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1.
Environ Sci Pollut Res Int ; 30(42): 95875-95891, 2023 Sep.
Article in English | MEDLINE | ID: mdl-37561306

ABSTRACT

The wastewater discharged from crude oil storage tanks (WCOST) contains high concentrations of salt and metal iron ions, and high chemical oxygen demand (COD). It belongs to "3-high" wastewater, which is difficult for purification. In this study, WCOST treatments were comparatively investigated via an advanced pretreatment and the traditional coagulation-microfiltration (CMF) processes. After WCOST was purified through the conventional CMF process, fouling occurred in the microfiltration (MF) membrane, which is rather harmful to the following reverse osmosis (RO) membrane unit, and the effluent featured high COD and UV254 values. The analysis confirmed that the MF fouling was due to the oxidation of ferrous ions, and the high COD and UV254 values were mainly attributable to the organic compounds with small molecular sizes, including aromatic-like and fulvic-like compounds. After the pretreatment of the advanced process consisting of aeration, manganese sand filtration, and activated carbon adsorption in combination with CMF process, the removal efficiencies of organic matter and total iron ions reached 97.3% and 99.8%, respectively. All the water indexes of the effluent, after treatment by the advanced multi-unit process, meet well the corresponding standard. The advanced pretreatment process reported herein displayed a great potential for alleviating the MF membrane fouling and enhanced the lifetime of the RO membrane system in the 3-high WCOST treatment.


Subject(s)
Petroleum , Water Purification , Wastewater , Waste Disposal, Fluid , Petroleum/analysis , Filtration , Ions/analysis , Iron/analysis , Osmosis , Membranes, Artificial
2.
Res Sq ; 2023 Jul 10.
Article in English | MEDLINE | ID: mdl-37502961

ABSTRACT

The uptake of Ca2+ into and extrusion of calcium from the mitochondrial matrix, regulated by the mitochondrial Ca2+ uniporter (MCU), is a fundamental biological process that has crucial impacts on cellular metabolism, signaling, growth and survival. Herein, we report that the embryonic lethality of Mcu-deficient mice is fully rescued by orally supplementing ferroptosis inhibitor lipophilic antioxidant vitamin E and ubiquinol. Mechanistically, we found MCU promotes acetyl-CoA-mediated GPX4 acetylation at K90 residue, and K90R mutation impaired the GPX4 enzymatic activity, a step that is crucial for ferroptosis. Structural analysis supports the possibility that GPX4 K90R mutation alters the conformational state of the molecule, resulting in disruption of a salt bridge formation with D23, which was confirmed by mutagenesis studies. Finally, we report that deletion of MCU in cancer cells caused a marked reduction in tumor growth in multiple cancer models. In summary, our study provides a first direct link between mitochondrial calcium level and sustained GPX4 enzymatic activity to regulate ferroptosis, which consequently protects cancer cells from ferroptosis.

3.
Phytother Res ; 36(4): 1692-1707, 2022 Apr.
Article in English | MEDLINE | ID: mdl-35129872

ABSTRACT

Rhamnazin (RN) is a flavonol isolated from the calyxes and fruits of Physalis alkekengi L. var. franchetii (Mast.) Makino, which has been used for treating pulmonary diseases in traditional Chinese medicine. The nuclear factor erythroid 2-related factor 2 (Nrf2) is a therapeutic target for pulmonary diseases. In the present study, the underlying mechanism and pharmacological effect of RN against pulmonary disorders are investigated. Human lung epithelial Beas-2B cell and RAW 264.7 murine macrophage-based cell models, and a cigarette smoke (CS)-induced pulmonary impairment mice model are adopted for investigation in vitro and in vivo. RN is identified to be an Nrf2 activator, which promotes Nrf2 dissociation from Keap1 via reacting with the Cys151 cysteine residue of Keap1, and suppresses Nrf2 ubiquitination. In addition, RN is able to attenuate toxicant-stimulated oxidative stress and inflammatory response in vitro. Importantly, RN significantly relieves CS-induced oxidative insult and inflammation, and RN-induced inhibition of inflammation is related to inhibition of nuclear transcription factor-κB (NF-κB) and induction of cell autophagy. In conclusion, our data indicate that RN is an activator of the Nrf2 pathway and evidently alleviates pulmonary disorders via restricting NF-κB activation and promoting autophagy. RN is a promising candidate for the therapy of pulmonary disorders.


