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1.
Nanotechnology ; 2024 Jul 22.
Article in English | MEDLINE | ID: mdl-39038472

ABSTRACT

One-step direct laser writing process has been an efficient route for constructing flexible metal structures. However, the effect of laser wavelength on the structuring process remains unclear, thus limiting the universal manufacturing process development. In this work, the feasibility of one-step writing flexible Cu structures with different wavelength continuous diode lasers has been verified. Here, photothermal reaction dominate in the decomposition of the reducing agent to form copper structures. Difference in the wavelength mainly affect the photothermal reaction amplitude for structuring, resulting in a variation in the formation of Cu structures. At our processing conditions, the photothermal reaction induced by 532 nm laser is higher than 808 nm laser, a higher reducing-joining degree of Cu structure can be achieved by 532 nm laser. This results in a superior conductivity, adhesion, and bendability of Cu structures fabricated by 532 nm laser than that of 808 nm laser. Further, strain sensor that can detect different bending angles and bending frequencies have been fabricated by 532 nm laser-written structures to demonstrate their practical application.

2.
Mol Biol Rep ; 51(1): 810, 2024 Jul 13.
Article in English | MEDLINE | ID: mdl-39001942

ABSTRACT

Carotenoids, natural tetraterpenoids found abundantly in plants, contribute to the diverse colors of plant non-photosynthetic tissues and provide fragrance through their cleavage products, which also play crucial roles in plant growth and development. Understanding the synthesis, degradation, and storage pathways of carotenoids and identifying regulatory factors represents a significant strategy for enhancing plant quality. Chromoplasts serve as the primary plastids responsible for carotenoid accumulation, and their differentiation is linked to the levels of carotenoids, rendering them a subject of substantial research interest. The differentiation of chromoplasts involves alterations in plastid structure and protein import machinery. Additionally, this process is influenced by factors such as the ORANGE (OR) gene, Clp proteases, xanthophyll esterification, and environmental factors. This review shows the relationship between chromoplast and carotenoid accumulation by presenting recent advances in chromoplast structure, the differentiation process, and key regulatory factors, which can also provide a reference for rational exploitation of chromoplasts to enhance plant quality.


Subject(s)
Carotenoids , Gene Expression Regulation, Plant , Plastids , Plastids/metabolism , Carotenoids/metabolism , Plants/metabolism , Plants/genetics , Plant Proteins/metabolism , Plant Proteins/genetics , Plant Development/genetics , Cell Differentiation
3.
ACS Appl Mater Interfaces ; 16(8): 10496-10507, 2024 Feb 28.
Article in English | MEDLINE | ID: mdl-38377380

ABSTRACT

With the flexibilization tendency of traditional electronics, developing sensing devices for the low-temperature field is demanding. Here, we fabricated a flexible copper-based thermistor by a laser direct writing process with Cu ion precursors. The copper-based thermistor performs with excellent temperature sensing ability and high stability under different environments. We discussed the effect of laser power on the temperature sensitivity of the copper-based thermistor, explained the sensing mechanism of the as-written copper-based films, and fabricated a temperature sensor array for realizing temperature management in a specific zone. All of the investigations have demonstrated that such copper-based thermistors can be used as candidate devices for low-temperature sensing fields.

4.
Mitochondrial DNA B Resour ; 8(5): 565-569, 2023.
Article in English | MEDLINE | ID: mdl-37200681

ABSTRACT

The mitochondrial genome of Camellia nitidissima was sequenced by Illumina and Pacbio sequencing. The results of sequences showed that a total length was 949,915 bp, and the GC content was 45.7% in assembled mitochondrial genome of C. nitidissima. 71 unigenes had been found, including 36 coding proteins and 35 non-coding proteins. Subsequently, the phylogenetic tree was built on 24 plants with the maximum-likelihood method, which had high bootstrap value and fited to the angiosperm phylogeny group classification (APG IV). The study's findings unravel the taxonomic status of C. nitidissima and benefit the evolution study.

