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1.
J Asian Nat Prod Res ; : 1-10, 2019 Dec 03.
Artigo em Inglês | MEDLINE | ID: mdl-31791147

RESUMO

Various bioactive polyketides have been found in Aloe barbadensis. However, the polyketide synthases (PKSs), which participate in biosynthesis of polyketides in A. barbadensis remain unknown. In this study, two type III PKSs (AbPKS1 and AbPKS2) were identified from A. barbadensis. AbPKS1 and AbPKS2 were able to utilize malonyl-CoA to yield heptaketides (TW93a and aloesone) and octaketides (SEK4 and SEK4b), respectively. AbPKS1 also exhibited catalytic promiscuity in recognizing CoA thioesters of aromatics to produce unusual polyketides. What Is more, a whole cell biocatalysis system with the capability of producing 26.4 mg/L of SEK4/SEK4b and 2.1 mg/L of aloesone was successfully established.

2.
J Asian Nat Prod Res ; : 1-7, 2019 Nov 18.
Artigo em Inglês | MEDLINE | ID: mdl-31738087

RESUMO

Bistachybotrysin K (1), one new phenylspirodrimane dimer with a central 6/7 oxygen heterocycle core, was isolated from the fungus Stachybotrys chartarum CGMCC 3.5365. Its structure was elucidated by extensive spectroscopic data and single-crystal X-ray diffraction. Compound 1 showed significant cytotoxicity against human tumor cell lines HCT116, NCI-H460, BGC823, Daoy, and HepG2 with IC50 values in the range of 1.1-4.7 µM.

3.
J Asian Nat Prod Res ; 21(9): 887-894, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-30614271

RESUMO

Three new phenylspirodrimanes derivatives named stachybotrysins H and I (1 and 2) and stachybotrin E (3), together with one known compound stachybotrylactam (4), were isolated from Stachybotrys chartarum CGMCC 3.5365. Their structures were determined by extensive NMR data and mass spectroscopic analysis. Compounds 1 and 2 showed inhibitory effect towards potassium channel Kv1.3 with IC50 values of 13.4 and 10.9 µM, respectively.


Assuntos
Canal de Potássio Kv1.3/antagonistas & inibidores , Compostos de Espiro/química , Stachybotrys/química , Animais , Células CHO , Linhagem Celular , Cricetinae , Cricetulus
4.
J Asian Nat Prod Res ; 20(7): 605-614, 2018 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-29989425

RESUMO

Glucuronidation is an important and popular metabolic reaction in vivo of drugs. The further evaluation of biological activity and toxicity of glucuronides is necessary in the course of the drug research and development. However, the synthesis of glucuronides is limited by the lack of efficient approach. Herein, we have developed a new glucuronide synthesis method using plant uridine diphosphate-dependent glucuronosyltransferases (UGTs), UGT88D4, UGT88D7, and EpGT8, enabling the convenient preparation for corresponding O-glucuronide metabolites (1a, 2a, 3a, and 3b) in milligram scale of two neurological active agents, IMM-H004 (1) and FLZ (2). Their structures were characterized by spectroscopic data analyses.


Assuntos
Glucuronídeos/síntese química , Glucuronosiltransferase/metabolismo , Plantas/enzimologia , Clonagem Molecular , Glucuronosiltransferase/química , Glucuronosiltransferase/genética , Concentração de Íons de Hidrogênio , Espectroscopia de Ressonância Magnética , Metais/química , Estrutura Molecular , Espectrometria de Massas por Ionização por Electrospray , Temperatura Ambiente
5.
J Asian Nat Prod Res ; 20(9): 844-851, 2018 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-29119831

RESUMO

Two new lanostane triterpenoids (1 and 2), two new ergostane-type steroids (3 and 4) together with two known lanostane triterpenoids (5 and 6) and one known steroid (7) were isolated from the cultured mycelia of Ganoderma capense (CGMCC 5.71). Their structures were determined on the basis of extensive spectroscopic (HRESIMS, 1D NMR, 2D NMR) data analyses. Compound 1 exhibited moderate cytotoxic activity against the human cancer cell line NCI-H1650 with an IC50 value of 22.3 µM, and 7 displayed cytotoxic activity against the human cancer cell line HCT116 with an IC50 value of 17.4 µM. In addition, compounds 2, 3, 5, and 6 displayed weak anti-HIV activity with IC50 values of 23.5, 46.7, 21.6, and 30.1 µM, respectively.