Subject(s)
Lung Diseases , Physalis , Animals , Flavonoids , Flavonols , Inflammation , Kelch-Like ECH-Associated Protein 1/metabolism , Mice , NF-E2-Related Factor 2/metabolism , NF-kappa B/metabolism , Oxidative Stress , Physalis/chemistry , Physalis/metabolism
4.
Chin J Integr Med ; 27(7): 520-526, 2021 Jul.
Article in English | MEDLINE | ID: mdl-33170941

ABSTRACT

OBJECTIVE: To investigate the effects of matrine on antigen presentation of dendritic cells (DCs), and to explore the pharmacological mechanism of matrine on anti-tumor effect. METHODS: Different concentrations (0, 1, 2, 4, 8 and 16 µ g/mL) of matrine were co-cultured with DCs, the harvested DCs were co-cultured with antigens of Lewis lung cancer (LLC) cells, and then DCs and T cells were co-cultured to produce DCs-activated killer (DAK) cells, which have significant tumor-killing activity. The expression of cytokines, mRNA and protein of toll-like receptors (TLRs) in DCs were detected by enzyme linked immunosobent assay, polymerase chain reaction and Western blot, respectively. And the killing effect of DAK were measured by MTT assay. RESULTS: Matrine significantly increased the mRNA expression of TLR7, TLR8, myeloid differentiation factor 88 (MyD88), tumor necrosis factor receptor-associated factor 6 (TRAF-6) and I κ B kinase (IKK), as well as the protein expression of TLR7 and TLR8, and up-regulated the levels of interleukin-12 (IL-12), IL-6 and tumor necrosis factor-α (TNF-α), meanwhile, it also increased the expressions of MHC-II, CD54, CD80 and CD86 in DCs. DCs-activated effector T cells had significant tumor-killing activity. When the concentration of matrine was more than 4 µg/mL, all indices had significant difference (P<0.01 or P<0.05). CONCLUSION: Matrine plays an anti-tumor role by regulating TLRs signal transduction pathway, promoting the secretion of inflammatory cytokines and enhancing immune function.


Subject(s)
Alkaloids , Dendritic Cells , Alkaloids/pharmacology , B7-1 Antigen , Cells, Cultured , Cytokines , Quinolizines/pharmacology , Matrines
5.
J Nanobiotechnology ; 18(1): 138, 2020 Sep 29.
Article in English | MEDLINE | ID: mdl-32993684

ABSTRACT

BACKGROUND: Neutrophil-based drug delivery system possesses excellent advantages in targeting at tumour because neutrophils are easily recruited by chemotactic factor in tumor microenvironment. Herein, we developed a novel tactic of multistage neutrophils-based nanoparticle delivery system for promoting photothermal therapy (PTT) of lung cancer. RESULTS: Au nanorod (AuNR) was successfully modified with bovine serum albumin (AuNRB) and further conjugated with RGD (AuNRBR), followed by neutrophil internalisation to obtain neutrophils-based delivery system (AuNRBR/N). The engineered neutrophils efficiently migrated across the epithelial cells due to inflammatory signal. They exhibited better toxicity against Lewis cells with laser irradiation in vitro. Moreover, AuNRBR/N showed significantly more targetability to tumour tissue compared with cell carrier-free AuNRBR, as demonstrated in Lewis tumour-bearing mice. The enhanced tumour homing efficiency of AuNRBR/N together with subsequently released AuNRBR from the neutrophils was favourable for further deep tissue diffusion and contributed to the inhibition of the tumour growth in PTT and improved survival rate (over 120 days). CONCLUSIONS: Overall results illustrated that the design of cell-based nanoparticle delivery system for PTT of cancer is promising.


Subject(s)
Drug Delivery Systems/methods , Nanoparticles/therapeutic use , Neutrophils/drug effects , Photothermal Therapy/methods , Animals , Cell Line, Tumor , Combined Modality Therapy , Female , Gold/pharmacology , Humans , Mice , Mice, Inbred C57BL , Nanotubes , Photochemotherapy/methods , Phototherapy , Survival Rate
6.
Planta Med ; 86(16): 1191-1203, 2020 Nov.
Article in English | MEDLINE | ID: mdl-32668478