5.
Gene ; 850: 146924, 2023 Jan 20.
Article in English | MEDLINE | ID: mdl-36191826

ABSTRACT

Flavonoids are the main medicinal ingredients in Camellia nitidissima, but the regulatory mechanism of flavonoid biosynthesis in flowers is unclear; therefore, the flavonoids in C. nitidissima have not been effectively used. The present study performed full-length transcriptome sequencing of C. nitidissima flower. Furthermore, the reported RNA-sequencing data of C. nitidissima petals were reanalyzed using the full-length transcriptome as a reference, and the regulatory mechanism of flavonoid synthesis in petals was elucidated. The analysis identified 43,350 isoforms annotated in non-redundant protein (Nr), Kyoto Encyclopedia of Genes and Genomes (KEGG), EuKaryotic Orthologous Groups (KOG), and Swiss-Prot databases, among which 34,602 aligned to Camellia sinensis genes. A total of 11,857 differentially expressed genes (DEGs), including 112 related to flavonoid synthesis, were identified by pairwise comparison. Subsequently, analysis of the phylogeny and the conserved motifs of R2R3-MYB using the proteins sequences identified three R2R3-MYB transcription factors that regulated flavonoid biosynthesis. Weighted gene co-expression network analysis (WGCNA) identified phenylalanine ammonia-lyase (PAL) and 4-coumarate: CoA ligase(4CL) as the hub genes and showed that bHLH79 interacted with PAL. Finally, validated the expression of seven DEGs involved in flavonoid biosynthesis using real-time quantitative PCR (qRT-PCR). Thus, the present study generated and used the full-length transcriptome as the reference to analyze the transcriptome of petals and proposed a possible regulatory mechanism of flavonoid synthesis in C. nitidissima. The study's findings unravel the genetic mechanisms underlying flavonoid synthesis and suggest candidate genes for the genetic improvement of C. nitidissima.


Subject(s)
Camellia , Transcriptome , Transcriptome/genetics , Camellia/genetics , Gene Expression Regulation, Plant , Phenylalanine Ammonia-Lyase/genetics , Flavonoids/genetics , Transcription Factors/genetics , Transcription Factors/metabolism , RNA , Ligases/genetics , Ligases/metabolism , Coenzyme A/genetics , Coenzyme A/metabolism
6.
Front Genet ; 13: 1048264, 2022.
Article in English | MEDLINE | ID: mdl-36386825

ABSTRACT

Wasabi (Eutrema japonicum) is one of the most famous vegetable crops in the family Brassicaceae. However, a limited genomic resource is available, which hinders genomic breeding and understanding of the genetic basis of vital traits. Here, we generated the genome assembly of wasabi using the hybrid genome assembly strategy, which combined the Nanopore long reads and Illumina reads. The genome assembly contains 687M bp and 39,534 high-quality annotated gene models. Besides, we annotated 68.85% of the genomic sequences as repetitive elements, including 43.72% of retrotransposons and 18.99% of DNA transposons. Using the customized pipeline, we also generated the complete organelle genomes of wasabi. This reference genome could provide essential genomic resources for evolution, breeding, and exploring the unique biological traits of wasabi.

7.
Mitochondrial DNA B Resour ; 7(9): 1645-1647, 2022.
Article in English | MEDLINE | ID: mdl-36147374

ABSTRACT

Vincetoxicum junzifengense B.J. Ye and S.P. Chen 2022 is a newly described species which belongs to the genus Vincetoxicum in the family Apocynaceae. The complete plastid genome of Vincetoxicum junzifengense B.J. Ye and S.P. Chen 2022 was determined and analyzed in this study. The total chloroplast genome was 159,666 bp in length, consisting of a large single-copy region of 90,565 bp, a small single-copy region of 19,691 bp, and two inverted repeat regions of 24,705 bp. The genome contained 131 genes, including 85 protein-coding genes, 37 transfer RNA genes, and eight ribosomal RNA genes. Phylogenetic analysis indicated that V. junzifengense is sister to V. versicolor.

8.
Nanomicro Lett ; 13(1): 184, 2021 Aug 31.
Article in English | MEDLINE | ID: mdl-34463821

ABSTRACT

Integrating construction and reconstruction of highly conductive structures into one process is of great interest in developing and manufacturing of electronics, but it is quite challenging because these two involve contradictive additive and subtractive processes. In this work, we report an all-laser mask-less processing technology that integrates manufacturing, modifying, and restoring of highly conductive Cu structures. By traveling a focused laser, the Cu patterns can be fabricated on the flexible substrate, while these as-written patterns can be selectively erased by changing the laser to a defocused state. Subsequently, the fresh patterns with identical conductivity and stability can be rewritten by repeating the writing step. Further, this erasing-rewriting process is also capable of repairing failure patterns, such as oxidation and cracking. Owing to the high controllability of this writing-erasing-rewriting process and its excellent reproducibility for conductive structures, it opens a new avenue for rapid healing and prototyping of electronics.

