The interest of Western medicine in Traditional Chinese Medicine (TCM) as a source of drug leads/new drugs to treat diseases without available efficient therapies has been dramatically augmented in the last decades by the extensive work and the outstanding findings achieved within this kind of medicine. The practice of TCM over thousands of years has equipped scientists with substantial experience with hundreds of plants that led to the discovery of artemisinin (qinghaosu), which is extracted from the medicinal plant Artemisia annua L. (qinghao). The unexpected success of artemisinin in combating malaria has drawn strong attention from the scientific community towards TCM. Artemisinin was discovered by Youyou Tu in 1972. Since then, several novel pharmacological activities based on the well-known properties of the sesquiterpene lactone structure with the oxepane ring and an endoperoxide bridge have been unravelled. Beyond malaria, artemisinin and its derivatives (artemisinins) exert profound activities towards other protozoans (Leishmania, Trypanosoma, amoebas, Neospora caninum, and Eimeria tenella), trematodes (Schistosoma, liver flukes), and viruses (human cytomegalovirus, hepatitis B and C viruses). Less clear is the effect against bacteria and fungi. Based on the promising results of artemisinin and the first generation derivatives (artesunate, artemether, arteether), novel drug development strategies have been pursued. These included the synthesis of acetal- and non-acetal-type artemisinin dimeric molecules as well as developing nanotechnological approaches, e.g. artemisinin-based liposomes, niosomes, micelles, solid lipid nanocarriers, nanostructured lipid carriers, nanoparticles, fullerenes and nanotubes. The current review presents an overview on different aspects of artemisinins, including sources, chemistry, biological/pharmacological properties, types of infectious pathogens that are susceptible to artemisinins in vitro and in vivo, in addition to the advancement in their drug delivery systems utilizing pharmaceutical technology. It would be expected that different therapeutic strategies based on the second and third generation artemisinin derivatives and artemisinin-based drug technologies would be available in the near future to treat specific infectious diseases. Abbreviations: ARM: Artemether; ARM-LNP: Artemether-loaded lipid nanoparticles; ART: Artemisinin; ACT: Artemisinin-based combination therapies; AC-PL: Artemisinin-curcumin-loaded PEGylated liposomes; ADPs: Artemisinin dimer piperazine derivatives; A-CL: Artemisinin-loaded conventional liposomes, artemisinin-curcumin-loaded; AST: Artesunate; BBB: Blood-brain barrier; AC-CL: Conventional liposomes; A-PL: artemisinin-loaded PEGylated liposomes; DHA: Dihydroartemisinin; %EE: Entrapment efficiency; GNO: Ground nut oil; kDNA: Kinetoplast; LNs: Lipid nanospheres; NPs: Liposomal nanoparticles; MRT: Mean residence times; MPEG: Methoxy polyethylene glycol; NP: Nanoparticle; NLC: Nanostructured lipid carrier; NCEs: New chemical entities; PSM: Plant secondary metabolites; SNL: Solid lipid nanovectors; TCM: Traditional Chinese Medicine; TR: Transferrin; TNBC: Triple negative breast cancer; VM: Vasculogenic mimicry Received 12 January 2016; Accept 3 May 2016

Objective: Digoxin is a therapeutic cardenolide widely used to treat various heart conditions such as atrial flutter, atrial fibrillation and heart failure in both Western as well as Chinese medicine. Digoxin is extracted from cultivated Digitalis lanata Ehrh. plants, known as Mao Hua Yang Di Huang in Chinese medicine. This manuscript presents two studies that were conducted to optimize the cultivation conditions for digoxin production in the TCM Mao Hua Yan Di Huang in a greenhouse under GAP conditions. Methods: Two experiments were designed in which 4 growth conditions were compared. Levels of digoxin, gitoxin, digitoxin, α-acetyl-digoxin, β-acetyl-digoxin were measured using HPLC-UV and compared between the conditions. Results: Normal soil, no CO₂ enrichment combined with a cold shock was found to be the optimal condition for producing digoxin in the first experiment. Gitoxin content was significantly lower in plants grown in this condition. Mechanical stress as well as the time of harvesting showed no statistically significant differences in the production of cardenolides. In the second experiment the optimal condition was found to be a combination of cold nights, sun screen, fertilizer use and no milled soil. Conclusion: This study shows that digoxin production can be increased by controlling the growth conditions of D. lanata Ehrh. The effect of cold was important in both experiments for improving digoxin production. Cultivating Chinese herbal medicines in optimized greenhouse conditions might be an economically attractive alternative to regular open air cultivation.