ABSTRACT

Physalis Calyx seu Fructus, a traditional Chinese medicine consisting of the calyxes and fruits of Physalis alkekengi var. franchetii, has been used as therapy for inflammation-related respiratory diseases such as excessive phlegm, cough, sore throat, and pharyngitis for a long history in China. The aim of the present study was to investigate the chemical constituents of Physalis Calyx seu Fructus and identify the bioactive constituents responsible for its traditional application as therapy for inflammation-related diseases. In the present study, one new phenylpropanoid (1: ), two new steroids (17: and 18: ), together with 55 known constituents have been purified from the EtOH extract of Physalis Calyx seu Fructus. Among them, seven and twelve known constituents were isolated for the first time from Physalis Calyx seu Fructus and the genus Physalis, respectively. Fourteen constituents, including steroids [physalins (5:  - 9, 12:  - 14: , and 15: ) and ergostane (21: )], a sesquiterpenoid (35: ), alkaloids (36: and 37: ), and a flavonoid (44: ), showed inhibitory effects against oxidative stress. Ten constituents, including steroids (5, 6, 8, 13: , and 15: ), sesquiterpenoids (34: and 35: ), alkaloids (37: and 41: ), and a flavonoid (43: ), were found be potential anti-inflammatory constituents of this medicinal plant. The inhibition of oxidative stress and inflammatory response may be related to the regulation of Nrf2 and nuclear factor-κB pathways. The ethnomedical use of Physalis Calyx seu Fructus as a treatment for respiratory diseases might be attributed to the combined inhibitory effects of steroids, alkaloids, sesquiterpenoids, and flavonoids against oxidative stress and inflammatory response.


Subject(s)
Physalis , China , Flowers , Fruit , Oxidative Stress
7.
Anticancer Agents Med Chem ; 20(10): 1241-1249, 2020.
Article in English | MEDLINE | ID: mdl-32116205

ABSTRACT

BACKGROUND: Rabdosia japonica has been historically used in China as a popular folk medicine for the treatment of cancer, hepatitis, and gastricism. Glaucocalyxin A (GLA), an ent-kaurene diterpene isolated from Rabdosia japonica, is one of the main active ingredients showing potent inhibitory effects against several types of tumor cells. To the best of our knowledge, studies regarding the structural modification and Structure- Activity Relations (SAR) of this compound have not yet been reported. OBJECTIVE: The aim of this study was to discover more potent derivatives of GLA and investigate their SAR and cytotoxicity mechanisms. METHODS: Novel 7-O- and 14-O-derivatives of GLA were synthesized by condensation of acids or acyl chloride. The anti-tumor activities of these derivatives against various human cancer cell lines were evaluated in vitro by MTT assays. Apoptosis assays of compound 17 (7,14-diacylation product) were performed on A549 and HL-60 cells by flow cytometry and TUNNEL. The acute toxicity of this compound was tested on mice, at the dose of 300mg per kg body weight. RESULTS: Seventeen novel 7-O- and 14-O-derivatives of GLA (1-17) were synthesized. These compounds showed potent cytotoxicity against the tested cancer cell lines, and almost all of them were found to be more cytotoxic than GLA and oridonin. Of the synthesized derivatives, compound 17 presented the greatest cytotoxicity, with IC50 values of 0.26µM and 1.10µM in HL-60 and CCRF-CEM cells, respectively. Furthermore, this compound induced weak apoptosis of A549 cells but showed great potential in stimulating the apoptosis of HL- 60 cells. Acute toxicity assays indicated that compound 17 is relatively safer. CONCLUSION: The results reported herein indicate that the synthesized GLA derivatives exhibited greater cytotoxicity against leukemia cells than against other types of tumors. In particular, 7,14-diacylation product of GLA was found to be an effective anti-tumor agent. However, the cytotoxicity mechanism of this product in A549 cells is expected to be different than that in other tumor cell lines. Further research is needed to confirm this hypothesis.


Subject(s)
Antineoplastic Agents/pharmacology , Diterpenes, Kaurane/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Apoptosis/drug effects , Cell Line, Tumor , Cell Proliferation/drug effects , Diterpenes, Kaurane/chemical synthesis , Diterpenes, Kaurane/chemistry , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Molecular Structure , Structure-Activity Relationship
8.
Toxicol In Vitro ; 62: 104660, 2020 Feb.
Article in English | MEDLINE | ID: mdl-31629066

