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1.
Molecules ; 26(17)2021 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-34500591

RESUMO

Triterpenoids and steroids are considered to be important for the fruit quality and health-promoting properties for the consumers. The aim of the study was the determination of the changes in triterpenoid and steroid biosynthesis and the accumulation in hypanthium and achenes of rugosa rose (Rosa rugosa Thunb.) hip during fruit development and ripening at three different phenological stages (young fruits, fully developed unripe fruits, and matured fruits). Triterpenoids and steroids were also determined in the peel and the pulp of the matured hips. The obtained results indicated that the distribution of the analyzed compounds in different fruit tissues is a selective process. The increased rate of hydroxylation of triterpenoids, the deposition of hydroxylated acids in fruit surface layer, and the continuous biosynthesis of phytosterols in achenes versus its gradual repression in hypanthium accompanied by the accumulation of their biosynthetic intermediates and ketone derivatives seem to be characteristic metabolic features of maturation of rugosa rose accessory fruit. These observations, apart from providing the important data on metabolic modifications occurring in developing fruits, might have a practical application in defining fruit parts, particularly rich in bioactive constituents, to enable the development of novel functional products.


Assuntos
Rosa/metabolismo , Esteroides/metabolismo , Triterpenos/metabolismo , Antioxidantes/metabolismo , Frutas/metabolismo
2.
Biomater Sci ; 9(19): 6355-6380, 2021 Sep 28.
Artigo em Inglês | MEDLINE | ID: mdl-34582530

RESUMO

Celastrol (CLT) is an active ingredient that was initially discovered and extracted from the root of Tripterygium wilfordii. The potential pharmacological activities of CLT in cancer, obesity, and inflammatory, auto-immune, and neurodegenerative diseases have been demonstrated in recent years. However, CLT's clinical application is extremely restricted by its low solubility/permeability, poor bioavailability, and potential off-target toxicity. The advent of nanotechnology provides a solution to improve the oral bioavailability, therapeutic effects or tissue-targeting ability of CLT. This review focuses on the most recent advances, improvements, inventions, and updated literature of various nanocarrier systems for CLT.


Assuntos
Portadores de Fármacos , Triterpenos , Nanotecnologia , Triterpenos Pentacíclicos , Tripterygium
3.
Zhongguo Zhong Yao Za Zhi ; 46(18): 4782-4792, 2021 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-34581089

