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1.
Article in Chinese | WPRIM | ID: wpr-887974

ABSTRACT

Overtaking lung cancer,breast cancer is now the most commonly diagnosed cancer seriously threatening people's health and life. As the main effective component of Tripterygium wilfordii,triptolide( TP) has attracted increasing attention due to its multitarget and multi-pathway anti-tumor activity. Recent studies have revealed that breast cancer-sensitive TP enables the inactivation of breast cancer cells by inducing tumor cell apoptosis and autophagy,interfering in tumor cell metastasis,resisting drug resistance,arresting tumor cell cycle,and influencing tumor microenvironment. It has been recognized as a promising clinical antitumor agent by virtue of its widely accepted therapeutic efficacy. This paper reviewed the anti-breast cancer action and its molecular mechanisms of TP on the basis of the relevant literature in the past ten years,and proposed application strategies in view of the inadequacy of TP to provide a reference for further research on the application of TP in the treatment of breast cancer.


Subject(s)
Breast Neoplasms/genetics , Diterpenes/pharmacology , Epoxy Compounds , Female , Humans , Phenanthrenes , Tumor Microenvironment
2.
Chinese Journal of Biotechnology ; (12): 2039-2049, 2021.
Article in Chinese | WPRIM | ID: wpr-887780

ABSTRACT

Triptolide has wide clinical applications due to its anti-inflammatory, anti-tumor and immunosuppressive activities. In this study, we investigated the effect of blocking isopentenyl pyrophosphate (IPP) translocation on the biosynthesis of triptolide by exogenously adding D,L-glyceraldehyde (DLG) to the suspension cells of Ttripterygium wilfordii at different stages (7 d, 14 d). Subsequently, the cell viability, biomass accumulation, triptolide contents, as well as the profiles of the key enzyme genes involved in the upstream pathway of triptolide biosynthesis, were analyzed. The results showed that IPP translocation is involved in the biosynthesis of triptolide. IPP is mainly translocated from the plastid (containing the MEP pathway) to the cytoplasm (containing the MVA pathway) in the early stage of the culture, but reversed in the late stage. Blocking the translocation of IPP affected the expression of key enzyme genes involved in the upstream pathway of triptolide, which in turn affected the accumulation of triptolide. Understanding the characteristics and mechanism of IPP translocation provides a theoretical basis for further promoting triptolide biosynthesis through synthetic biology.


Subject(s)
Diterpenes , Epoxy Compounds , Hemiterpenes , Organophosphorus Compounds , Phenanthrenes
3.
Article in Chinese | WPRIM | ID: wpr-879180

ABSTRACT

This study aims to study the chemical components from the gum resin of Boswellia carterii. Five cembranoid diterpenes were isolated from the gum resin of B. carterii by various of column chromatographies including silica gel, Sephadex LH-20, and semi-preparative HPLC. Their structures were identified on the basis of physicochemical properties, mass spectrometry(MS), nuclear magnetic resonance(NMR), Ultraviolet(UV) and infrared(IR) spectroscopic data. These compounds were identified as(1S,2E,4R,5S,7E,11E)-4-methoxy-5-hydroxycembrane(1),(1R~*,4R~*,5E,8E,12E,15E)-4-hydroxycembra-5,8,12,15-tetraene(2), cembrene A(3),(3S,4S,7R)-4-hydroxycembrane(4), and pavidolide D(5). Compound 1 was a new compound. Compounds 2, 4, and 5 were obtained from the gum resin of B. carterii for the first time. Compound 2 showed weak inhibition on the human liver cancer cell line HepG2.