ABSTRACT

Herba Epimedii is a famous Chinese edible herb, and due to its potential hepatotoxic effects, the safety associated with this herb has attracted a great deal of attention. In this study, the components of four types of the Herba Epimedii extracts were identified by HPLC-MS/MS. Among these components, 11 components that were present in all four extracts and could be obtained as reference substances were evaluated for their ability of cytotoxicity in HL-7702 and HepG2 cells, resulting in the identification of icarisid I and sagittatoside A as the most relevant with respect to the toxicity of the extracts. The targeted toxicological effects were further investigated using a series of correlated biological indicators to elucidate potentially hepatotoxic mechanisms. The results showed that the extracts and the selected compounds had varying degrees of influence on the leakage of ALT, AST and LDH; the activity of SOD, GSH and MDA; the increase in intercellular ROS; and the decrease in MMP. Among the tested substances, the ethanol extracts exhibited stronger hepatotoxicity, with icarisid I and sagittatoside A correlating with this toxic effect, and the hepatoxic mechanisms of which may be associated with damaged cell structure, increased oxidative stress and induction of apoptosis.


Subject(s)
Chemical and Drug Induced Liver Injury , Epimedium , Plant Extracts/toxicity , Alanine Transaminase/metabolism , Aspartate Aminotransferases/metabolism , Cell Line , Cell Survival/drug effects , Glutathione/metabolism , Humans , L-Lactate Dehydrogenase/metabolism , Malondialdehyde/metabolism , Matrix Metalloproteinases/metabolism , Plant Extracts/chemistry , Reactive Oxygen Species/metabolism , Superoxide Dismutase/metabolism
9.
J Pharm Pharmacol ; 72(5): 649-669, 2020 May.
Article in English | MEDLINE | ID: mdl-31826333

ABSTRACT

OBJECTIVES: Withanolides are a group of modified C28 ergostane-type steroids with a C-22, C-26 δ-lactone side chain or a C-23, C-26 γ-lactone side chain. They enjoy a limited distribution in the plant kingdom and predominantly occur in several genera of Solanaceae. Of which, the genus Physalis is an important resource for this type of natural molecules. The present review aims to comprehensively illustrate the structural characteristics and classification of withanolides, and particularly focus on the progression on phytochemical and pharmacological aspects of withanolides from Physalis ranging from January 2015 to June 2019. KEY FINDINGS: Approximately 351 natural withanolides with novel and unique structures have so far been identified from genus Physalis, mainly isolated from the species of P. angulata and P. peruviana. Withanolides demonstrated diverse biological activity, such as anticancer, anti-inflammatory, antimicrobial, immunoregulatory, trypanocidal and leishmanicidal activity. Their observed pharmacological functions supported the uses of Physalis species in traditional or folk medicines. SUMMARY: Due to their unique structure skeleton and potent bioactivities, withanolides are regarded to be promising drug candidates, particularly for developing anticancer and anti-inflammatory agents. Further investigations for discovering novel withanolides of genus Physalis, exploiting their pharmacological values and evaluating their potency as therapeutic agents are significant work.


Subject(s)
Physalis/chemistry , Withanolides/chemistry , Withanolides/pharmacology , Anti-Infective Agents/pharmacology , Anti-Inflammatory Agents/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Hypoglycemic Agents/pharmacology , Plant Extracts/chemistry , Plant Extracts/classification , Plant Extracts/pharmacology , Plants, Medicinal/chemistry , Plants, Medicinal/classification , Trypanocidal Agents/pharmacology , Withanolides/analysis , Withanolides/classification
10.
Phytother Res ; 33(11): 2971-2978, 2019 Nov.
Article in English | MEDLINE | ID: mdl-31407455

ABSTRACT

Moutan Cortex has been widely used to treat various types of arthritis in traditional Chinese medicine. Paeonol is isolated as an active ingredient from Moutan Cortex. However, the effect and potential mechanism of paeonol on gouty arthritis have not been evaluated. In this study, rats were treated intragastrically with paeonol for consecutive 7 days. On Day 5, rats were intra-articularly injected with monosodium urate (MSU) crystals in the ankle joints to induce MSU-induced arthritis (MIA). Paw volume was detected at various time points. Gait score was measured at 24 hr after MSU crystal injection. Ankle joints were collected for evaluation of histological score and expression of proinflammatory cytokines using hematoxylin and eosin staining and immunohistochemistry staining, respectively. Nuclear level of nuclear factor (NF)-κBp65 in synovial tissues was analyzed by western blot assay. NF-κB DNA-binding activity was measured by enzyme linked immunosorbent assay. Paeonol markedly lowered the paw volume, gait score, and histological score in MIA rats. Mechanistically, paeonol markedly reduced the expression of TNF-α, IL-1ß, and IL-6 in synovial tissues of MIA rats. In addition, the elevated level of p65 in nucleus and NF-κB DNA-binding activity in synovial tissues of MIA rats were reduced significantly by paeonol treatment. These findings suggest that paeonol exerts anti-inflammatory effect in MIA rats through inhibiting expression of proinflammatory cytokines and NF-κB activation.