Assuntos
Ganoderma/química , Micélio/química , Esteroides/química , Triterpenos/química , Ganoderma/metabolismo , Estrutura Molecular , Micélio/metabolismo , Esteroides/metabolismo
6.
Zhongguo Zhong Yao Za Zhi ; 42(12): 2323-2328, 2017 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-28822187

RESUMO

The glycosides of 4'-demethylepipodophyllotoxin (DMEP) possess various pharmacological activities; however, the chemical synthesis of these glycosides faces challenges in regioselectivity, stereoselectivity, and the protection and de-protection of functional groups. In this work, a novel glycosyltransferase (GT) gene AbGT5 from Aloe barbadensis was successfully cloned, heterogeneously expressed and purified. Recombinant AbGT5 was able to catalyze the glycosylation of DMEP and the glycosylated product, which was separated from the preparative scale reaction, was characterized as DMEP 4'-O-ß-D-glucoside via MS, 1H-NMR, 13C-NMR, HSQC and HMBC. According to the investigations of enzyme properties, AbGT5 show the highest activity around 20 ℃ in the buffer of pH 9.0, and it was independent of divalent metal ions. Under the optimum conditions, the conversion rate of DMEP can reach 80%. Above all, in this work the enzymatic glycosylation of DMEP was achieved with high efficiency by the novel GT AbGT5.


Assuntos
Glucosídeos/química , Glicosídeos/química , Glicosiltransferases/metabolismo , Podofilotoxina/análogos & derivados , Aloe/enzimologia , Aloe/genética , Glicosilação , Glicosiltransferases/genética , Podofilotoxina/química
7.
J Asian Nat Prod Res ; 19(6): 541-549, 2017 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-28395517

RESUMO

Five monoterpenoids were isolated from the endophytic fungus Periconia sp. F-31, including three new carene-type monoterpenoids, 2-carene-5,8-diol (1), 2-carene-8,10-diol (2), 2-carene-8-acetamide (3), one new menthene-type monoterpenoid 8-hydroxy-1,7-expoxy-2-menthene (4), and one known monoterpenoid anethofuran (5). The structures of all compounds were elucidated based on a comprehensive spectroscopic data analysis, electronic circular dichroism (ECD), and calculated ECD.


Assuntos
Antineoplásicos/isolamento & purificação , Ascomicetos/química , Monoterpenos/isolamento & purificação , Antineoplásicos/química , Antineoplásicos/farmacologia , Dicroísmo Circular , Cristalografia por Raios X , Ensaios de Seleção de Medicamentos Antitumorais , Estrutura Molecular , Monoterpenos/química , Monoterpenos/farmacologia , Ressonância Magnética Nuclear Biomolecular
8.
J Asian Nat Prod Res ; 19(10): 1028-1035, 2017 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-28145126

RESUMO

A new steroid glucoside (1), along with nine known steroids (2-10) and four known sorbicillinoids (11-14), were isolated from the endophytic fungus Trichoderma sp. Xy24. Their structures were elucidated on the basis of spectroscopic data analyses and by comparison with reported data. Compounds 3, 5-7, 9, 10, and 13 exhibited significant inhibitory effects on HIV-1 virus with IC50 values ranging 1.9-9.3 µM; compounds 10, 13, and 14 showed potent inhibitory activity on LPS-induced NO production in BV2 microglia cells with inhibitory rates of 108.2, 100, and 75.1% at 10 µM, respectively. In addition, compound 10 displayed moderate cytotoxicity against BCG823 and HePG2 cell lines with IC50 values of 11.1 and 17.7 µM, respectively.


Assuntos
Glucosídeos/isolamento & purificação , Glucosídeos/farmacologia , Esteroides/isolamento & purificação , Esteroides/farmacologia , Trichoderma/química , Anti-Inflamatórios não Esteroides/farmacologia , Glucosídeos/química , Células HCT116 , HIV-1/efeitos dos fármacos , Células Hep G2 , Humanos , Concentração Inibidora 50 , Microglia/efeitos dos fármacos , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Paclitaxel/farmacologia , Esteroides/química
9.
J Asian Nat Prod Res ; 19(7): 651-658, 2017 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-27835936

RESUMO

Three new sesquiterpenoids trichoacorenols B-C and cyclonerodiol B (1-3), along with three known ones (4-6), were isolated from the mangrove plant endophytic fungus Trichoderma sp. Xy24 using various column chromatography techniques. The structures of these compounds were determined on the basis of extensive spectroscopic data analyses. Compounds 1, 2, 4, and 5 were four acorane sesquiterpenes, 3 and 6 were two monocyclic sesquiterpenediols. Compounds 3 and 5 exhibited significant neural anti-inflammatory activity by inhibiting LPS-induced NO production in BV2 cells with the inhibitory rates of 75.0% and 39.2% at 0.1 µM, respectively, which are more potent than curcumin, a positive control with the inhibitory rate of 21.1% at 0.1 µM.


Assuntos
Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Sesquiterpenos/isolamento & purificação , Sesquiterpenos/farmacologia , Trichoderma/química , Animais , Anti-Inflamatórios/química , Curcumina/farmacologia , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Óxido Nítrico/biossíntese , Rhizophoraceae/microbiologia , Sesquiterpenos/química
10.
Zhongguo Zhong Yao Za Zhi ; 41(24): 4568-4571, 2016 Dec.
Artigo em Chinês | MEDLINE | ID: mdl-28936839

RESUMO

Secoisolariciresinol dehydrogenase (SDH) is a key enzyme involved in the biosynthetic pathway of podophyllotoxin.In this study, two SDH candidate genes,SO282 and SO1223, were cloned from callus of Dysosma versipellis by homology-based PCR and rapid amplification of cDNA end (RACE).The SDH candidate genes were expressed in Escherichia coli and the subsequent enzyme assay in vitro showed that recombinant SO282 had the SDH activity. These results pave the way to the follow-up investigation of the biosynthetic of podophyllotoxin.