RESUMO

This study investigated the protective effect of total triterpenoids from Chaenomeles speciosa against Helicobacter pylori(Hp)-induced gastritis in mice and explored its possible mechanism. The chronic atrophic gastritis(CAG) model mice were randomly divided into four groups of model, total triterpenoids from C. speciosa(50 and 100 mg·kg~(-1)) and triple therapy, with C57 BL/6 J mice without Hp infection taken as the normal group. Mice in the treatment groups were given corresponding drugs once a day for 4 weeks. Then the following indexes were detected: the contents of reactive oxygen species(ROS), monocyte chemotactic protein 1(MCP-1), keratinocyte chemokines(KC), TNF-α, IL-1ß, IL-6, IL-18, IL-4 and IL-10 in blood and gastric tissue, the activities and contents of LDH, MPO, SOD, GSH-Px, CAT and MDA in gastric tissue and the activities of ß-glucuronidase, ß-galactosidase, cathepsins B and D in blood, gastric tissue and lysosome. Besides, the mRNA expression levels of Toll-like receptor 4(TLR4), myeloid differentiation factor 88(MyD88), Bcl-2, Bcl-xl, Bax and Bad in gastric tissue were determined by quantitative real-time PCR. Western blot was employed to detect the protein expression levels of TLR4, MyD88, p-IKKß, p-IκBα, NOD-like receptor 3(NLRP3), apoptosis-associated speck-like protein(ASC), pro-caspase-1, caspase-1, thioredoxin-interacting protein(TXNIP), pro-IL-1ß, pro-IL-18, Bcl-2, Bcl-xl, Bax, Bad, cytochrome C, apoptotic protease-activating factor-1(Apaf-1), pro-caspase-9, pro-caspase-3, cleaved-caspase-9, cleaved-caspase-3, poly(ADP-ribose) polymerase 1(PARP-1), cleaved-PARP-1 and cytosol and nucleus NF-κB p65 in gastric tissue. The results indicated that the total triterpenoids from C. speciosa significantly suppressed Hp proliferation, alleviated the damage to gastric mucosa and improved lymphocyte infiltration and gland atrophy. They were also effective in reducing the activities of ß-glucuronidase, ß-galactosidase, cathepsins B and D in blood and gastric tissue, elevating the activities of ß-glucuronidase and cathepsin D in lysosomal organelles, decreasing the contents of ROS, MCP-1, KC, TNF-α, IL-1ß, IL-6, IL-18 in blood, MDA content and MPO and LDH activities in gastric tissue and increasing the contents of IL-4 and IL-10 in blood and activities of SOD, CAT and GSH-Px in gastric tissue. Other phenomena were also observed after the treatment with total triterpenoids from C. speciosa, including the down-regulation of the mRNA and protein expression levels of TLR4, MyD88, Bax and Bad, the protein expression levels of p-IKKß, p-IκBα, NLRP3, ASC, pro-caspase-1, caspase-1, TXNIP, pro-IL-1ß, pro-IL-18, cytochrome C, Apaf-1, cleaved-caspase-9, cleaved-caspase-3, cleaved-PARP-1 and nuclear NF-κB p65, reduction of p-IKKß/IKKß and p-IκBα/IκBα ratios and up-regulation of the mRNA and protein expression levels of Bcl-2 and Bcl-xl, up-regulation of pro-caspase-9, pro-caspace-3, cytosol NF-κB p65 protein expression levels and Bcl-2/Bax and Bcl-xl/Bad ratios in gastric tissue. These aforementioned results suggest that the total triterpenoids from C. speciosa have significant protective effects against CAG induced by Hp, and its mechanism may be related to enhancing the function of endogenous antioxidant system, suppressing the oxidative stress and inflammatory reaction induced by Hp, correcting lysosomal dysfunction and inflammatory activation of TLR4/NF-κB/NLRP3 inflammasome signaling pathway and thus inhibiting mitochondria-mediated apoptosis.


Assuntos
Gastrite , Helicobacter pylori , Rosaceae , Triterpenos , Animais , Gastrite/tratamento farmacológico , Camundongos , NF-kappa B/genética
4.
Mater Sci Eng C Mater Biol Appl ; 129: 112361, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34579880

RESUMO

Heap-up of α-synuclein (α-Syn) and its association with tau protein are esteemed to trigger the onset of Parkinson's disease (PD). The purpose of this study was to develop multi-functional liposomes incorporated with 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), cholesterol, 1,2-dimyristoyl-sn-glycero-3-phosphocholine and phosphatidylserine (PS) to load astragaloside IV (AS-IV) and nestifin-1 (NF-1), followed by grafting with wheat germ agglutinin (WGA) and leptin (Lep) (WGA-Lep-AS-IV-NF-1-PS-liposomes) to protect dopaminergic neurons from apoptosis. Experimental results showed that increasing the mole percentage of DSPC and PS enhanced the particle size, particle stability and entrapment efficiency of AS-IV and NF-1, and reduced the drug releasing rate. Strong affinity of NF-1 to PS was evidenced by nuclear magnetic resonance spectroscopy. WGA-Lep-AS-IV-NF-1-PS-liposomes diminished transendothelial electrical resistance and improved the capacity of propidium iodide, AS-IV and NF-1 to penetrate the blood-brain barrier (BBB). Immunocytochemical staining exhibited the ability of functionalized liposomes to target Lep receptor and α-Syn in MPP+-insulted SH-SY5Y cells. Western blots revealed a substantial reduction of α-Syn and phosphorylated tau protein in the anti-oxidative pathway through interaction with PS. During the course of treatment with WGA-Lep-AS-IV-NF-1-PS-liposomes, the combined activity of AS-IV and NF-1 and recognition capability simultaneously decreased the expression of Bax, and increased the expressions of Bcl-2, tyrosine hydroxylase and dopamine transporter. The liposomes carrying AS-IV and NF-1 can rescue degenerated neurons and are a promising formulation to achieve better PD management.