Subject(s)
Acetophenones/therapeutic use , Arthritis, Gouty/chemically induced , Arthritis, Gouty/prevention & control , Cytokines/metabolism , Inflammation Mediators/metabolism , Uric Acid , Animals , Arthritis, Gouty/metabolism , Down-Regulation/drug effects , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/therapeutic use , Gait/drug effects , Gait Analysis , Male , NF-kappa B/metabolism , Paeonia/chemistry , Rats , Rats, Sprague-Dawley , Signal Transduction/drug effects , Synovial Membrane/drug effects
11.
Molecules ; 24(7)2019 Apr 01.
Article in English | MEDLINE | ID: mdl-30939785

ABSTRACT

Herba Epimedii, a commonly used Chinese medicine, has attracted much attention recently because of its potential hepatotoxic effects. 2″-O-Rhamnosyl icariside II, baohuoside I and baohuoside II are the main components of Herba Epimedii, and previous research indicates that these three compounds are related to the hepatotoxicity of Herba Epimedii. To test this idea, in this study, HL-7702 and HepG2 cells were chosen as the in vitro models and the influences of these three compounds on a series of cytotoxicity indices, including ALT, AST, LDH, SOD, GSH, MDA, ROS and MMP, were determined. The results showed that at certain concentrations, the three compounds had different effects on the indices. Among them, baohuoside I at high concentration (32 µg/mL) displayed more significant cytotoxicity than the other two compounds; therefore, it was inferred to be more closely correlated with the liver injury induced by Herba Epimedii combined with the previous study, and its toxic mechanisms may be involved in increasing oxidative stress and inducing apoptosis. The findings of this study may provide evidence of the toxic composition of Herba Epimedii to preliminarily discuss the toxic mechanisms and provide improved guidance for its clinical safety.


Subject(s)
Apoptosis/drug effects , Carcinoma, Hepatocellular/pathology , Epimedium/chemistry , Flavonoids/pharmacology , Glycosides/pharmacology , Hepatocytes/pathology , Carcinoma, Hepatocellular/drug therapy , Carcinoma, Hepatocellular/metabolism , Cells, Cultured , Hepatocytes/drug effects , Humans , Liver Neoplasms/drug therapy , Liver Neoplasms/metabolism , Liver Neoplasms/pathology , Phytotherapy , Plant Extracts/pharmacology
12.
BMC Neurol ; 19(1): 48, 2019 Mar 29.
Article in English | MEDLINE | ID: mdl-30925914

ABSTRACT

BACKGROUND: Aim to quantitatively analyze the clinical effectiveness for motor cortex stimulation (MCS) to refractory pain. METHODS: The literatures were systematically searched in database of Cocharane library, Embase and PubMed, using relevant strategies. Data were extracted from eligible articles and pooled as mean with standard deviation (SD). Comparative analysis was measured by non-parametric t test and linear regression model. RESULTS: The pooled effect estimate from 12 trials (n = 198) elucidated that MCS shown the positive effect on refractory pain, and the total percentage improvement was 35.2% in post-stroke pain and 46.5% in trigeminal neuropathic pain. There is no statistical differences between stroke involved thalamus or non-thalamus. The improvement of plexus avulsion (29.8%) and phantom pain (34.1%) was similar. The highest improvement rate was seen in post-radicular plexopathy (65.1%) and MCS may aggravate the pain induced by spinal cord injury, confirmed by small sample size. Concurrently, Both the duration of disease (r = 0.233, p = 0.019*) and the time of follow-up (r = 0.196, p = 0.016*) had small predicative value, while age (p = 0.125) had no correlation to post-operative pain relief. CONCLUSIONS: MCS is conducive to the patients with refractory pain. The duration of disease and the time of follow-up can be regarded as predictive factor. Meanwhile, further studies are needed to reveal the mechanism of MCS and to reevaluate the cost-benefit aspect with better-designed clinical trials.


