Phytosomes: an effective approach to enhance the oral bioavailability of active constituents extracted from plants

Many active constituents from herbal plants have well-established pharmacological effects in vitro. But they demonstrate less or no activities in vivo due to various problems of themselves, which severely restricts their clinical applications. After forming phytosomes with phospholipids in aprotic solvent, the active constituents exhibit different physicochemical properties from the free form. In particular, the bioavailability of the active constituent-phytosomes is enhanced greatly due to the improved capacity to cross the biomembrane and reach circulation. Therefore, increasing attention has been attracted to the use of phytosomes in recent years. Based on the published reports, we reviewed the recent progress in the research of phytosomes including preparation, characterization, structure verification and clinical applications.

Plant Tissue Culture and Biosynthesis Provide a Fast Way to Produce Active Constituents of Traditional Chinese Medicines

The plant kingdom has provided literally thousands of natural products with widely diverse chemical structures and a vast array of biological activities.Many of them have seen subsequent application in discovery of new druids and the pharmaceutical industry and clinical therapeutic application.

Improvement of (Eruca sativa Mill) yield, oil, chemical constituents and antioxidant activity utilizing a by-product of yeast production (CMS) with zinc and boron under salinity stress conditions

The impact of low-quality irrigation water on plant development has garnered significant attention from researchers. In light of this, two field experiments were conducted to evaluate the performance, yield, oil production and composition, as well as active constituents of Rocket(Eruca sativa Mill) cultivated in calcareous soil under saline water irrigation. Foliar sprays containing condensed molasses soluble(CMS), zinc(Zn), and boron(B) alone or in combination were used for irrigation. The data obtained from measuring various parameters of Rocket following foliar spraying with CMS, Zn, B or their combinations demonstrated that most treatments resulted in a significant increase in these parameters. The highest values for most measurements were observed when foliar application included all three components(CMS + Zn + B), resulting in a seed yield of 184.6 g/m2and an oil content of 675.3 kg/ha. Compared to the control group, the macronutrient content of N, P, K, Mg, and Ca increased by 34.4%, 56%, 42%, 45%, and 39% respectively in the seeds treated with these components.Furthermore, carbohydrates, proteins, phenolics flavonoids, and antioxidants showed increases of 24%, 34%,21%, 43%, and 28% respectively compared to the control group. Gas-liquid chromatography analysis identified ten components present in the seed oil characterized by higher unsaturated fatty acids ranging from 81.28% to92.28% and lower saturated fatty acids ranging from 6.72% to 8.21%. Therefore, foliar spray application including CMS, zinc, and boron can help alleviate salinity effects on Rocket plants grown under saline water irrigation conditions while improving growth, yield, oil production, and nutritional content such as total carbohydrates, proteins, and macronutrients levels.

Advances in Pharmacological Research on Active Components of Traditional Chinese Medicine in the Treatment of Inflammatory Bowel Disease-related Bowel Cancer

In recent years,with the modern development of traditional medicine,the research on the treatment of inflammatory bowel disease and bowel cancer is increasingly deep.This paper reviews the pharmacological research progress of flavonoids,alkaloids,polyphenols,polysaccharides,steroids and saponins in the treatment of inflammatory bowel disease and canceration.

Study on the Mechanism of Atractylodes lancea in the Treatment of Diabetes Based on Network Pharmacology

[Objectives]To predict the mechanism of Atractylodes lancea in the treatment of diabetes by using the method of network pharmacology.[Methods]The active constituents of A.lancea were mined and their action targets were predicted by using TCMSP database,and the targets of diabetes were screened out by GeneCards,and OMIM databases.The"constituent-target-pathway-disease"network of A.lancea in the treatment of diabetes was constructed by using Cytoscape software.The target protein-related interaction network was constructed by STRING database,and the biological function annotation and pathway analysis of key targets were carried out.[Results]The 4 active constituents of A.lancea could treat diabetes by intervening in 47 targets,95 GO biological processes and 116 main biological pathways.[Conclusions]The wogonin,NSC63551,3β-acetoxy atractylone andβ-carotene in A.lancea may regulate nuclear receptor activity,transcription factor activity(directly bind to the ligand-regulated sequence-specific DNA),steroid receptor,G protein-coupled amine receptor activity,sodium-chloride transporter activity,neurotransmitter receptor activity and other pharmacological effects,by mediating AGE-RAGE pathway,IL-17 pathway,PI3K-Akt pathway,p53 pathway,etc.,so as to treat diabetes.