Subject(s)
Boswellia , Cell Line , Diterpenes , Humans , Molecular Structure , Resins, Plant
4.
Article in Chinese | WPRIM | ID: wpr-888142

ABSTRACT

The chemical constituents from the roots of Aconitum kongboense were studied. Twenty-five diterpenoid alkaloids were isolated from the 95% methanol extract of the roots of A. kongboense by silica gel, reverse-phase silica gel and basic alumina column chromatography. They included a new aconitine-type diterpenoid alkaloid, named as kongboensenine(1), and twenty-four known ones(2-25), i.e., acotarine F(2), acotarine G(3), 14-acetyltalatisamine(4), talatisamine(5), indaconitine(6), yunaconitine(7), chasmanine(8), 6-epi-foresticine(9), homochasmanine(10), 8-deacetyl-yunaconitine(11), chasmaconitine(12), ajaconine(13), franchetine(14), ezochasmanine(15), crassicautine(16), 14-O-deacylcrassicausine(17), genicunine A(18), falconeridine(19), sachaconitine(20), liljestrandisine(21), 8-methyl-14-acetyltalatisamine(22), kongboendine(23), 14-benzoylchasmanine(24) and pseudaconine(25). Their structures were elucidated by common spectroscopic methods including high-resolution electrospray ionization mass spectrometry(HR-ESI-MS) and nuclear magnetic resonance(NMR) techniques. Compounds 2-4, 10, 13, 15-19 and 21-22 were isolated from this plant for the first time. Experimental results showed that all compounds did not have a significant inhibitory activity against acetylcholinesterase(AChE).


Subject(s)
Acetylcholinesterase , Aconitum/metabolism , Alkaloids , Diterpenes , Magnetic Resonance Spectroscopy , Molecular Structure , Plant Roots/metabolism
5.
Article in Chinese | WPRIM | ID: wpr-888100

ABSTRACT

The genus Chloranthus has 13 species and 5 varieties in China, which can be found in the southwest and northeast regions. Phytochemical studies on Chloranthus plants have reported a large amount of terpenoids, such as diterpenoids, sesquiterpenoids, and sesquiterpenoid dimers. Their anti-inflammation, anti-tumor, antifungal, antivirus, and neuroprotection activities have been confirmed by previous pharmacological research. Herein, research on the chemical constituents from Chloranthus plants and their biological activities over the five years was summarized to provide scientific basis for the further development and utilization of Chloranthus plants.


Subject(s)
Diterpenes , Phytochemicals/pharmacology , Plants , Sesquiterpenes/pharmacology , Terpenes
6.
Article in Chinese | WPRIM | ID: wpr-888073

ABSTRACT

The purpose of the research is to study the bioactive constituents of Callicarpa nudiflora. From the 65% ethanol extract of C. nudiflora leaves, ten compounds were isolated by macroporous adsorption resin, Sephadex LH-20, ODS, silica gel, and preparative HPLC. These compounds were identified as callicapene M6(1), sterebin A(2), isomartynoside(3), crenatoside(4), luteolin-7-O-neohesperidoside(5), apigenin-7-O-β-D-neohesperidoside(6), isoacteoside(7), acteoside(8),(7R)-campneoside I(9), and(7S)-campneoside I(10) on the basis of NMR, HR-ESI-MS, and optical rotation data. Compound 1 was obtained as a new compound. Compounds 2 and 4 were isolated from the genus Callicarpa for the first time. Compounds 9 and 10 were isolated from C. nudiflora for the first time.


Subject(s)
Callicarpa , Chromatography, High Pressure Liquid , Diterpenes , Molecular Structure , Plant Leaves
7.
Article in English | WPRIM | ID: wpr-888792

ABSTRACT

A phytochemical investigation was carried out on the extract of a medicinal plant Callicarpa nudiflora, resulting in the characterization of five new 3, 4-seco-isopimarane (1-5) and one new 3, 4-seco-pimarane diterpenoid (6), together with four known compounds. The structures of the new compounds were fully elucidated by extensive analysis of MS, 1D and 2D NMR spectroscopic data, and time-dependent density functional theory (TDDFT) calculation of electronic circular dichroism (ECD) spectra, and DFT calculations for NMR chemical shifts and optical rotations.