Subject(s)
Motor Cortex , Pain, Intractable/therapy , Trigeminal Neuralgia/therapy , Cost-Benefit Analysis , Electric Stimulation Therapy , Humans , Pain Measurement , Phantom Limb/therapy , Treatment Outcome
13.
Curr Protein Pept Sci ; 20(7): 736-749, 2019.
Article in English | MEDLINE | ID: mdl-30678624

ABSTRACT

Weaned piglets experience sudden changes in their dietary patterns such as withdrawal from the easily digestible watery milk to a coarse cereal diet with both systemic and intestinal disruptions coupling with the expression of pro-inflammatory proteins which affects the immune system and the concentrations of haptoglobin including both positive and negative acute-phase proteins in the plasma. L-arginine is an important protein amino acid for piglets, but its inadequate synthesis is a nutritional problem for both sows and piglets. Recent studies indicated that dietary supplementation of L-arginine increased feed intake, uterine growth, placental growth and nutrient transport, maternal growth and health, embryonic survival, piglets birth weight, piglet's growth, and productivity, and decreased stillbirths. L-arginine is essential in several important pathways involved in the growth and development of piglets such as nitric oxide synthesis, energy metabolism, polyamine synthesis, cellular protein production and muscle accretion, and the synthesis of other functional amino acids. However, the underlying molecular mechanism in these key pathways remains largely unresolved. This review was conducted on the general hypothesis that L-arginine increased the growth and survival of post-weaning piglets. We discussed the effects of dietary L-arginine supplementation during gestation, parturition, lactation, weaning, and post-weaning in pigs as each of these stages influences the health and survival of sows and their progenies. Therefore, the aim of this review was to discuss through a logical approach the effects of L-arginine supplementation on piglet's growth and survival from conception to postweaning.


Subject(s)
Arginine/pharmacology , Dietary Supplements , Fertilization/drug effects , Weaning , Animals , Growth and Development/drug effects , Swine
14.
J Agric Food Chem ; 67(3): 968-974, 2019 Jan 23.
Article in English | MEDLINE | ID: mdl-30580517

ABSTRACT

In the present study, lignin from eucalyptus was extracted with 80% alkaline dioxane (0.05 M NaOH) from ball-milled wood and subsequently fractionated by gradient acid precipitation from the filtrate. Meanwhile, the residual lignin was prepared by a double enzymatic hydrolysis process. The yield of the lignin extracted by alkaline dioxane (LA-2) was 29.5%. The carbohydrate contents and molecular weights of the gradient acid precipitated lignin fractions gradually decreased from 4.90 to 1.36% and from 7770 to 5510 g/mol, respectively, with the decline of the pH value from 6 to 2. Results from two-dimensional heteronuclear single quantum coherence nuclear magnetic resonance (NMR) and 31P NMR spectroscopy showed an evident reduction of ß- O-4 ' linkages with the pH value decrease, while the contents of aliphatic -OH, phenolic -OH, and carboxylic groups displayed an increasing trend. Moreover, the residual lignin exhibited the highest molecular weight (11690 g/mol), the most abundant ß- O-4 ' linkages (71.1%), and the highest S/G ratio (4.68).


Subject(s)
Eucalyptus/chemistry , Lignin/chemistry , Plant Extracts/chemistry , Alkalies/chemistry , Dioxanes/chemistry , Hydrogen-Ion Concentration , Hydrolysis , Lignin/isolation & purification , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Plant Extracts/isolation & purification , Wood/chemistry
15.
Mol Med Rep ; 17(1): 1717-1723, 2018 Jan.
Article in English | MEDLINE | ID: mdl-29138863

ABSTRACT

Pulmonary fibrosis is a chronic, progressive, lethal lung disease characterized by alveolar cell necrosis and dysplasia of interstitial fibrotic tissue, resulting in loss of lung function and eventual respiratory failure. Previously, glucocorticoid drugs were used to treat this lung disorder. However, positive responses were recorded in less than half of treated patients and the cytotoxicity caused by high dosage treatment is still a concern. The present study investigated whether ulinastatin, a typical urinary trypsin inhibitor that mitigates numerous inflammatory responses, could be a treatment option for lung fibrosis. The results demonstrated that ulinastatin had the ability to ameliorate interstitial fibrosis and alveolar exudates and to protect against lung diseases induced by smoke, irradiation or silica particles. The mechanism of ulinastatin resulted in the downregulation of inflammatory cascades: Transforming growth factor­ß1, tumor necrosis factor­α and nuclear factor­κB, as demonstrated by western blotting and ELISA. Ulinastatin treatment with a high dose (100,000 U/kg body weight/day) resulted in an attenuated inflammatory response, and inhibited fibrosis formation in lungs, suggesting that ulinastatin may become a part of a clinical therapeutic strategy.


