Ear, External ; pathology ; Humans ; Keloid ; drug therapy ; Triamcinolone Acetonide ; therapeutic use ; Triterpenes ; therapeutic use

Xuanfu Daizhe Decoction, first seen in Zhang Zhongjing's Treatise on Cold Damage Diseases, was composed of seven medicinal materials: Inulae Flos, Glycyrrhizae Radix, Ginseng Radix, Zingiberis Rhizoma Recens, Haematitum, Pinelliae Rhizoma and Jujubae Fructus. It was used to treat gastric fullness and hardness and belching due to the wrong treatment of typhoid fever and sweating. With detailed records and description in ancient medical books, Xuanfu Daizhe Decoction was widely adopted in clinical practice by physicians of later generations, which expanded its main therapeutic functions. By comprehensive collation of ancient and modern literature on Xuanfu Daizhe Decoction, this paper systematically explored the historical evolution of the prescription from the source, composition, dosage, processing, clinical application, function interpretation and decocting method. It was found that the composition and processing method of the prescription in the past dynasties were relatively consistent, and there was a gradual decrease in dosage in clinical application. In ancient times, Xuanfu Daizhe Decoction was mainly used to treat nausea, vomiting, hiccups, constipation, etc., while modern clinicians mainly used it for digestive diseases such as reflux esophagitis and gastritis. Through the analysis and textual research, the composition, dosage, processing, function evolution and decocting method of this prescription were determined, which provided reference for the research and development of compound preparations of Xuanfu Daizhe Decoction.
Drugs, Chinese Herbal/therapeutic use* ; Medicine, Chinese Traditional ; Plant Extracts ; Rhizome ; Triterpenes

OBJECTIVETo research the microemulsion preparation of Ganoderma lucidum polysaccharides and triterpenes and investigate its properities. Evaluate the effects of polysaccharides and triterpenes microemulsions against transplant tumor growth.

METHODThe microemulsion formula was optimized by constructing the pseudo-ternary phase diagrams of blank microemulsion. The polysaccharides and triterpenes microemulsions were prepared on the blank microemulsions. The appearance, particle distribution and Zeta potential were investigated by transmission electron microscope and grain size analyzer. The Heps mice were randomly administered with polysaccharides and triterpenes microemulsions (114.5, 57.25 mg x kg(-1) x d(-1)) for 7 days. The effectiveness was assessed based on tumor inhibitory ratio of mice with Heps tumors. The toxicity was evaluated by measurements of the mice weight, immune organ weight.

RESULTThe optimal microemulsion formula was composed of tween 20, dimethyl carbinol, water and 9-octadecenoic acid with the ratio of 14.3: 14.3: 33. 3:2. Polysaccharides and triterpenes microemulsions in transmission electron microscope were consisted of small spherical drop. The average particle size was 32.43 nm and the Zeta potential was -3.41 mV. The polysaccharides and triterpenes microemulsions showed an inhibition rate of 37.66% (57.25 mg x kg(-1) x d(-1)) and 52.34% (114.5 mg x kg(-1) x d(-1)) respectively against Heps tumor growth.

CONCLUSIONThe acquired microemulsion with small particle size is stable. It significantly inhibits the tumor growth in Heps mice.

Animals ; Antineoplastic Agents, Phytogenic ; therapeutic use ; Emulsions ; Female ; Liver Neoplasms, Experimental ; drug therapy ; Male ; Mice ; Neoplasm Transplantation ; Particle Size ; Polysaccharides ; therapeutic use ; Reishi ; chemistry ; Triterpenes ; therapeutic use

OBJECTIVETo study the protective mechanisms of the astragaloside against ischemia-reperfusion lung injury in rats.