Subject(s)
Abietanes/isolation & purification , Callicarpa/chemistry , Diterpenes/isolation & purification , Molecular Structure , Phytochemicals/isolation & purification , Plant Leaves
8.
Article in Chinese | WPRIM | ID: wpr-921801

ABSTRACT

Five compounds were isolated from the alcohol extract of Olibanum by MCI, silica gel, ODS, and Sephadex LH-20 column chromatographies and preparative high-performance liquid chromatography(HPLC). On the basis of spectral data and literature data, the compounds were identified as:(1S,3R,4S,7R,11S,12R)-1:12,4:7-diepoxisonane-8(19)-ene-3,11-diol(1), boscartin A(2),(+)-resinolin(3),(+)-5-hydroxy-3,4-dimethyl-5-pentylfuran-2(5H)-one(4), and acerogenin A(5). Compound 1 is a new compound, and compounds 3-5 were isolated from Olibanum for the first time. The structure of compound 1 was determined by spectroscopic analysis and single-crystal X-ray diffraction. Compounds 1 and 2 were tested for PC12 neurotoxicity, and the results showed that they were both safe compounds.


Subject(s)
Chromatography, High Pressure Liquid , Diterpenes , Frankincense , Molecular Structure
9.
Article in Chinese | WPRIM | ID: wpr-921673

ABSTRACT

Triptolide(TP), the main active and toxic component of Tripterygium wilfordii, has the limitations of low bioavailability, poor absorption, low concentration in plasma, and small lethal dose. Microneedle(MN), the hybrid of hypodermic needle and transdermal patch, is a physical penetration-enhancing system. Dissolving microneedles(DMNs) can be tailored to specific needs of degradation rate. In this study, the TP-loaded DMNs(DMNs-TP) were prepared with the two-step centrifugation method. The optimal ratio of PVA to PVP K30, water content in matrix solution, demoulding method, and plasticizer for preparing DMNs were investigated with the indexes of formability and mechanical strength. The drug loading capacity was determined by HPLC and morphological characteristics were observed under an optical microscope. The mechanical properties were investigated by H&E staining and Franz diffusion cell was used to detect the in vitro skin permeation characteristics. Through the experiment, we confirmed that the optimal backing material should be PVA and PVP K30(3∶1) and the optimal ratio of matrix material to water should be 3∶4. The prepared DMNs-TP were pyramidal with smooth surface and length of approximately 550 μm. Each patch(2.75 cm~2) had the drug loading capacity of(153.41±2.29) μg, and TP was located in the upper part of the needle. The results of in vitro skin permeation assay demonstrated that the cumulative penetration of TP in DMNs-TP reached 80% in 24 h, while little TP solution penetrated the skin, which proved that DMNs promoted the transdermal delivery of TP.


Subject(s)
Administration, Cutaneous , Diterpenes , Drug Delivery Systems , Epoxy Compounds , Needles , Phenanthrenes , Skin
11.
Arq. bras. cardiol ; 115(4): 669-677, out. 2020. tab, graf
Article in Portuguese | SES-SP, LILACS, SES-SP | ID: biblio-1131333

ABSTRACT

Resumo Fundamento: Diversos estudos têm mostrado que as classes de diterpenos exercem efeito significativo no sistema cardiovascular. Os diterpenos, em particular, estão entre os principais compostos associados às propriedades cardiovasculares, como a propriedade vasorrelaxante, inotrópica, diurética e a atividade hipotensora. Embora o mecanismo de vasorrelaxamento do manool seja visível, seu efeito sobre a pressão arterial (PA) ainda é desconhecido. Objetivo: Avaliar o efeito hipotensor in vivo do manool e verificar o efeito de vasorrelaxamento ex vivo em anéis aórticos de ratos. Métodos: Os animais foram divididos aleatoriamente em dois grupos: normotensos e hipertensos. O grupo normotenso foi submetido à cirurgia sham e adotou-se o modelo 2R1C para o grupo hipertenso. Realizou-se monitoramento invasivo da PA para testes com manool em diferentes doses (10, 20 e 40 mg/kg). Foram obtidas curvas de concentração-resposta para o manool nos anéis aórticos, com endotélio pré-contraído com fenilefrina (Phe) após incubação com Nω-nitro-L-arginina metil éster (L-NAME) ou oxadiazolo[4,3-a]quinoxalina-1-ona (ODQ). Os níveis plasmáticos de óxido nítrico (NOx) foram medidos por ensaio de quimioluminescência. Resultados: Após a administração de manool, a PA se reduziu nos grupos normotenso e hipertenso, e esse efeito foi inibido pelo L-NAME em animais hipertensos apenas na dose de 10 mg/kg. O manool ex vivo promoveu vasorrelaxamento, inibido pela incubação de L-NAME e ODQ ou remoção do endotélio. Os níveis plasmáticos de NOx aumentaram no grupo hipertenso após a administração de manool. O manool induz o relaxamento vascular dependente do endotélio na aorta de ratos, mediado pela via de sinalização NO/cGMP e redução da PA, e também pelo aumento plasmático de NOx. Esses efeitos combinados podem estar envolvidos na modulação da resistência periférica, contribuindo para o efeito anti-hipertensivo do diterpeno. Conclusão: Esses efeitos em conjunto podem estar envolvidos na modulação da resistência periférica, contribuindo para o efeito anti-hipertensivo do diterpeno.