Background: The dried roots of Inula helenium L. (IH) and Inula racemosa Hook f. (IR) are used commonly as folk medicine under the name of “tumuxiang (TMX)”. Phenolic acid compounds and their derivatives, as main active constituents in IH and IR, exhibit prominent anti-inflammation effect. Objective: To develop a holistic method based on chemical characteristic and anti-inflammation effect for systematically evaluating the quality of twenty-seven TMX samples (including 18 IH samples and 9 IR samples) from different origins. Methods: HPLC fingerprints data of AL (Aucklandia lappa Decne.) whose dried root was similar with HR was added for classification analysis. The HPLC fingerprints of twenty-seven TMX samples and four AL samples were evaluated using hierarchical clustering analysis (HCA) and principle component analysis (PCA). The spectrum-efficacy model between HPLC fingerprints and anti-inflammatory activities was investigated by principal component regression (PCR) and partial least squares(PLS). Results: All samples were successfully divided into three main clusters and peaks 7, 9, 11, 22, 24 and 26 had a primary contribution to classify these medicinal herbs. The results were in accord with the appraisal results of herbs. The spectrum-efficacy relationship results indicated that citric acid, quinic acid, caffeic acid-β-D-glucopyranoside, chlorogenic acid, caffeic acid, 1,3-O-dicaffeoyl quinic acid, tianshic acid and 3p-Hydroxypterondontic acid had main contribution to anti-inflammatory activities. Conclusion: This comprehensive strategy was successfully used for identification of IH, IR and AL, which provided a reliable and adequate theoretical basis for the bioactivity relevant quality standards and studying the material basis of anti-inflammatory effect of TMX. Abbreviations: IH: Inula helenium L.; IR: Inula racemosa Hook f.; TMX: Tumuxiang; AL: Aucklandia lappa Decne.; HCA: Hierarchical clustering analysis; PCA: Principle component analysis; PCR: Principal component regression; PLS: Partial least squares; TCMs: Traditional Chinese Medicines; ChP 2015: Chinese Pharmacopoeia 2015; WHO: World health organization; FDA: Food and drug administration; HPLC-DAD: High-performance liquid chromatography-diode array detection; GC-MS: Gas chromatography-mass spectroscopy; HPLC-MS: High-performance liquid chromatography-mass spectroscopy; UPLC-MS: Ultra high-performance liquid chromatography-mass spectroscopy; RMSE: Root mean square error; RMSECV: Root mean square error of cross-validation; RRT: Relative retention time; RPA: Relative peak area; RSDs: Relative standard deviations

Safflower, Carthamus tinctorius L., is an annual oilseed crop that is cultivated on small plots all over the world. The seed oil content ranges from 20% to 45%; the oil is high in linoleic acid, an unsaturated fatty acid that aids in lowering the blood cholesterol level. Thus, safflower has long been used as medical plant in many countries, especially in China and India. However, for industrial purposes, it has long been neglected because of the low seed yield or oil content, until its physical role was revealed. In recent years, research works carried out in many countries mostly focused on improving the seed or oil yield. In this review, after illustrating the fatty acid composition of safflower seed oil as well as the genetic characteristics of safflower and their relationships with agronomic traits, a brief analysis of the current worldwide situation and future prospects of safflower utilization are presented.