METHODSIschemia-reperfusion lung injury was induced in SD rats. Astragalus armour glucoside was dissolved in 1% of sodium carboxymethyl cellulose at different concentrations (8, 6, and 3 mg/ml) was intragastrically administered in the rats at the dose of 1 ml/100 g. Cellular and subcellular structural changes in the lung tissue were observed at the end of the experiment using optical and transmission electron microscope, with the wet/dry ratio of the lung tissue and myeloperoxidase (MPO) activity measured.

RESULTSThe wet/dry ratio and myeloperoxidase activity in the lung tissue were significantly higher in the model group than in the sham-operated group (P<0.05), and were significantly lowered by the treatment with astragalus armour glucoside at different doses (P<0.01 or 0.05), and the effect was especially obvious in rats receiving a moderate dose. Pulmonary capillary expansion, erythrocyte leakage and exudate in the alveolar space with obvious pathological changes in the type I and II epithelial cells were observed in model group. Pulmonary capillary expansion was reduced in rats treated with high, medium and low dose of Astragalus armour glucoside, and the medium dose group showed the most obvious effect, in which no edema fluid in the alveolar space or erythrocyte leakage was found with also reduced type II lung epithelial cell degranulation.

CONCLUSIONAstragaloside has obvious antioxidant effect in rats with ischemia-reperfusion lung injury, and a medium dose produces the best effect.

Animals ; Female ; Ischemic Preconditioning ; Lung ; drug effects ; pathology ; Male ; Phytotherapy ; Rats ; Rats, Sprague-Dawley ; Reperfusion Injury ; drug therapy ; pathology ; Saponins ; pharmacology ; therapeutic use ; Triterpenes ; pharmacology ; therapeutic use

Inonotus obliquus has high nutritional and medicinal value, especially in treating malignant tumors, diabetes, cardiovascular disease and AIDS, attracting significant attention from scholars in recent years. In this paper, the biological characteristics, chemical composition and pharmacologic effects of Inonotus obliquus were summarized. And the applications in medicine and food were introduced. Future research on Inonotus obliquus was also discussed in order to make Inonotus obliquus obtain effective exploitation and satisfy people's demands.
Anti-Inflammatory Agents ; chemistry ; pharmacology ; therapeutic use ; Antineoplastic Agents ; chemistry ; pharmacology ; therapeutic use ; Antioxidants ; chemistry ; pharmacology ; therapeutic use ; Antiviral Agents ; chemistry ; pharmacology ; therapeutic use ; Basidiomycota ; chemistry ; Biomedical Research ; trends ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; therapeutic use ; Humans ; Hypoglycemic Agents ; chemistry ; pharmacology ; therapeutic use ; Platelet Aggregation Inhibitors ; chemistry ; pharmacology ; therapeutic use ; Triterpenes ; chemistry ; isolation & purification

Platycodon grandiflorum, as the traditional Chinese medicine, has been employed for dispersing the lung and resolving phlegm soothing the throat, and promoting pus discharge in ancient days. Triterpenoids are its main effective constituents which have dominant activities on antitussive, expectorant, antitumor, antioxidant and immune enhancement. This paper has mainly reviewed the progress of P. grandiflorum on the processing in planting area, chemical constituents, quality standard, pharmacological effects and clinical application in recent ten years, which has provided the important references for its further study, exploitation and application.
Animals ; Cough ; drug therapy ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; therapeutic use ; Humans ; Molecular Structure ; Pharyngitis ; drug therapy ; Phytotherapy ; methods ; trends ; Platycodon ; chemistry ; Saponins ; chemistry ; isolation & purification ; therapeutic use ; Triterpenes ; chemistry ; isolation & purification ; therapeutic use