Abstract Background: Many studies have shown that the diterpenoid classes exert a significant effect on the cardiovascular system. Diterpenes, in particular, are among the main compound links to cardiovascular properties such as vasorelaxant, inotropic, diuretic and hypotensive activity. While the manool vasorelaxation mechanism is visible, its effect on blood pressure (BP) is still unknown. Objective: To evaluate the in vivo hypotensive effect of manool and check the ex vivo vasorelaxation effect in rat aortic rings. Methods: The animals were divided randomly into two groups: normotensive and hypertensive. The normotensive group was sham-operated, and the 2K1C model was adopted for the hypertensive group. Invasive BP monitoring was performed for manool tests at different doses (10, 20 and 40 mg/kg). Concentration-response curves for manool were obtained in the aorta rings, with endothelium, pre-contracted with phenylephrine (Phe) after incubation with Nω-nitro-L-arginine methyl ester(L-NAME) or oxadiazole [4,3-a]quinoxalin-1-one (ODQ). Nitric oxide (NOx) plasma levels were measured by chemiluminescence assay. Results: After manool administration, BP was reduced in normotensive and hypertensive groups, and this effect was inhibited by L-NAME in hypertensive animals only in 10 mg/kg dose. Ex vivo manool promoted vasorelaxation, which was inhibited by L-NAME and ODQ incubation or endothelium removal. NOx plasma levels increased in the hypertensive group after manool administration. Manool elicits endothelium-dependent vascular relaxation in rat aorta mediated by the NO/cGMP signaling pathway and BP reduction, also by NOx plasma increase. These combined effects could be involved in modulating peripheral resistance, contributing to the antihypertensive effect of diterpene. Conclusion: These effects together could be involved in modulating peripheral resistance, contributing to the antihypertensive effect of diterpene.


Subject(s)
Animals , Rats , Arterial Pressure , Hypertension/drug therapy , Aorta, Thoracic , Vasodilation , Vasodilator Agents/pharmacology , Blood Pressure , Endothelium, Vascular , Diterpenes/pharmacology , Nitric Oxide/pharmacology
12.
Bol. latinoam. Caribe plantas med. aromát ; 19(2): 236-246, mar. 2020. ilus, tab
Article in English | LILACS | ID: biblio-1104216

ABSTRACT

Chloroform extract (CE) and fractions obtained from Aldama arenaria roots were evaluated for their in vitro antiproliferative activity against 10 human tumor cell lines [leukemia (K-562), breast (MCF-7), ovary expressing a multidrug-resistant phenotype (NCI/ADR-RES), melanoma (UACC-62), lung (NCI-H460), prostate (PC-3), colon (HT29), ovary (OVCAR-3), glioma (U251), and kidney (786-0)]. CE presented weak to moderate antiproliferative activity (mean log GI50 1.07), whereas fractions 3 and 4, enriched with pimaranetype diterpenes [ent-pimara-8(14),15-dien-19-oic acid and ent-8(14),15-pimaradien-3ß-ol], presented moderate to potent activity for most cell lines, with mean log GI50 of 0.62 and 0.59, respectively. The results showed promising in vitro antiproliferative action of the samples obtained from A. arenaria, with the best results for NCI/ADR-RES, HT29, and OVCAR-3, and TGI values ranging from 5.95 to 28.71 µg.ml -1, demonstrating that compounds of this class may be potential prototypes for the discovery of new therapeutic agents.