Fibrosis is the remodeling and repair processes of chronic injuries. There are few effective therapies. Chinese medicine formula, the main pattern of traditional Chinese medicine (TCM) in clinic, applies a multi-component, multi-target and complicated approach in the treatment of diseases, and certainly shows good comprehensive therapeutic effects on fibrosis. In this review, the clinical study, effects and mechanism of action of Fuzheng Huayu recipe in the treatment of liver, pulmonary, and renal fibrosis was analyzed and evaluated. Meanwhile, based on the understanding of TCM pathogenesis for liver cirrhosis, this review will also briefly introduce the research of different classical Chinese medicine formulae with various functions in the treatment of experimental liver fibrosis induced by different methods, including comparing the efficacy, analyzing the action characteristics and mechanism of effective formulae, exploring pathological and biological basis of TCM diagnostic and therapeutic pattern, which will contribute to the research of TCM in the treatment of organ fibrosis. Abbreviations: Alb: albumin; EMT: epithelial-to-mesenchymal transition; TGF-β: transforming growth factor β; PI: phosphatidylinositol; TCM: traditional Chinese medicine; FZHY: Fuzheng Huayu; ALT: alanine aminotransferase; AST: aspartate aminotransferase; GGT: gamma-glutamyl transpeptidase; ALP: alkaline phosphatase; COPD: chronic obstructive pulmonary diseases; IL: interleukin; α-SMA: a-smooth muscle actin; TNF-a: tumor necrosis factor a; HgCl₂: mercuric chloride; RIF: renal interstitial fibrosis; UUO: unilateral ureteral obstruction; SCr: serum creatinine; BUN: blood urea nitrogen; Hyp: hydroxyproline; HA: hyaluronic acid; BDL: bile duct ligation; HGF: hepatocyte growth factor; Prdx6: peroxiredoxin 6; Hsp70: heat shock protein 70; SOD: superoxide dismutase; TIMP: tissue inhibitor of metalloproteinase; CD31: endothelial cell adhesion molecule-1; vWF: von Willebrand factor; VEGF: vascular endothelial growth factor; VEGFR2: vascular endothelial growth factor receptor-2; DAF: decay-accelerating factor; KCs: kupffer cells; MDA: malondialdehyde; HSP: heat shock protein; HO: heme oxygenase; GSH: glutathione; HIF-1a: hypoxia inducible factor-1a; EGFP: enhanced green fluoresenct protein

Objective: Essential oils are complex mixtures of chemical compounds, extracted from a wide range of plants. The volatile fraction of essential oils is responsible for their characteristic aroma and presents diverse biological properties that have been studied over the years. In Traditional Chinese Medicine, Piper nigrum is considered to be pungent and hot. Although its chemical constituents and respective pharmacological properties have been described by several authors, the volatile fraction is still underestimated as a therapeutic agent. The aim of this study was to evaluate the analgesic properties of the volatile fraction of Piper nigrum essential oil, in patients presenting different types of pain. Methods: Fifty-four patients presenting pain, were included in a randomized, double-blind, placebo-controlled study, over a 9-week period. The patients were randomly divided into two groups, and asked to inhale a vial containing Piper nigrum essential oil, or a vial containing a placebo (sesame oil), for 15 minutes. A numerical pain scale was applied before and after the inhalation. Results: Results showed a statistically significant decrease in pain intensity in the patients that inhaled the black pepper essential oil, while the placebo group patients showed no significant change in pain intensity. Conclusion: Although the results are preliminary due to the limited sample size and short inhalation time, the volatile fraction of the Piper nigrum essential showed promising results in reducing pain. In the Chinese medicine perspective, these results support the use of black pepper in different types of pain, since it warms the center and disperses cold.

Objective: To discuss mechanism of moxibustion (thermal stimulation) effect and best moxibustion stimulus parameter. Methods: Experiments were performed on 48 male Sprague-Dawley rats. Unit discharges from individual single neuron were recorded extracellularly with glass-microelectrode in Subnucleus Reticularis Dorsalis (SRD). Visceral-intrusive stimulation is done by colorectal distension. Thermal stimulation with different temperature (40°C, 42°C, 44°C, 46°C, 48°C, 50°C, 52°C) and different stimulus area (diameter of circle : 1.0 cm, 1.5 cm, 2.0 cm, 2.5 cm, 3.0 cm, 3.5 cm, 4.0cm) was applied around RN12 during nociceptive colorectal distension. Results: SRD neurons could be activated by visceral stimulation within noxious range. Under low temperature of stimulus, especially under 45°C of pain threshold to ordinary people, visceral nociceptive afferent facilitated thermal stimulus from the body surface. While after thermal stimulation reached a harmful degree, the thermal stimulus will inhibit visceral nociceptive afferent. Moreover, statistics show that the higher the temperature is, the smaller the size of stimulation area is needed, and they correlate with each other negatively. Conclusion: Visceral nociception could be inhibited by somatic thermal stimulation with specific parameter at medulla level. According to our finding, best thermal stimulation temperature is around 48°C and the best size of stimulation area is around 3.14-7.07cm² (with 2.0-3.0cm diameter).