Ursolic acid (UA) is a sort of pentacyclic triterpenoid carboxylic acid purified from natural plant. UA has a series of biological effects such as sedative, anti-inflammatory, anti-bacterial, anti-diabetic, antiulcer, etc. It is discovered that UA has a broad-spectrum anti-tumor effect in recent years, which has attracted more and more scholars' attention. This review explained anti-tumor actions of UA, including (1) the protection of cells' DNA from different damages; (2) the anti-tumor cell proliferation by the inhibition of epidermal growth factor receptor/mitogen-activated protein kinase signal or of FoxM1 transcription factors, respectively; (3) antiangiogenesis, (4) the immunological surveillance to tumors; (5) the inhibition of tumor cell migration and invasion; (6) the effect of UA on caspase, cytochromes C, nuclear factor kappa B, cyclooxygenase, tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) or mammalian target of rapamycin signal to induce tumor cell apoptosis respectively, and etc. Moreover, UA has selective toxicity to tumor cells, basically no effect on normal cells. With further studies, UA would be one of the potential anti-tumor agents.
Angiogenesis Inhibitors ; pharmacology ; therapeutic use ; Animals ; Antineoplastic Agents, Phytogenic ; chemistry ; pharmacology ; therapeutic use ; Apoptosis ; drug effects ; Humans ; Immunologic Surveillance ; drug effects ; Neoplasms ; blood supply ; drug therapy ; immunology ; pathology ; Triterpenes ; chemistry ; pharmacology ; therapeutic use

OBJECTIVE: To investigate the effects of astragaloside Ⅳ (AS-Ⅳ) on microglia/macrophage M1/M2 polarization and inflammatory response after cerebral ischemia in rats. METHODS: Forty eight male SD rats were randomly divided into sham operation control group, model control group and AS-Ⅳ group with 16 rats in each. Focal cerebral ischemia model was induced by occlusion of the right middle cerebral artery (MCAO) using the intraluminal filament. After ischemia induced, the rats in AS-Ⅳ group were intraperitoneally injected with 40 mg/kg AS-Ⅳ once a day for 3 days. The neurological functions were evaluated by the modified neurological severity score (mNSS) and the corner test on d1 and d3 after modelling. The infarct volume was measured by 2, 3, 5-triphenyl tetrazolium chloride (TTC) staining on d3 after ischemia. The expression of M1 microglia/macrophage markers CD86, inducible nitric oxide synthase (iNOS) and pro-inflammatory factors TNF-α, IL-1β, IL-6, M2 microglia/macrophages markers CD206, arginase-1 (Arg-1), chitinase-like protein (YM1/2) and anti-inflammatory factors interleukin-10 (IL-10) and transforming growth factor beta (TGF-β) was detected by real-time RT-PCR. The expression of CD16/32/Iba1 and CD206/Iba1 was determined by double labeling immunefluorescence method in the peripheral area of cerebral ischemia. RESULTS: Compared with model control group, AS-Ⅳ treatment improved neurological function recovery and reduced infarct volume after ischemia ( CONCLUSIONS The findings suggest that AS-Ⅳ ameliorates brain injury after cerebral ischemia in rats, which may be related to inhibiting inflammation through promoting the polarization of the microglia/macrophage from M1 to M2 phenotype in the ischemic brain.
Animals ; Anti-Inflammatory Agents/therapeutic use* ; Brain Ischemia/drug therapy* ; Cell Polarity/drug effects* ; Inflammation/drug therapy* ; Macrophages/drug effects* ; Male ; Microglia/drug effects* ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Saponins/therapeutic use* ; Triterpenes/therapeutic use*