Subject(s)
Glycoproteins/pharmacology , Pulmonary Fibrosis/drug therapy , Trypsin Inhibitors/pharmacology , Animals , Down-Regulation , Drug Evaluation, Preclinical , Glycoproteins/therapeutic use , Lung/drug effects , Lung/metabolism , Lung/pathology , Male , NF-kappa B/metabolism , Pulmonary Fibrosis/metabolism , Rats, Sprague-Dawley , Signal Transduction , Transforming Growth Factor beta1/metabolism , Trypsin Inhibitors/therapeutic use , Tumor Necrosis Factor-alpha/metabolism
16.
Protein Pept Lett ; 24(5): 442-448, 2017.
Article in English | MEDLINE | ID: mdl-28266265

ABSTRACT

Dietary iron is a crucial nutrient element for biological processes of both hosts and gut microbiota. Deficiency in dietary iron is a highly common disorder in the developing locations of the world and can be healed by oral iron administration or complementary iron diet. While the redundant iron that enters the gut lumen leads to negative effects, and modulates the gut microbial composition and function. Such modulation led to a significant effect on vital biological pathways of the host, including metabolic disease (obesity and type 2 diabetes), metabolites (SCFA, blood glucose and cholesterol), bile acid metabolism, endocrine, neural, and other well-being patterns. This review covers the multifaceted aspects of different nutritional iron stress on the composition and function of microbial gut in monogastrics and consequential health conditions as well as it reveals unclear points that need further studies.


Subject(s)
Anemia , Gastrointestinal Microbiome , Iron Deficiencies , Iron, Dietary , Metabolic Diseases , Anemia/microbiology , Anemia/physiopathology , Animals , Gastrointestinal Microbiome/drug effects , Gastrointestinal Microbiome/physiology , Humans , Iron, Dietary/metabolism , Iron, Dietary/pharmacology , Metabolic Diseases/microbiology , Metabolic Diseases/physiopathology
17.
Fitoterapia ; 118: 94-100, 2017 Apr.
Article in English | MEDLINE | ID: mdl-28300699

ABSTRACT

Two new ent-kauranoid-type diterpenoids (1 and 2) and one new rare dimer of ent-kauranoids (3) with a cyclobutane ring by a [2+2] cycloaddition, together with nine known diterpenoids (4-12) were obtained from the aerial parts of Rabdosia japonica. Their chemical structures were established by 1D and 2D NMR techniques and mass spectrometry and by comparison with spectroscopic data reported. All ent-kauranoids were test for their cytotoxic effects against A549, HCT116, CCRF-CEM and HL-60 tumor cell lines. Compounds 1, 2, 4, 5, 7, 10 and 12 showed potent and selective cytotoxicity. In addition, some selected ent-kauranoids were test for their anti-HBV activities, and the results showed compound 8 had inhibitory effect on HBsAg with a 59% inhibition ratio at the concentration of 20µg/mL.


Subject(s)
Antiviral Agents/chemistry , Diterpenes, Kaurane/chemistry , Isodon/chemistry , Antiviral Agents/isolation & purification , Cell Line, Tumor , Diterpenes, Kaurane/isolation & purification , Drug Screening Assays, Antitumor , HL-60 Cells , Hepatitis B virus/drug effects , Humans , Magnetic Resonance Spectroscopy , Mass Spectrometry , Molecular Structure , Plant Components, Aerial/chemistry , Plant Extracts/chemistry
18.
Yao Xue Xue Bao ; 51(11): 1751-8, 2016 11.
Article in Chinese | MEDLINE | ID: mdl-29908133

ABSTRACT

The method of UHPLC-LTQ-Orbitrap mass spectrometry coupled with higher energy collision dissociation (HCD) was established to rapidly analyze the constituents absorbed into blood after oral administration of steroidal saponins from Radix Ophiopogonis. A total of 31 constituents, including 13 furostanol steroidal saponins and 18 spirostanol steroidal saponins, were characterized based on the accurate mass measurements, fragmentation patterns, chromatographic retention times, and diagnostic product ions. Among them, 8 compounds were unambiguously identified by comparison with their corresponding standards. The results provide comprehensive insights and guidance for elucidation of material basis of Radix Ophiopogonis activity.


