; inhibited the lipopolysaccharide- (LPS-) stimulated increases of NF-κB p65 subunit, COX-2, iNOS, TNF-α, and IL-1ß; and blocked the LPS-induced biodegrade of IκB-α in RAW 264.7 murine macrophages. Taken together, MPP displayed potential preventive effects against inflammation- and oxidative stress-related diseases.

The genus Litsea in traditional Chinese medicine: an ethnomedical, phytochemical and pharmacological review.

ETHNOPHARMACOLOGICAL RELEVANCE: The genus Litsea, mainly distributed in the tropical and subtropical regions, has been used in traditional and indigenous Chinese medicines for the treatment of diarrhea, stomachache, dyspepsia, gastroenteritis, diabetes, edema, cold, arthritis, asthma, pain, traumatic injury, etc. for a long history. The present review aims to provide a comprehensive summary on the ethnomedical uses, phytochemistry, and pharmacology of the Litsea species used in traditional Chinese medicine (TCM). Based on these data, evidences supporting their ethnopharmacological effectiveness are illustrated, and opportunities for the future research and development as well as the therapeutic potential of this genus are analyzed to highlight the gaps in our knowledge that deserves further investigation. MATERIAL AND METHODS: Information on the Litsea species was collected via electronic search (using Pubmed, SciFinder, Google Scholar, Web of Science and CNKI) and a library search for articles published in peer-reviewed journals. Furthermore, information was also obtained from some local books on ethnopharmacology. RESULTS: Twenty plants of the genus Litsea are found to be important traditional medicines in China, and have a long medicinal application for diarrhea, stomachache, dyspepsia, gastroenteritis, diabetes, edema, cold, arthritis, asthma, pain, traumatic injury, etc. Over 200 ingredients have been identified from these 20 Litsea species used in TCM, and flavonoids, terpenoids and alkaloids are considered as the characteristic and bioactive constituents. The crude extracts and the isolated metabolites of these medicinal plants have exhibited some in vitro and in vivo pharmacological effects, including antimicrobial, hepatoprotection, anti-inflammatory, antiasthmatic, immunomodulation, anti-diabetic, anticholelithogenic, as well as function on central nervous system, etc. CONCLUSIONS: The extensive literature survey reveals Litsea species to be a group of important medicinal plants used for the ethnomedical treatment of gastrointestinal diseases, diabetes, inflammatory disorders, and microbial infection in TCM. Pharmacological investigations have supported the use of some Litsea species in the traditional medicines. In addition, further researches targeting individual ingredients responsible for the pharmacological effects, as well as their mechanisms of action are necessary. The outcome of these studies will further support the therapeutic potential of the genus Litsea, and provide convincing evidences to its future clinical applications in modern medicine.