Assuntos
Lipossomos , Doença de Parkinson , Neurônios Dopaminérgicos , Humanos , Leptina , Doença de Parkinson/tratamento farmacológico , Fosfatidilserinas , Saponinas , Triterpenos , Aglutininas do Germe de Trigo , Proteínas tau
5.
Zhongguo Zhong Yao Za Zhi ; 46(17): 4314-4322, 2021 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-34581034

RESUMO

Bolbostemma paniculatum is a commonly used Chinese medicinal material effective in clearing heat, removing toxin, eliminating phlegm, and alleviating swelling. The anti-tumor activity it possesses makes it a research hotspot. At present, 76 compounds have been isolated from B. paniculatum, including triterpenoids, sterols, alkaloids, anthraquinones, organic acids, etc., with anti-tumor, antiviral, and immunosuppressive pharmacological activities. This study reviewed the research on the chemical constituents and pharmacological effects of B. paniculatum over the past 20 years, aiming to provide a scientific basis for the research on the pharmacodynamic material basis and promote the development and utilization of B. paniculatum.


Assuntos
Cucurbitaceae , Medicamentos de Ervas Chinesas , Triterpenos , Medicamentos de Ervas Chinesas/farmacologia , Edema
6.
Zhongguo Zhong Yao Za Zhi ; 46(17): 4334-4343, 2021 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-34581036

RESUMO

Xanthoceras sorbifolia, an excellent oil-rich woody species, has high comprehensive economic value in edible, medicinal, and ornamental fields. The chemical composition, pharmacological effect, and quality control of X. sorbifolia were introduced, and its development and application were reviewed in this study. As revealed by the previous research, the main chemical constituents of X. sorbifolia were triterpenoids, flavonoids, fatty acids, phenylpropanoids, steroids, phenolic acids, organic acids, etc. It possesses pharmacological effects, such as neuroprotection, bacteriostasis, anti-oxidation, anti-tumor, anti-inflammation, analgesia, anti-HIV, and anti-coagulation. X. sorbifolia is widely applied in medical, food, chemical industry, and other fields, and deserves in-depth research and development.


Assuntos
Sapindaceae , Triterpenos , Anti-Inflamatórios , Flavonoides , Pesquisa
7.
Zhongguo Zhong Yao Za Zhi ; 46(17): 4433-4437, 2021 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-34581047

RESUMO

The combination of normal-phase silica gel column chromatography, octadecyl silica(ODS) column chromatography, semi-preparative high performance liquid chromatography(HPLC), etc. was employed to isolate and purify the chemical components from Euphorbia resinifera, and 7 triterpenoids were separated from the ethanol extract of the medicinal materials. Their structures were identified by various spectroscopy methods as cycloartan-1,24-diene-3-one(1), cycloartan-1,24-diene-3-ol(2), 3ß-hydroxy-lanosta-8,24-diene-11-one(3), lnonotusane C(4), eupha-8,24-diene-3ß-ol-7,11-dione(5), eupha-24-methylene-8-ene-3ß-ol-7,11-dione(6), and eupha-8,24-diene-3ß,11ß-diol-7-one(7). Compounds 1 and 2 are new compounds, and compound 3 is obtained from nature for the first time.


Assuntos
Medicamentos de Ervas Chinesas , Euphorbia , Triterpenos , Estrutura Molecular
8.
Zhongguo Zhong Yao Za Zhi ; 46(18): 4730-4735, 2021 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-34581082