El extracto de cloroformo (CE) y las fracciones obtenidas de las raíces de Aldama arenaria fueron evaluadas por su actividad antiproliferativa in vitro contra 10 líneas celulares tumorales humanas [leucemia (K-562), mama (MCF-7), ovario que expresa un fenotipo resistente a múltiples fármacos (NCI/ADR-RES), melanoma (UACC-62), pulmón (NCI-H460), próstata (PC-3), colon (HT29), ovario (OVCAR-3), glioma (U251) y riñón (786-0)]. CE presentó actividad antiproliferativa débil a moderada (log GI50 promedio de 1.07), mientras que las fracciones 3 y 4, enriquecidas con diterpenos de tipo pimarane [ent-pimara-8 (14), ácido 15-dien-19-oico y ent-8 (14), 15-pimaradien-3ß-ol], presentaron actividad moderada a potente para la mayoría de las líneas celulares, con un log GI50 promedio de 0.62 y 0.59, respectivamente. Los resultados mostraron una prometedora acción antiproliferativa in vitro de las muestras obtenidas de A. arenaria, con los mejores resultados para NCI/ADR-RES, HT29 y OVCAR-3, y valores de TGI que van desde 5.95 a 28.71 µg.ml -1, lo que demuestra que los compuestos de esta clase pueden ser prototipos potenciales para el descubrimiento de nuevos agentes terapéuticos.


Subject(s)
Plant Extracts/pharmacology , Chloroform , Plectranthus/chemistry , Cell Line, Tumor/drug effects , Cell Proliferation/drug effects , In Vitro Techniques , Plant Extracts/chemistry , Ethnobotany , Cuba , Diterpenes/pharmacology , Diterpenes/chemistry
13.
Braz. arch. biol. technol ; 63: e20180752, 2020. tab
Article in English | LILACS | ID: biblio-1132231

ABSTRACT

Abstract Commercial roasted and ground coffees are usually blends of Coffea arabica and Coffea canephora. Considering the differences in price and sensory characteristics between these two species, the identification of the presence of each species in commercial blends is of great interest. The aim of this study was to describe typical profiles of caffeine and diterpenes (kahweol and cafestol) contents and the ratios among these compounds to support the characterization of Coffea species in roasted coffees. 32 good cup quality Brazilian C. arabica coffees (from coffee quality contests) produced using different postharvest treatments were studied. All analysis were performed by HPLC. Higher ranges were observed in diterpene contents - kahweol varied from 1.75 to 10.68 g/kg (coefficient of variation of 510%) and cafestol from 1.76 to 9.66 g/kg (449%) - than caffeine, that varied from 5.1 to 16.2 g/kg (coefficient of variation of 218%). Wide ranges of the kahweol/cafestol ratio (0.63 to 2.77) and the caffeine/kahweol ratio (0.84 to 5.15) were also observed. Hence it was proposed the additional use of a new parameter, the ratio of caffeine/sum of diterpenes (kahweol + cafestol) that presents values from 0.54 to 2.39. The results indicated that the combined use of these parameters could be a potential tool for discriminating Coffea species in blends of roasted and ground coffee. It was proposed as potentially indicative of C. arabica: values of kahweol/cafestol ratio above 0.50, associated with caffeine/kahweol ratio lower than 5.50 and caffeine/sum of diterpenes ratio lower than 2.50.