More than 25 dammarane-type tetracyclic triterpenoid saponins have been isolated from ginseng, the root and rhizome of Panax ginseng C.A. Meyer (Araliaceae). The genuine sapogenins of those saponins, 20(S)-protopanaxa-diol and -triol, were identified as 20(S) 12beta-hydroxy-and 20(S) 6alpha,12beta-dihydroxy-dammarenediol-II, respectively. There are two types of preparations from ginseng: white ginseng prepared by drying after peelling off and red ginseng prepared by steaming and drying. Some partly deglycosylated saponins such as ginsenoside Rh-1, Rh-2, and Rg-3 are obtained from red ginseng as artifacts produced during steaming. Several workers studied the metabolic transformation by human intestinal bacteria after oral administration of ginsenoside Rb-1 and Rb-2 and found that the stepwise deglyco-sylation yielded compound K and finally 20(S)-protopanaxadiol. Ginsenoside Rg-1 was converted into 20(S)-protopanaxatriol via ginsenoside Rh-1. Yun et al. in Korea conducted the epidemiological case-control studies of ginseng and suggested its cancer preventing activities. Kitagawa et al. demonstrated in vitro that ginsenosides, especially 20(R)-ginsenoside Rg-3, specifically inhibited cancer cell invasion and metastasis. Azuma et al. found that ginsenoside Rb-2 inhibited tumor angiogenesis, and Kikuchi et al. reported that ginsenoside Rh-2 inhibited the human ovarian cancer growth in nude mice. Recently, ginsenoside Rg-3 was produced as an anti-angiogenic anti-cancer drug in China. The aforementioned reports suggest that less glycosylated protopanaxadiol derivatives are effective in cancer prevention. Apart from Ginseng tetracyclic triterpenoid saponins, some oleanane-type pentacyclic triterpenoid compounds showed the anti-carcinogenic activity in the two-stage anti-cancer-promotion experiments in vitro and in vivo.
Animal ; Antineoplastic Agents, Phytogenic/*therapeutic use ; Human ; Molecular Structure ; Neoplasms/*prevention & control ; *Panax/chemistry ; Sapogenins/chemistry ; Saponins/chemistry/isolation & purification/metabolism/*pharmacology ; Triterpenes/chemistry/*pharmacology

The ethyl acetate fraction of ethanol extract of Eucommiae Cortex can effectively inhibit joint inflammation and bone destruction in rats with collagen-induced arthritis(CIA) and has a potential therapeutic effect on rheumatoid arthritis. The triterpenoid(EU-Tid) and iridoid(EU-Idd) of Eucommiae Cortex are derivatives isolated from the ethyl acetate fraction of the ethanol extract of Eucommiae Cortex, and it is not clear whether they have inhibitory effects on joint inflammation and bone erosion in CIA rats. Therefore, based on the CIA model, the effects of EU-Tid, EU-Idd, and their combination(EU-TP) on arthritis in rats were observed, and the material basis of Eucommiae Cortex against arthritis was further clarified. The samples were collected two and four weeks after administration to observe the pathological changes in different stages of arthritis in CIA rats. For the rats in the model control group, with the prolongation of the disease course, the paw volume and arthritis score increased and histopathological lesions aggravated. Compared with the model control group, the drug administration groups showed reduced paw volumes and arthritis scores, and improved joint lesions and cartilage destruction. Additionally, the mRNA expression levels of tumor necrosis factor-α(TNF-α), interleukin-17(IL-17), and interleukin-23(IL-23) in the spleen were down-regulated in the drug administration groups. EU-TP and EU-Tid at concentrations of 160 and 320 μg·mL~(-1) could significantly inhibit the proliferation of human fibroblast-like synoviocytes-RA(HFLS-RA) and nitric oxide(NO) release in the supernatant of RAW264.7 cells induced by lipopolysaccharide(LPS) at the concentration range of 10-80 μg·mL~(-1) in vitro. EU-Idd had no effect on the proliferation of HFLS-RA but could reduce the NO release at concentrations of 40 and 80 μg·mL~(-1). The results indicated that the terpenoids of Eucommiae Cortex had great potential in the treatment of rheumatoid arthritis.
Rats ; Humans ; Animals ; Arthritis, Experimental/drug therapy* ; Iridoids/pharmacology* ; Triterpenes/therapeutic use* ; Arthritis, Rheumatoid/drug therapy* ; Tumor Necrosis Factor-alpha ; Plant Extracts/pharmacology* ; Inflammation/drug therapy* ; Ethanol ; Cytokines