RESUMO

The present study aimed to explore the mechanism of the sweating of Dipsacus asper on content changes of triterpene sa-ponins by detecting the total triterpene saponins and the index component asperosaponin Ⅵ in the crude and sweated D. asper, and analyzing the differentially expressed proteins by isobaric tags for relative and absolute quantification(iTRAQ) combined with LC-MS/MS. After sweating, the content of total triterpene saponins decreased manifestly, while that of asperosaponin Ⅵ increased significantly. As revealed by the iTRAQ-LC-MS/MS analysis, 140 proteins with significant differential expression were figured out, with 50 up-regulated and 90 down-regulated. GO analysis indicated a variety of hydrolases, oxido-reductases, and transferases in the differential proteins. The results of activity test on two differentially expressed oxido-reductases were consistent with those of the iTRAQ-LC-MS/MS analysis. As demonstrated by the analysis of enzymes related to the triterpene saponin biosynthesis pathway, two enzymes(from CYP450 and UGT families, respectively, which are involved in the structural modification of triterpene saponins) were significantly down-regulated after sweating. The findings suggested that sweating of D. asper presumedly regulated triterpene saponins by affecting the expression of downstream CYP450 s and UGTs in the biosynthesis pathway of triterpene saponins of D. asper.


Assuntos
Dipsacaceae , Saponinas , Triterpenos , Cromatografia Líquida , Humanos , Sudorese , Espectrometria de Massas em Tandem
9.
Zhongguo Zhong Yao Za Zhi ; 46(18): 4744-4748, 2021 Sep.
Artigo em Chinês | MEDLINE | ID: mdl-34581084

RESUMO

Four new lanostane triterpenoids, 3ß-hydroxy-12α-methoxylanosta-7,9(11),24-triene(1), 3ß-hydroxy-12α-methoxy-24-methylene-lanost-7,9(11)-dien(2), 3,7-dioxo-lanosta-8,24-diene(3), and 3,7-dioxo-24-methylene-lanost-8-en(4), were isolated from the latex of Euphorbia resinifera with a variety of chromatography methods. Their structures were elucidated based on spectroscopic data and/or comparison with the data reported in previous research. Compounds 1, 2, and 4 showed moderate inhibition of LPS-induced NO production by RAW264.7, with IC_(50) of 30.4, 37.5, and 28.3 µmol·L~(-1), respectively.


Assuntos
Euphorbia , Triterpenos , Látex , Estrutura Molecular , Esteroides
10.
Chem Biol Interact ; 348: 109645, 2021 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-34516973

RESUMO

Semi-synthetic A-cycle modified triterpenic derivatives with A-cycle condensed with a heterocyclic fragment (compound 1) and fragmented A-ring (compound 2) were tested for cytotoxicity against several tumor cell cultures and doxorubicin (Dox)-resistant cell lines. The equal cytotoxicity of the tested compounds to the parental tumor cell lines (HBL-100, K562) and their resistant subclones (HBL-100/Dox, K562/i-S9) was revealed. The overexpression of ABCB1 (MDR1) gene and P-glycoprotein (P-gp) was confirmed for both resistant subclones of tumor cells. Compounds 1 and 2 were shown to inhibit the ABC-transporter gene expression (MDR1, MRP, MVP, and BCRP) and the transport of well-known P-gp substrate Rhodamine 123 from resistant cells. The docking of triterpenoids 1 and 2 into the drug binding site of P-gp revealed a similarity between the conformation of the tested triterpenoids and that of classical inhibitor verapamil, thus assuming these compounds to be more likely the inhibitors than the substrates of P-gp. Any tested triterpenic derivatives, when combined at non-toxic concentrations with doxorubicin, improved cytotoxic effect of the therapeutic drug against resistant subclones of tumor cells.


Assuntos
Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo , Antineoplásicos/química , Antineoplásicos/farmacologia , Resistencia a Medicamentos Antineoplásicos/efeitos dos fármacos , Triterpenos/química , Triterpenos/farmacologia , Linhagem Celular Tumoral , Humanos , Relação Estrutura-Atividade
11.
Appl Microbiol Biotechnol ; 105(19): 7353-7365, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34515845