Subject(s)
Caffeine/analysis , Coffee/chemistry , Diterpenes/analysis , Coffee Industry , Chromatography, High Pressure Liquid
14.
Article in Chinese | WPRIM | ID: wpr-880776

ABSTRACT

OBJECTIVE@#To investigate the protective effect of arctiin with anti-inflammatory bioactivity against triptolide-induced nephrotoxicity in rats and explore the underlying mechanism.@*METHODS@#Forty SD rats were divided into 4 groups for gastric lavage of normal saline, arctiin (500 mg/kg), triptolide (500 μg/kg), or both arctiin (500 mg/kg) and triptolide (500 μg/kg). Blood samples were collected for analysis of biochemical renal parameters, and the renal tissues were harvested for determining the kidney index and for pathological evaluation with HE staining. In the @*RESULTS@#In SD rats, arctiin significantly antagonized triptolide-induced elevation of BUN, Scr and kidney index (@*CONCLUSIONS@#Arctiin can protect the kidney from triptolide-induced damages in rats possibly through the anti-inflammatory pathway.


Subject(s)
Animals , Anti-Inflammatory Agents , Diterpenes/toxicity , Epoxy Compounds/toxicity , Furans , Glucosides , Kidney/drug effects , Phenanthrenes/toxicity , Rats , Rats, Sprague-Dawley
15.
An. bras. dermatol ; 94(3): 313-319, May-June 2019. tab, graf
Article in English | LILACS | ID: biblio-1011106

ABSTRACT

Abstract: Background: Actinic keratosis (AK) represents a risk of progression to squamous cell carcinoma. Ingenol mebutate gel is a novel therapeutic option for field-directed treatment. Objectives: To evaluate the safety, tolerability and patients' perspectives, related to the therapeutic success of managing AKs on the face and scalp with ingenol mebutate gel in Brazilian individuals. Methods: This was an observational, retrospective and descriptive study of 68 areas of actinic keratosis on the face and scalp treated with Ingenol mebutate gel involving a total of 37 patients. The drug was applied for three consecutive days on an area of of 25 cm2 and documentation was performed on baseline and days 4, 8, 15, 60 and 180. On day 4, the composite local skin reaction score was calculated. At the end, a questionnaire was applied to evaluate patients' perspectives about the treatment. Results: Adherence was 100%, no serious adverse events were recorded and the mean composite local skin reaction score (standard deviation) was 8.61±4.22. The treatment was considered optimum by 75.68% of the patients. Study limitations: Calculation of composite local skin reaction score performed only on the fourth day. Conclusions: Treatment with ingenol mebutate gel was considered safe and tolerable in Brazilian subjects. Patients had a maximum adherence rate and a great improvement in self-esteem. The results of this research reproduce the findings of the literature.


Subject(s)
Humans , Male , Female , Middle Aged , Aged , Aged, 80 and over , Dermatologic Agents/therapeutic use , Diterpenes/therapeutic use , Keratosis, Actinic/drug therapy , Gels/therapeutic use , Scalp Dermatoses/drug therapy , Administration, Cutaneous , Brazil , Surveys and Questionnaires , Retrospective Studies , Treatment Outcome , Facial Dermatoses/drug therapy
16.
Rev. Assoc. Med. Bras. (1992) ; 65(4): 535-540, Apr. 2019.
Article in English | LILACS | ID: biblio-1003065

ABSTRACT

The Guidelines Project, an initiative of the Brazilian Medical Association, aims to combine information from the medical field in order to standardize producers to assist the reasoning and decision-making of doctors. The information provided through this project must be assessed and criticized by the physician responsible for the conduct that will be adopted, depending on the conditions and the clinical status of each patient.


Subject(s)
Humans , Cystitis, Interstitial/drug therapy , Pentosan Sulfuric Polyester/therapeutic use , Administration, Intravesical , Brazil , Dimethyl Sulfoxide/therapeutic use , Chondroitin Sulfates/therapeutic use , Treatment Outcome , Botulinum Toxins, Type A/therapeutic use , Diterpenes/therapeutic use , Clinical Decision-Making , Hyaluronic Acid/therapeutic use , Lidocaine/therapeutic use , Mycobacterium bovis
17.
Ciênc. Saúde Colet ; 24(3): 827-838, mar. 2019. tab, graf
Article in English | LILACS | ID: biblio-989625

