Curcumin: From a controversial "panacea" to effective antineoplastic products.

BACKGROUND: Curcumin, a controversial "panacea," has been broadly studied. Its bioactivities including antioxidant, anti-inflammatory, and especially antineoplastic activities have been documented. However, due to its extensive bioactivities, some scientists hold a skeptical point of view toward curcumin and described curcumin as a "deceiver" to chemists. The objective of this study was to explore curcumin's another possibility as a potential supplementary leading compound to cancer treatments. METHODS: Literature searches were conducted using electronic databases. Search terms such as "curcumin," "curcumin analogues," and so on were used. The literatures were collected and summarized. In this article, reported targets of curcumin are reviewed. The limitations of a curcumin as a therapeutic anticancer product including low bioavailability and poor targeting are mentioned. Furthermore, modified curcumin analogues and antitumor mechanisms are listed and discussed in the aspects of cell death and tumor microenvironment including angiogenesis, tissue hypoxia status, and energy metabolism. RESULTS: Several possible modification strategies were presented by analyzing the relationships between the antitumor activity of curcumin analogues and their structural characteristics, including the introduction of hydrophilic group, shortening of redundant hydrocarbon chain, the introduction of extra chemical group, and so on. CONCLUSIONS: From our perspective, after structural modification curcumin could be more effective complementary product for cancer therapies by the enhancement of targeting abilities and the improvement of bioavailability.

A novel recombinant peptide INSR-IgG4Fc (Yiminsu) restores insulin sensitivity in experimental insulin resistance models.

Type 2 diabetes mellitus (T2DM) is a chronic degenerative endocrine and metabolic disease with high mortality and morbidity, yet lacks effective therapeutics. We recently generated a novel fusion peptide INSR-IgG4Fc, Yiminsu (YMS), to facilitate the high-affinity binding and transportation of insulin. Thus, the aim of the present study was to determine whether the novel recombinant peptide, YMS, could contribute to restoring insulin sensitivity and glycaemic control in insulin resistance models and revealing its underlying mechanism. Palmitic acid (PA)-treated LO2 cells and high fat diet (HFD)-fed mice were treated with YMS. Therapeutic effects of YMS were measured using Western blotting, ELISA, qPCR, Histology and transmission electron microscopy. We observed that YMS treatment effectively improved insulin signaling in PA-treated LO2 cells and HFD-fed mice. Notably, YMS could significantly reduce serum levels of glucose, triglycerides, fatty acids and cholesterol without affecting the serum insulin levels. Moreover, our data demonstrated that YMS could restore glucose and lipid homeostasis via facilitating insulin transportation and reactivating PI3K/Akt signaling in both PA-treated cells and liver, gastrocnemius and brown fat of HFD-fed mice. Additionally, we noticed that the therapeutic effects of YMS was similar as rosiglitazone, a well-recognized insulin sensitizer. Our findings suggested that YMS is a potentially candidate for pharmacotherapy for metabolic disorders associated with insulin resistance, particularly in T2DM.

[Effects of the extracts from Ajuga decumbens on anti-fatigue in mice].

OBJECTIVE: To investigate the effects of extracts from Ajuga decumbens on anti-fatigue in mice. METHODS: One hundred and twenty female Kunming (KM) mice were randomly divided into quiet control group, sport control group, positive control group and 3 experimental groups which were the low, medium and high dose group given the extracts from Ajuga decumbens. The low, medium and high dose group were given the extracts with 100 mg/kg, 200 mg/kg, 400 mg/kg by body weight of mice for 30 d, respectively, but the positive control group was given American ginseng granules, while the quiet control group and the sport control groups were treated with saline. After this, the exhausting time, the physio-biochemical indexes (including lactic acid, blood urea nitrogen, blood sugar, total cholesterol and triglyceride) in serum, the contents of muscle and liver glycogen, and the antioxidative indexes (including glutathione peroxidase, superoxide dismutase, catalase and malondialdehyde) of organs in mice were investigated. RESULTS: The exhausting time, the number of red blood cell, the contents of hemoglobin and blood sugar, the contents of muscle and liver glycogen, and the activities of glutathione peroxidase, superoxide dismutase and catalase in organs of mice in the medium dose group and the high dose group were significantly more than those of the sport control group, but the contents of blood lactic acid, blood urea nitrogen and that of triglyceride and total cholesterol in serum, and the content of malondialdehyde in organs of mice in the medium dose group and the high dose group were significantly lower than those of the sport control group. And the effect of medium dose extracts from Ajuga decumbens on anti-fatigue was better than that of American ginseng granules. CONCLUSIONS: The extracts from Ajuga decumbens has significant anti-fatigue effect in mice.

[Effects of Lonicera Japonica flavone on immunomodulation in mice].

OBJECTIVE: To study immunomodulating activity of Lonicera Japonica flavone by investigating immune enzymatic activity of serum and antoxidized activity of lymphoid organs in mice. METHODS: Fifty KM mice were randomly divided into control group, model group, low dose group, middle dose group and high dose group(n = 10), respectively. And low dose group, middle dose group and high dose group were given Lonicera Japonica flavone with 100 mg/kg, 200 mg/kg and 400 mg/kg every day, respectively, while control group and model group were administered with NS. After continuously giving drug 7 weeks, other groups were injected with Dexamethasome (Dex: 25 mg /kg) for 3 days by subcutaneous injection, but the control group were treated with NS. And after giving Lonicera Japonica flavone 1 week simultaneously, organ indexes , the activity of acid phosphatase (ACP), alkaline phosphatase (AKP) and lysozyme (LSZ) in serum , and the content of monoamine oxidase (MAO), total antioxidant capacity (T-AOC), total superoxide dismutase (SOD) and malondialdehyde (MDA) in lymphoid organs in mice were tested, respectively. RESULTS: Lonicera Japonica flavone could significantly improve the organ indexes, and significantly improve the activity of ACP, AKP and LSZ in serum, and significantly improve the contents of T-AOC and SOD, but reduce that of MAO and MDA in lymphoid organs in immunosuppressed mice. CONCLUSION: Ionicera Japonica flavone can significantly improve the activity of immune enzyme in serum and the antioxidized activity of lymphoid organs in mice. It suggests that Ionicera Japonica flavone has a good immunomodulatory effects.