RESUMO

The telomerase reverse transcriptase (TERT) is the core catalytic subunit of telomerase. Its canonical function is synthesizing telomeric repeats to maintain telomere length and chromosomal stability. Accumulating evidence suggests that TERT has other important fundamental functions in addition to its catalytic telomere repeat synthesis activity. However, the non-canonical roles of TERT independent of its enzymatic activity are not clear in filamentous fungi. In the present study, we characterized the GlTert gene in Ganoderma lucidum. The non-canonical roles of GlTert were explored using GlTert-silenced strains (Terti8 and Terti25) obtained by RNA interference. Silencing GlTert delayed the fungal growth, decreased the length between hyphal branches, and induced fungal resistance to oxidative stress in G. ludicum. Further examination revealed that the intracellular ROS (reactive oxygen species) levels were increased while the enzyme activities of the antioxidant systems (superoxide dismutase, catalase, glutathione peroxidase, and ascorbate peroxidase) were decreased in GlTert-silenced strains. In addition, silencing GlTert decreased the ganoderic acid (GA) biosynthesis of G. lucidum. Taken together, our results indicate that GlTert plays a fundamental function on fungal growth, oxidative stress, and GA biosynthesis in G. lucidum, providing new insights for the canonical functions of TERT in filamentous fungi. KEY POINTS: • GlTert affected fungal growth and hyphal branching of G. lucidum. • Silencing GlTert increased the intracellular ROS levels of G. lucidum. • GlTert regulated GA biosynthesis of G. lucidum.


Assuntos
Reishi , Telomerase , Estresse Oxidativo , Telomerase/genética , Triterpenos
12.
Phytomedicine ; 91: 153682, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34483017

RESUMO

BACKGROUND: Mogroside V, the main ingredient of Siraitia grosvenorii, has been proved to have therapeutic effects on pulmonary diseases. The specific mechanism still remains to be clarified, which hinders the potence of its medicinal value. PURPOSE: Serum and lung metabolomics based on LC-MS analysis were applied to explore the mechanism of mogroside V against lung inflammation. METHOD: In this study, balb/c mice were divided into control, model, mogeoside V and SH groups. We evaluated the protective effects of mogroside V on lung inflammation in asthmatic mice. Suhuang Zhike Jiaonang was used as positive drug. Metabolic profiles of serum and lung samples of mice in control, model and mogroside V groups were analyzed by LC-MS. RESULTS: Administration of mogroside V effectively relieved the expression of biochemical cytokines and lung inflammatory infiltration of asthmatic mice caused by ovalbumin (OVA). And visceral index of mice treated with mogroside V was close to control group. These results indicated that mogroside V ameliorated OVA-induced lung inflammation. LC-MS based metabolomics analysis demonstrated 6 main pathways in asthmatic mice including Vitamin B6 metabolism, Taurine and hypotaurine metabolism, Ascorbate and aldarate metabolism, Histidine metabolism, Pentose and glucuronate interconversions, Citrate cycle (TCA cycle) were regulated after using mogroside V. CONCLUSION: The study firstly elucidates the metabolic pathways regulated by mogroside V on lung inflammation through metabolomics, providing a theoretical basis for more sufficient utilization and compatibility of mogroside V.


Assuntos
Metabolômica , Pneumonia , Triterpenos/farmacologia , Animais , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Pulmão , Camundongos , Camundongos Endogâmicos BALB C , Ovalbumina , Pneumonia/induzido quimicamente , Pneumonia/tratamento farmacológico
13.
Ecotoxicol Environ Saf ; 225: 112746, 2021 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-34482064

RESUMO

Betulinic acid (BA), a pentacyclic triterpenoid, has been associated with several biological effects, such as antioxidant, anti-inflammatory and antiviral activities. Previous studies have demonstrated that BA has the ability to alleviate intestinal mucosal damage, however, the potential mechanism associated with the effect has not been reported. This study aimed to investigate the possible protective mechanism of BA against cyclophosphamide (CYP)-induced intestinal mucosal damage. Here, we found that BA pretreatment prevented intestinal mucosal barrier dysfuction from CYP-challenged mice by repairing the intestinal physical, chemical, and immune barriers. Moreover, BA treatment suppressed the CYP-induced oxidative stress by activating the nuclear factor erythroid 2 [NF-E2]-related factor (Nrf2) pathway blocked reactive oxygen species (ROS) accumulation. In addition, BA inhibited CYP-triggered intestinal inflammation through down-regulating the nuclear transcription factor kappa B (NF-κB)/mitogen-activating protein kinase (MAPK) pathways. Furthermore, BA pretreatment reduced intestinal apoptosis by blocking ROS-activated mitochondrial apoptotic pathway. Overall, the current study demonstrated the protective effect of BA against CYP-caused intestinal mucosal damage by regulating the Nrf2 and NF-κB/MAPK signalling pathways, which may provide new therapeutic targets to attenuate intestinal impairment and maintain intestinal health.