ABSTRACT

Abstract To evaluate the effect of vitamin A supplementation in postpartum infants and women on serum retinol levels and breast milk. The databases Medline, PubMed, Lilacs and SciELO were consulted. The descriptors used were vitamin A, dietary supplement, child, postpartum period, infant and nutrition programs policies. Search found 7432 articles. After elimination of duplicity and application of eligibility criteria, 8 studies remained. All evaluated the effect of vitamin A supplementation on immediate postpartum, five studies used retinyl palmitate supplementation, one with retinyl palmitate and two did not specify the form of supplementation. Six studies evaluated colostrum and two included supplementation of children. It was found that supplementation in the puerperium increases the concentrations of serum retinol and breast milk, however, this result was in the short term and was relevant when the previous concentrations of the mother were low. When maternal serum concentrations are adequate, the retinol content in milk does not change, with little relevance for children. Further studies should be performed to evaluate the effect of megadoses supplementation on serum concentrations of children.


Resumo Avaliar o efeito da suplementação de vitamina A, em lactentes e mulheres no pós-parto, nos níveis de retinol sérico e no leite materno. Foram consultadas as bases de dados Medline, PubMed, Lilacs e SciELO. Os descritores utilizados foram: vitamin A, dietary supplement, child, postpartum period, infant e nutrition programs policies. A busca identificou 7432 artigos. Após eliminação da duplicidade e aplicação dos critérios de elegibilidade permaneceram 8 estudos. Todos avaliaram o efeito da suplementação de vitamina A no pós parto imediato, cinco estudos utilizaram a suplementação com retinil palmitato, um com palmitato de retinila e dois não especificaram a forma de suplementação. Seis estudos avaliaram o colostro e dois incluíram a suplementação de crianças. Encontrou-se que a suplementação no puerpério aumenta as concentrações de retinol sérico e do leite materno, no entanto, este resultado foi a curto prazo e foi relevante quando as concentrações prévias da mãe eram baixas. Quando as concentrações séricas maternas encontram-se adequadas, pouco se altera o teor de retinol no leite, tendo pouco relevância para as crianças. Mais estudos devem ser realizados para avaliar o efeito da suplementação com megadoses nas concentrações séricas de crianças.


Subject(s)
Humans , Female , Pregnancy , Infant, Newborn , Vitamin A/analogs & derivatives , Dietary Supplements , Milk, Human/chemistry , Time Factors , Vitamin A/administration & dosage , Vitamin A/metabolism , Vitamin A Deficiency/prevention & control , Colostrum/chemistry , Postpartum Period , Diterpenes
18.
Article in Chinese | WPRIM | ID: wpr-781245

ABSTRACT

OBJECTIVE@#To investigate whether kirenol, the major pharmacologically active compound of the Chinese medicinal herb , can protect mice from dextran sulfate sodium (DSS)-induced ulcerative colitis (UC).@*METHODS@#C57BL/6 mice with or without kirenol pretreatment were treated with DSS in drinking water for 7 days to induce UC. The symptoms of UC including weight loss, diarrhea and bloody stool were observed daily and graded using the disease activity index (DAI). Colon injury of the mice was assessed by measuring the length of the colon and HE staining of the colon tissue. The levels of inflammatory cytokines produced by the mesenteric lymph nodes (MLNs) lymphocytes were measured using enzyme-linked immunosorbent assay; the apoptosis of the lymphocytes and CD4 T cells was analyzed using flow cytometry.@*RESULTS@#The mice receiving pretreatment with kirenol showed obviously ameliorated symptoms of UC and milder pathological changes in the colon as compared with the control mice. Kirenol treatment significantly down-regulated the secretion of IFN-γ, IL-17A, IL-6 and TNF-α by the MLNs lymphocytes and increased the apoptosis of lymphocytes, especially CD4 T cells in the DSS-treated mice.@*CONCLUSIONS@#Kirenol can protect against T cell-mediated colon injury in DSS-treated mice possibly by suppressing the secretion of inflammatory mediators and inducing apoptosis of the inflammatory lymphocytes.