Chemical profile of the active fraction of Yi-Gan San by HPLC–DAD–Q-TOF–MS and its neuroprotective effect against glutamate-induced cytotoxicity

Yi-Gan San(YGS), a traditional Chinese medicine for dementia-related symptoms, was previously fractionated. One active fraction, YGS40 exhibited a neuroprotective effect against glutamate-induced cytotoxicity. In the present study, high-performance liquid chromatography, coupled with diode-array detection and quadrupole time-of-flight mass spectrometry, was applied for the identification of its chemical constituents and for quantification studies. The chemical profile of YGS40 consisted of sixty-four identified or tentatively characterized compounds. The levels of the major marker compounds increased significantly in the mixed decoction compared with those in the single plant decoction. The results suggest the high precision of the analyses of most of the constituents in YGS40 and establish the quantitative variations of the major marker compounds between the single and mixed decoction processes.

PROSTATE CANCER BONE-METASTASIS IS INHIBITEDBY CELASTROL, AN ACTIVE CONSTITUENT OF TRIPTERYGIUM WILFORDII HOOK.F.(雷公藤)

Prostate cancer(PCa)is one of the most common malignant tumours and a leading cause of cancer deaths.Treatment failure of PCa is often due to bone-metastasis.Celastrol,an active constituent of the roots of Tripterygium wilfordii,has shown antitumour effects in previous studies in accordance with its use in TCM.Here we report for the first time an in-depth study of the effects of celastrol on

Chemical composition and pharmacological properties of Flos sophorae immaturus, Flos sophorae and Fructus sophorae: a review

The flower buds and fruits of Sophora japonica are known as Flos sophorae immaturus(Chinese Huaimi,FSI),Flos sophorae(Chinese Huaihua,FLS)and Fructus sophorae(Chinese Huaijiao,FRS)due to their different physiological forms.FSI and FLS are precious resources of homology of medicine and food,while FRS is a valuable Chinese herb,and all of which have been used for thousands of years.There are great differences in the active ingredients,functions and toxicological properties of FSI,FLS and FRS.However,they are often confused and assumed to have fairly similar validity,which is detrimental to their precision development of resources of homology of medicine and food.This review summarized the active constituents,analytical techniques and pharmacological properties of FSI,FLS and FRS,then systematically compared their differences.The article will help people better understand and distinguish the differences and characteristics of FSI,FLS and FRS in bioactive constituents,content of functional components and pharmacological properties,which can contribute to their highly efficient targeted applications in the future food and medical fields.

Immunological Activities of Components from Leaves of Liriodendron chinensis

Objectives To investigate the anti-inflammatory components from the leaves of Liriodendron chinensis. Methods The 95% alcohol extract from the leaves of L. chinensis was subjected to column chromatography, and the structures of purified compounds were determined by spectral methods. The bioassay was performed through the inhibitory effects on the inflammatory cells activated by lipopolysaccharide （LPS）. Results Nine compounds were isolated, including octacosanoic acid （1）, stearic acid （2）, （2R-2-hydroxy-N-[（2S,3S,4R,8E- l ,3,4-tri-hydroxyicos-8-en- 2-yl]tetracosanamide （3）, （2 R）- 2- hyd roxy- N- [（2 S, 3 S,4 R,8 E）- 1 - O-β- D-glucopyranosyloxy-3,4-dihydroxy- octadec-8-en-2-yl]eicosanamide （4）, （2R）-2-hydroxy-N-[（2S,3S,4R,8E）-l-O-β-D- glucopyranosyloxy-3,4-dihydroxyoctadec-8-en-2-yl]hexadecanamide （5）, dicentrinone （6）, liriodenine （7）, daucosterol （8）, and liriodendritol （9） and among which five compounds could significantly lower the content of nitric oxide （NO） from peritoneal macrophages of rats induced by LPS and reduce the splenic lymphocyte proliferation in mice. This is the first report on the occurrence of ceramides and dicentrinone in the plants of Liriodendron Linn. Conclusion The five compounds are likely to be anti-inflammatory compounds concerning to their pronounced inhibitory action on the activated inflammatory cells. This assessment might provide a basis for searching the potent active compounds used for the treatment of inflammation.