Assuntos
Fator 2 Relacionado a NF-E2 , Triterpenos , Animais , Ciclofosfamida/toxicidade , Mucosa Intestinal/metabolismo , Camundongos , Mitógenos/metabolismo , Fator 2 Relacionado a NF-E2/genética , Fator 2 Relacionado a NF-E2/metabolismo , NF-kappa B/metabolismo , Estresse Oxidativo , Triterpenos Pentacíclicos , Triterpenos/metabolismo , Triterpenos/farmacologia
15.
BMC Complement Med Ther ; 21(1): 219, 2021 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-34470625

RESUMO

BACKGROUND: Pears have been world-widely used as a sweet and nutritious food and a folk medicine for more than two millennia. METHODS: We conducted a review from ancient literatures to current reports to extract evidence-based functions of pears. RESULTS: We found that pears have many active compounds, e.g., flavonoids, triterpenoids, and phenolic acids including arbutin, chlorogenic acid, malaxinic acid, etc. Most of researchers agree that the beneficial compounds are concentrated in the peels. From various in vitro, in vivo, and human studies, the medicinal functions of pears can be summarized as anti-diabetic,-obese, -hyperlipidemic, -inflammatory, -mutagenic, and -carcinogenic effects, detoxification of xenobiotics, respiratory and cardio-protective effects, and skin whitening effects. Therefore, pears seem to be even effective for prevention from Covid-19 or PM2.5 among high susceptible people with multiple underlying diseases. CONCLUSION: For the current or post Covid-19 era, pears have potential for functional food or medicine for both of communicable and non-communicable disease.


Assuntos
Frutas/química , Alimento Funcional , Compostos Fitoquímicos/farmacologia , Pyrus/química , COVID-19 , Flavonoides , Humanos , Fenóis , Triterpenos
16.
Biol Res ; 54(1): 27, 2021 Sep 06.
Artigo em Inglês | MEDLINE | ID: mdl-34488902

RESUMO

BACKGROUND: Demethylzeylasteral (T-96) is a pharmacologically active triterpenoid monomer extracted from Tripterygium wilfordii Hook F (TWHF) that has been reported to exhibit anti-neoplastic effects against several types of cancer cells. However, the potential anti-tumour effects of T-96 against human Prostate cancer (CaP) cells and the possible underlying mechanisms have not been well studied. RESULTS: In the current study, T-96 exerted significant cytotoxicity to CaP cells in vitro and induced cell cycle arrest at S-phase in a dose-dependent manner. Mechanistically, T-96 promoted the initiation of autophagy but inhibited autophagic flux by inducing ROS-mediated endoplasmic reticulum (ER) stress which subsequently activated the extrinsic apoptosis pathway in CaP cells. These findings implied that T-96-induced ER stress activated the caspase-dependent apoptosis pathway to inhibit proliferation of CaP cells. Moreover, we observed that T-96 enhances the sensitivity of CaP cells to the chemotherapeutic drug, cisplatin. CONCLUSIONS: Taken together, our data demonstrated that T-96 is a novel modulator of ER stress and autophagy, and has potential therapeutic applications against CaP in the clinic.