9.
Mol Biol Rep ; 48(5): 3903-3912, 2021 May.
Article in English | MEDLINE | ID: mdl-34052979

ABSTRACT

Camellia nitidissima Chi. is an ornamental plant of the genus Camellia L. Its flowers contain a lot of flavonoids and polyphenols. Flavonoid 3'-hydroxylase (F3'H) plays an important role in the synthesis of flavonoids, polyphenols and anthocyanins. We used PCR amplification, quantitative PCR, High-performance liquid chromatography, subcellular localization, and agrobacterium-mediated leaf disk method to study the the function of CnF3'H. The full length of CnF3'H was 1859 bp (GenBank code: HQ290518.1), with an open reading frame of 1577 bp, and encoded 518 amino acid. A phylogenetic tree analysis showed that CnF3'H was closely related to Camellia sinensis L. and C. sinensis cultivar Zhonghuang. CnF3'H was expressed in flowers, leaves, fruits, sepals, petals and stamens of C. nitidissima, and during the flowering process the expression level in flower decreased initially and then increased. CnF3'H expression was significantly positive correlated with polyphenol contents in C. nitidissima. A CnF3'H-EGFP expression vector was constructed to do the subcellular localization, we found that CnF3'H was obviously localized in the nuclear envelope and cytomembrane. In transgenic tobacco flowers, the total polyphenol content and various polyphenol constituents were significantly increased with high CnF3'H expression level, while total flavonoid contents and some flavonol constituents were increased slightly. These findings suggest that CnF3'H promotes the synthesis of polyphenols better than flavonoids.


Subject(s)
Camellia/metabolism , Cytochrome P-450 Enzyme System/physiology , Anthocyanins/metabolism , China , Chromatography, High Pressure Liquid/methods , Cytochrome P-450 Enzyme System/metabolism , Flavonoids/metabolism , Flowers/metabolism , Gene Expression Regulation, Plant/genetics , Mixed Function Oxygenases/metabolism , Phylogeny , Plant Leaves/metabolism , Plant Proteins/genetics , Polyphenols/metabolism
10.
Genes (Basel) ; 11(11)2020 11 12.
Article in English | MEDLINE | ID: mdl-33198369

ABSTRACT

Plant secondary metabolism is complex in its diverse chemical composition and dynamic regulation of biosynthesis. How the functional diversification of enzymes contributes to the diversity is largely unknown. In the flavonoids pathway, dihydroflavonol 4-reductase (DFR) is a key enzyme mediating dihydroflavanol into anthocyanins biosynthesis. Here, the DFR homolog was identified from Camellia nitidissima Chi. (CnDFR) which is a unique species of the genus Camellia with golden yellow petals. Sequence analysis showed that CnDFR possessed not only conserved catalytic domains, but also some amino acids peculiar to Camellia species. Gene expression analysis revealed that CnDFR was expressed in all tissues and the expression of CnDFR was positively correlated with polyphenols but negatively with yellow coloration. The subcellular localization of CnDFR by the tobacco infiltration assay showed a likely dual localization in the nucleus and cell membrane. Furthermore, overexpression transgenic lines were generated in tobacco to understand the molecular function of CnDFR. The analyses of metabolites suggested that ectopic expression of CnDFR enhanced the biosynthesis of polyphenols, while no accumulation of anthocyanins was detected. These results indicate a functional diversification of the reductase activities in Camellia plants and provide molecular insights into the regulation of floral color.


Subject(s)
Alcohol Oxidoreductases/genetics , Alcohol Oxidoreductases/metabolism , Camellia/metabolism , Polyphenols/biosynthesis , Anthocyanins/biosynthesis , Anthocyanins/genetics , Camellia/genetics , Cell Membrane/enzymology , Cell Nucleus/enzymology , Flowers/genetics , Flowers/metabolism , Gene Expression Regulation, Plant , Phylogeny , Plant Proteins/genetics , Plant Proteins/metabolism , Plants, Genetically Modified/genetics , Polyphenols/genetics , Secondary Metabolism , Nicotiana/genetics , Nicotiana/metabolism
11.
Aging Clin Exp Res ; 32(5): 769-779, 2020 May.
Article in English | MEDLINE | ID: mdl-31175606