Chinmedomics:Newer Theory and Application

The scientific interpretation of the effectiveness of traditional Chinese medicine（TCM） is a communication channel between Chinese medicine and modern medicine. The evaluation of TCM efficacy is an important prerequisite for discovering active constituents. Therefore, there is an urgent need to establish a biological language for scientific explanation of the effectiveness of TCM, and modern scientists can further accept the significant value of TCM theory and its clinical practice. The syndrome and corresponding formulation are two important parts in TCM, and they are directly related to the effectiveness of TCM. Our team has taken syndrome and formulation as the research objects, integrated serum pharm-chemistry of TCM with metabolomics technology, developed a new platform termed Chinmedomics, which is capable of evaluating effectiveness of TCM and discovering the syndrome biomarkers as well as the effective substances. The correlation between the endogenous biomarkers of syndrome and exogenous constituents of formulation is analyzed to find the highly associated compounds as the effective substances, and further clarifying their activities, and may discover lead compounds. This effective strategy could speed the drug discovery from natural resources. This article systematically introduced the establishment and application of Chinmedomics theory, in order to provide references for studies on TCM, and some characteristic examples are presented to highlight the application of this new strategy for discovering the potential active constituents of TCM.

Pharmacokinetics Applications of Traditional Chinese Medicines

Traditional Chinese medicine(TCM) has been widely used in many oriental countries for thousands of years and played an indispensable role in the prevention and treatment of diseases, especially the complicated and chronic ones. It is a very complex mixture containing hundreds or thousands of different components. Pharmacokinetic study on active constituents in TCM preparations is a good way for us to explain and predict a variety of events related to the efficacy and toxicity of TCM. In the drug discovery phases, pharmacokinetics is a key to guide medicinal chemists in the optimization process of a chemical series and to assist pharmacologists to design in vivo studies.To explore the potentially bioactive components in TCM, it is necessary to further study the in vivo pharmacokinetic characteristics of multiple absorbed components and find out the optical time-course behavior to providing more substantial research for new leads in drug discovery. Pharmacokinetics screening method could provide a reliable means of prospecting natural products in the search for new leads in drug discovery. This review summarizes the research progress of PK on TCM in the search for suitable lead compounds in recent years.

Herbal Medicine in Ischemic Stroke:Challenges and Prospective

Herbal medicines, mainly of plant source, are invaluable source for the discovery of new therapeutic agents for all sorts of human ailments. The complex pathogenesis of stroke and multifactorial effect of herbal medicine and their active constituents may suggest the promising future of natural medicine for stroke treatment. Anti-oxidant, anti-inflammatory, anti-apoptotic, neuroprotective and vascular protective effect of herbal medicines are believed to be efficacious in stroke treatment. Herbs typically have fewer reported side effects than allopathic medicine, and may be safer to use over longer period of time. Herbal medicines are believed to be more effective for the longstanding health complaints, such as stroke. Several medicinal plants and their active constituents show the promising results in laboratory research. However failure in transformation of laboratory animal research to the clinical trials has created huge challenge for the use of herbal medicine in stroke. Until and unless scientifically comprehensive evidence of the efficacy and safety of herbal medicine in ischemic stroke patients is available, efforts should be made to continue implementing treatment strategies of proven effectiveness. More consideration should be paid to natural compounds that can have extensive therapeutic time windows, perfect pharmacological targets with few side effects. Herbal medicine has excellent prospective for the treatment of ischemic stroke, but a lot of effort should be invested to transform the success of animal research to human use.