Assuntos
Autofagia , Neoplasias da Próstata , Apoptose , Linhagem Celular Tumoral , Humanos , Masculino , Neoplasias da Próstata/tratamento farmacológico , Espécies Reativas de Oxigênio , Triterpenos
17.
Zhongguo Zhong Yao Za Zhi ; 46(12): 3123-3132, 2021 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-34467704

RESUMO

The chemical constituents from the leaves of Ilex guayusa were investigated. Sixteen triterpenoids were isolated from the 95% ethanol extract of dried leaves of I. guayusa by silica gel, Sephadex LH-20, and ODS column chromatographies and semi-prepa-rative HPLC. Those triterpenoids were identified by NMR, HR-MS, and literature analysis: 3ß-hydroxy-11α,12α-epoxy-24-nor-urs-4(23)-ene-28,13ß-olide(1), 3ß-hydroxy-24-nor-4(23),12-oleanadien-28-methyl ester(2), oleanolic acid(3), 3ß,28-dihydroxy-12-oleanene(4), 2α,3ß-dihydroxy-11α,12α-epoxy-24-'nor-olean-4(23)-ene-28,13ß-olide(5), ursolic acid(6), 3ß,23-dihydroxy ursolic acid(7), 3ß,28-dihydroxy-12-ursene(8), 3ß-28-nor-urs-12-ene-3,17-diol(9), 3ß-hydroxyurs-11-ene-28,13ß-olide(10), 13ß,28-epoxy-3ß-hydroxy-11-ursene(11), 3ß-hydroxy-28,28-dimethoxy-12-ursene(12), 3ß-hydroxy-24-nor-urs-4(23),12-dien-28-oic acid(13), 3ß-hydroxy-24-nor-urs-4(23),12-dien-28-methyl ester(14), 2α,3ß-dihydroxy-11α,12α-epoxy-24-nor-urs-4(23)-ene-28,13ß-olide(15) and 2α,3ß-dihydroxy-11α,12α-epoxy-24-nor-urs-4(23),20(30)-dien-28,13ß-olide(16). Compounds 1-2 were new compounds, and compounds 4-5, 7 and 9-16 were isolated from I. guayusa for the first time.


Assuntos
Medicamentos de Ervas Chinesas , Ilex guayusa , Ácido Oleanólico , Triterpenos , Estrutura Molecular , Folhas de Planta
18.
Zhongguo Zhong Yao Za Zhi ; 46(12): 3144-3149, 2021 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-34467706

RESUMO

The effect of intestinal flora changes on the pharmacokinetics of astragaloside Ⅳ in rats with type 2 diabetes mellitus was explored in this study. The rat model in preliminary experiment was established by high-sugar and high-fat diet combined with the intraperitoneal injection of low-dose streptozotocin(STZ). Rats were divided into model group, astragaloside Ⅳ group, berberine group and combination group(five rats in each group). After two weeks of gavage, the rats' feces was taken for 16 S rRNA sequencing of intestinal flora. Pharmacokinetic experiments were performed on astragaloside Ⅳ in the four groups one day after the preliminary experiment. Plasma samples were precipitated in methanol with ginsenoside Rb_1 as an internal standard, and the plasma concentrations of astragaloside Ⅳ at different time points were determined by UPLC-MS/MS. The chromatographic separation was performed on a Waters Acquity UPLC BEH-C_(18) column(2.1 mm×100 mm, 1.7 µm) via gradient elution. The mobile phase was acetonitrile(A) and 5 mmol·L~(-1) ammonium formate solution with 0.2% formic acid(B). The flow rate was 0.4 mL·min~(-1), the injection volume 5 µL and the column temperature 40 ℃. The mass spectrometry was carried out with electrospray ionization source(ESI) in multiple reaction monitoring and positive ion modes. The specificity, linearity range, accuracy, precision, stability and dilution effect of the method all met the requirements for the determination of astragaloside Ⅳ in plasma. Plasma concentration-time curves were plotted and relevant pharmacokinetic parameters were calculated by DAS 3.2.8. The results showed that the concentration of absorbed astragaloside Ⅳ increased within 0-3.95 h and began to decline since 3.95 h. After 36 h, the metabolism was complete. The area under the plasma concentration-time curve(AUC_(0-t)) and the peak concentration(C_(max)) of astragaloside Ⅳ were increased in the three administration groups compared with the model group, but without significant difference, which suggested that the pharmacokinetic characteristics of saponin components would not necessarily change after the drug-induced alteration of intestinal flora.