Subject(s)
Animals , Apoptosis , Colitis, Ulcerative , Cytokines , Dextran Sulfate , Diterpenes , Mice , Mice, Inbred C57BL , T-Lymphocytes
19.
Article in Chinese | WPRIM | ID: wpr-777503

ABSTRACT

Eight C_(19)-diterpenoid alkaloids( 1-8) were isolated from the ethyl acetate soluble fraction of 95% ethanol extract of the ground roots of Aconitum austroyunnanense through various column chromatographies on silica gel,ODS,Sephadex LH-20 and MCI gel.Their structures were elucidated as 14α-benzoyloxy-13β,15α-dihydroxy-1α,6α,8β,16β,18-pentamethoxy-19-oxoaconitan( 1),N-deethylaconitine( 2),spicatine B( 3),leucanthumsine A( 4),acofamine B( 5),macrorhynine B( 6),aconitilearine( 7),and ambiguine( 8) based on their chemical and physicochemical properties and spectroscopic data. Compound 1 was a new compound and alkaloids 2-8 were isolated from this plant for the first time. Some isolated alkaloids were tested in vitro for cytotoxic potential by employing the MTT method. As a result,alkaloid 1 exhibited weak cytotoxic activity against three tested tumor cell lines( A-549,He La,and Hep G2) with IC_(50) values less than 20 μmol·L~(-1).


Subject(s)
Aconitum , Alkaloids , Diterpenes , Molecular Structure , Plant Roots
20.
Article in Chinese | WPRIM | ID: wpr-777501

ABSTRACT

To solve the problems of the poor resolution of chromatographic separation,the weak durability of the relative correction factors,and the low accuracy of content determination results in the quantitative analysis of multi-components by single-marker( QAMS) method with andrographolide as the internal reference substance in the existing research of Andrographis Herba,a new QAMS method using dehydroandrographolide as the internal reference substance was established for the first time in this study. This new method can be used to simultaneously determine four diterpene lactones,including andrographolide( A),neoandrographolide( B),14-deoxyandrographolide( C),and dehydroandrographolide( S) through the optimization of chromatographic conditions and systematic investigation of methodology. At the present HPLC chromatographic conditions,four components could be well separated( R > 1. 5),and the methodology validations could satisfy the requirement of quantitative analysis. The relative correction factors( RCFs) of fA/S,fB/S,fC/S were determined as 0. 65,0. 54,0. 78,respectively. The relative standard deviations( RSDs) of their RCFs ranged between 1. 3%-5. 1%,0. 25%-0. 33%,0. 070%-0. 15%,0. 070%-0. 22%,respectively with three brands of HPLC instruments,five brands of C18 column,different flow rates( 0. 9,1. 0,1. 1 m L·min~(-1)),and different column temperatures( 25,30,35 ℃),indicating good durability of the RCFs. The relative retention value( RRV) method was used to locate the chromatographic peak of the components to be determined.The RRVs of rA/S,rB/S,and rC/Swere 0. 44,0. 86,0. 97,respectively. The RSDs of the RRVs ranged between 0. 030%-1. 6% with different HPLC instruments and columns,showing accurate peak location. The present QAMS method and the external standard method( ESM)were both used to determine the contents of four diterpene lactones from Andrographis Herba( 6 batches of medicinal materials and 18 batches of cut crude drugs). The relative errors of the determined content results between two methods were less than 2. 0%. It demonstrated that there was no significant difference in content results between these two methods,indicating good accuracy of the present QAMS method. Therefore,in this study,an accurate and highly durable QAMS method using dehydroandrographolide as the internal reference substance was established for simultaneous determination of four diterpene lactones. This method could be used to effectively control the quality of Andrographis Herba and provide technical basis for the formulation of traditional Chinese medicine industry standard and improvement of the Chinese Pharmacopoeia standard of Andrographis Herba.


Subject(s)
Andrographis , Chromatography, High Pressure Liquid , Diterpenes , Drugs, Chinese Herbal , Quality Control
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