Assuntos
Berberidaceae/enzimologia , Álcool Oxidorredutases Dependentes de NAD(+) e NADP(+)/genética , Proteínas de Plantas/genética , Berberidaceae/genética , Clonagem Molecular , DNA Complementar , Podofilotoxina/biossíntese
11.
Zhongguo Gu Shang ; 27(7): 545-50, 2014 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-25338438

RESUMO

OBJECTIVE: To investigate the therapeutic effects of manipulative reduction for calcaneal fractures. METHODS: From January 2009 to June 2012, 53 cases (60 affected feet) of Sanders type I-IV calcaneal fractures were treated by manipulative reduction and external fixation with cardboard splint,including 45 males and 8 females with an average age of (33.5 +/- 1.54) years old ranging from 18 to 65. The course of disease ranged 0.5 h to 7 d. Before treatment the feet were swelling, ache and activity limitation in evidence, some feet were wide flat deformity, the cortical bone was broken in the imaging examination. All selected cases were evaluated using Creighton-Nebraska health foundation assessment scale for fractures of calcaneus. RESULTS: All cases were followed up at 12 months after treatment, 13 feet got excellent curative effect, 34 good, 11 moderate and 2 poor. CONCLUSION: Manipulative reduction for Sanders type I-IV calcaneal fractures could get excellent curative effect. Manipulative reduction for calcaneal fractures could avoid surgical trauma while assure high curative effects. Manipulative reduction is not only economical and easy therapy, but also can restore maximum function of the calcaneus with few complications and facilitate early rehabilitation of ankle and joint function.


Assuntos
Calcâneo/lesões , Fixadores Externos , Fraturas Ósseas/cirurgia , Manipulação Ortopédica/métodos , Contenções , Adolescente , Adulto , Idoso , Calcâneo/cirurgia , Feminino , Fraturas Ósseas/reabilitação , Humanos , Masculino , Pessoa de Meia-Idade
12.
Zhongguo Zhong Yao Za Zhi ; 39(11): 2039-42, 2014 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-25272838

RESUMO

Naringenin (1) was transformed to three metabolites (2-4) by Mucor sp. Based on LCMS(n)-IT-TOF and NMR spectroscopic data, 2-4 were identified as naringenin-7-O-sulphate, naringenin-4'-O-sulphate, and naringenin-5-O-sulphate, respectively. These results might provide hints to the mammalian/human metabolism of naringenin.


Assuntos
Medicamentos de Ervas Chinesas/metabolismo , Flavanonas/metabolismo , Mucor/metabolismo , Sulfatos/metabolismo , Biotransformação , Medicamentos de Ervas Chinesas/química , Flavanonas/química , Espectroscopia de Ressonância Magnética , Estrutura Molecular
13.
Zhongguo Gu Shang ; 27(6): 491-5, 2014 Jun.
Artigo em Chinês | MEDLINE | ID: mdl-25241469

RESUMO

OBJECTIVE: To explore clinical effects of manipulative reduction with minimally invasive percutaneous plate osteosynthesis in treating distal tibiofibular fractures. METHODS: From 2009 to 2011, 60 patients with distal tibiofibular fractures were treated by manipulative reduction with minimally invasive percutaneous plate osteosynthesis. Among them, there were 32 males and 28 females aged from 14 to 70 years old with an average of 41.22 +/- 2.06. According to AO classification of fractures,5 cases were type A1, 22 cases were type A2,21 cases were type A3 and 12 cases were type C1. Operation time, blood loss,time of callus and fracture healing were observed, Mazur scoring of ankle joint were used to evaluate therapeutic. RESULTS: Fifty-eight incisions were healed at stage I ,and 2 cases were infected at distal tibial. Operation time was with an average of (62.34 +/- 5.66) min ranged 45 to 90 min;blood loss was 30 to 150 ml with an average of (80.57 +/- 5.59) ml;formation of callus appeared from 4 to 12 weeks,with an average of (8.24 +/- 2.06) weeks, and fracture healing time was from 3 to 6 months, with an average of (4.50 +/- 1.13) months. According to Mazur scoring of ankle joint 40 cases got excellent results, 18 good, and 2 fair. CONCLUSION: Manipulative reduction with minimally invasive percutaneous plate osteosynthesis can obtain reliable fixation. It is a good choice of treating distal tibiofibular fractures by protecting blood supply of fractures.


Assuntos
Fraturas da Tíbia/cirurgia , Adolescente , Adulto , Idoso , Placas Ósseas , Feminino , Fixação Interna de Fraturas/instrumentação , Humanos , Masculino , Pessoa de Meia-Idade , Procedimentos Cirúrgicos Minimamente Invasivos , Resultado do Tratamento , Adulto Jovem
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