Assuntos
Diabetes Mellitus Tipo 2 , Microbioma Gastrointestinal , Saponinas , Animais , Cromatografia Líquida de Alta Pressão , Cromatografia Líquida , Ratos , Ratos Sprague-Dawley , Reprodutibilidade dos Testes , Espectrometria de Massas em Tandem , Triterpenos
19.
An Acad Bras Cienc ; 93(suppl 3): e20201351, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34468491

RESUMO

Obesity is a major risk factor for type 2 diabetes mellitus development and is characterized by an abnormal expansion of adipose tissue and low-grade chronic inflammation that contribute to insulin resistance. Although there are multiple treatments, most therapies can produce undesirable side effects and therefore, new and effective treatments with fewer side effects are necessary. Previously, we demonstrated that a natural extract from the leaves of Eucalyptus tereticornis (OBE100) has anti-inflammatory, hypoglycemic and hypolipidemic activities. The major compounds identified in OBE100 were three pentacyclic triterpenoids, ursolic acid, oleanolic acid, and ursolic acid lactone. Triterpenoids have shown multiples biological activities. This current study compared the biological effect produced by OBE100 with five different reconstituted mixtures of these triterpenoids. Different cell lines were used to evaluate cytotoxicity, reactive oxygen species production, inflammatory cytokine expression, glucose uptake induction, leptin and adiponectin expression, and lipid accumulation. OBE100 treatment was the most efficacious and none of the formulated triterpenoid mixtures significantly improved on this. Moreover, OBE100 was less toxic and reduced reactive oxygen species production. Our study showed that the proven beneficial properties of triterpenoids may be enhanced due to the interaction with minor secondary metabolites present in the natural extract improving their anti-inflammatory properties.


Assuntos
Diabetes Mellitus Tipo 2 , Eucalyptus , Resistência à Insulina , Triterpenos , Extratos Vegetais/farmacologia , Triterpenos/farmacologia
20.
Curr Issues Mol Biol ; 43(2): 932-940, 2021 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-34449548

RESUMO

Prostate cancer (PCa) is addressed as the second most common form of onco-threat worldwide and is usually considered as the major cause of mortality in men. Recent times have seen a surge in exploration of plant-derived components for alternative therapeutical interventions against different oncological malignancies. Dammarolic acid or Asiatic acid (AsA) is an aglycone asiaticoside that has been reported for its efficacy in several ailments including cancer. The current study aimed to investigate the anti-proliferative potency of AsA against human prostate cancer PC-3 cells. Purified AsA was diluted and PC-3 cells were exposed to 20, 40, and 80 µM concentration and incubated for 24 h. Post-exposure, PC-3 cells showcased a substantial loss of their viability at 20 µM (p < 0.05), moreover, this reduction in cell viability escalated proportionally with an increase in AsA at concentrations of 40 and 80 µM (p < 0.01; p < 0.001) respectively. AsA-impelled loss of cellular viability was also evident from the acridine orange-stained photomicrographs, which was also used to quantify the viable and apoptotic cells using Image J software. Additionally, quantification of ROS within PC-3 cells also exhibited an increase in DCF-DA-mediated fluorescence intensity post-exposure to AsA in a dose-dependent manner. AsA-induced apoptosis in PC-3 cells was shown to be associated with augmented activity of caspase-3 proportionally to the AsA concentrations. Thus, initially, this exploratory study explicated that AsA treatment leads to anti-proliferative effects in PC-3 cells by enhancing oxidative stress and inciting apoptosis en route to onset of nuclear fragmentation.


Assuntos
NF-kappa B/antagonistas & inibidores , Triterpenos Pentacíclicos/farmacologia , Neoplasias da Próstata/tratamento farmacológico , Neoplasias da Próstata/patologia , Anti-Infecciosos/farmacologia , Apoptose/efeitos dos fármacos , Caspase 3/metabolismo , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Masculino , NF-kappa B/metabolismo , Células PC-3 , Neoplasias da Próstata/metabolismo , Triterpenos/farmacologia
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