Subject(s)
Drugs, Chinese Herbal/pharmacokinetics , Ophiopogon/chemistry , Saponins/pharmacokinetics , Administration, Oral , Animals , Chromatography, High Pressure Liquid , Mass Spectrometry , Plant Roots/chemistry , Reference Standards , Saponins/blood
19.
Zhongguo Zhong Yao Za Zhi ; 39(13): 2583-7, 2014 Jul.
Article in Chinese | MEDLINE | ID: mdl-25276986

ABSTRACT

With the kernel of efficacy, "Xiaohe Silian" was a pattern and method for new drug discovery which was constituted with "metabolism-efficacy, toxicity-efficacy, quality-efficacy and structure-efficacy". Its connotation was in keeping with traditional Chinese medicine (TCM) clinical pharmacy. This paper systematically summarized the research method of new drug discovery practice process for TCM. To avoid western drug like in TCM new drug discovery, we carried out combination analysis with TCM clinical pharmacy. The correlation analysis between basic elements of "Xiaohe Silian(n) and TCM clinical pharmacy was studied to guarantee this method could integrate closely with TCM clinic from all angles. Hence, this method aimed to provide a new method for TCM new drug discovery on the basis of TCM clinical pharmacy with insisting on holistic view of multicomponent study, kinetic view of metabolic process when the curative effect occurred and molecular material view of quality control and structure-activity exposition.


Subject(s)
Drug Discovery/methods , Drugs, Chinese Herbal/pharmacology , Drug Therapy , Drugs, Chinese Herbal/analysis , Humans , Medicine, Chinese Traditional
20.
Molecules ; 19(10): 16925-36, 2014 Oct 22.
Article in English | MEDLINE | ID: mdl-25340298

ABSTRACT

As one of the most important components of Panax ginseng, ginsenoside Rg1 has certain anti-aging effects, improving the activity of learning and memory. Studies have showed that ginsenoside Rg1 improves the memory impairment associated with Alzheimer's disease (AD). In this study, the effects of ginsenoside Rg1 were investigated through the activity of toll-like receptor (TLR) 3, TLR4 and their signaling transduction pathways in amyloid ß peptide 25-35 (Aß25-35) induced AD cell model. Thus we investigated several critical components of the TLR pathway. The neuroglial cell line NG108-15 was stimulated with or without Aß25-35, while different concentrations of ginsenoside Rg1 were administered. After 24 h, tumor necrosis factor-α (TNF-α), interferon-ß (IFN-ß) in cell supernatant and inducible nitric oxide synthase (iNOS) in cell lysate supernatant were measured with enzyme-linked immunosorbent assays (ELISAs). The mRNA and protein expression of TLR3, TLR4, nuclear factor kappa B (NF-κB) and tumor necrosis factor receptor-associated factor-6 (TRAF-6) were detected by real-time PCR and western blot methods, respectively. The experimental results showed that Aß25-35 could markedly raise the level of TNF-α, IFN-ß and iNOS, and increase the expressions of mRNA and TLR3, TLR4, NF-κB and TRAF-6 protein in the NG108-15 cells. At the same time, the ginsenoside Rg1 significantly reduced the expressions of proteins and mRNA of TLR3, TLR4, NF-κB and TRAF-6, and down-regulated the levels of TNF-α, IFN-ß of cell supernatant and iNOS of cell lysate supernatant in a concentration-dependent manner. In conclusion, ginsenoside Rg1 has good activity for suppressing the signaling transduction pathway of TLR3 and TLR4, and decreasing the inflammation factors induced by Aß25-35 in NG108-15 cells, and this may be the mechanism of ginsenoside Rg1 action in AD treatment, but more studies are needed to identify its specificity.


Subject(s)
Alzheimer Disease/drug therapy , Gene Expression Regulation/drug effects , Ginsenosides/pharmacology , Inflammation Mediators/metabolism , Neuroglia/metabolism , Toll-Like Receptor 3/metabolism , Toll-Like Receptor 4/metabolism , Alzheimer Disease/chemically induced , Alzheimer Disease/metabolism , Amyloid beta-Peptides/toxicity , Animals , Blotting, Western , Cells, Cultured , Disease Models, Animal , Enzyme-Linked Immunosorbent Assay , Interferons/metabolism , Mice , NF-kappa B/metabolism , Neuroglia/drug effects , Nitric Oxide Synthase Type II/metabolism , Panax/chemistry , Peptide Fragments/toxicity , RNA, Messenger/genetics , Real-Time Polymerase Chain Reaction , Reverse Transcriptase Polymerase Chain Reaction , Toll-Like Receptor 3/genetics , Toll-Like Receptor 4/genetics , Tumor Necrosis Factor-alpha/metabolism
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