ABSTRACT

BACKGROUND: Selegiline or levodopa treatment has been suggested as a therapeutic method for Parkinson's disease (PD) in many clinical trial reports. However, the combined effects of two drugs still remain controversial. The aim of this report was to evaluate the clinical efficacy and safety of selegiline plus levodopa (S + L) combination therapy in the treatment of PD compared to that of L monotherapy, to provide a reference resource for rational drug use. METHODS: Randomized controlled trials (RCTs) of S + L for PD published up to September, 2018 were searched. Mean difference (MD), odds ratio (OR), and 95% confidence interval (CI) were calculated and heterogeneity was assessed with the I2 test. Sensitivity analysis was also performed. The outcomes measured were as follows: the unified Parkinson's disease rating scale (UPDRS) scores, modified Webster score, adverse events and mortality. RESULTS: Fourteen RCTs with 2008 participants were included. Compared with L monotherapy, the pooled effects of S + L combination therapy on UPDRS score were (eleven trials; MD - 7.00, 95% CI - 8.35 to - 5.65, P < 0.00001) for total UPDRS score (nine trials; MD - 5.74, 95% CI - 7.71 to - 3.77, P < 0.00001) for motor UPDRS score (seven trials; MD - 1.61, 95% CI - 2.18 to - 1.04, P < 0.00001) for activities of daily living UPDRS score (three trials; MD - 0.38, 95% CI - 0.61 to - 0.14, P = 0.002) for mental UPDRS score. The Webster score showed significant decrease in the S + L combination therapy compared to L monotherapy (four trials; MD - 5.71, 95% CI - 7.11 to - 4.32, P < 0.00001). Compared with L monotherapy, S + L combination therapy did not increase the number of any adverse events significantly in PD patients (ten trials; OR 1.58, 95% CI 0.83-3.00, P = 0.16). CONCLUSIONS: S + L combination therapy is superior to L monotherapy for the improvement of clinical symptoms in PD patients. Moreover, the safety profile of S + L combination therapy is comparable with that of L monotherapy.


Subject(s)
Levodopa/therapeutic use , Parkinson Disease/drug therapy , Selegiline/therapeutic use , Activities of Daily Living , Combined Modality Therapy , Drug Therapy, Combination , Humans , Mental Status and Dementia Tests , Treatment Outcome
12.
Nanoscale ; 12(2): 563-571, 2020 Jan 02.
Article in English | MEDLINE | ID: mdl-31725146

ABSTRACT

Flexible conductive structures are essential for the fabrication of commercial integrated electronic devices. Developing efficient processes for manufacturing these structures with high conductivity and stability is significant. Based on a modifiable cost-effective Cu-based ionic liquid precursor, here we present an in situ laser patterning technique to manufacture flexible electrodes. The fabricated Cu structure has excellent conductivity, approximately comparable to bulk Cu, while its oxidation resistance could be further enhanced through introducing an additional carbon source to form a Cu@C microstructure. The chemical and electrical stabilities are evaluated. This method provides a possible bottom-up route for manufacturing microelectronic devices in one step, as we demonstrated through a flexible heater.

13.
Front Plant Sci ; 8: 1545, 2017.
Article in English | MEDLINE | ID: mdl-28936220

ABSTRACT

The golden camellia, Camellia nitidissima Chi., is a well-known ornamental plant that is known as "the queen of camellias" because of its golden yellow flowers. The principal pigments in the flowers are carotenoids and flavonol glycosides. Understanding the biosynthesis of the golden color and its regulation is important in camellia breeding. To obtain a comprehensive understanding of flower development in C. nitidissima, a number of cDNA libraries were independently constructed during flower development. Using the Illumina Hiseq2500 platform, approximately 71.8 million raw reads (about 10.8 gigabase pairs) were obtained and assembled into 583,194 transcripts and 466, 594 unigenes. A differentially expressed genes (DEGs) and co-expression network was constructed to identify unigenes correlated with flower color. The analysis of DEGs and co-expressed network involved in the carotenoid pathway indicated that the biosynthesis of carotenoids is regulated mainly at the transcript level and that phytoene synthase (PSY), ß -carotene 3-hydroxylase (CrtZ), and capsanthin synthase (CCS1) exert synergistic effects in carotenoid biosynthesis. The analysis of DEGs and co-expressed network involved in the flavonoid pathway indicated that chalcone synthase (CHS), naringenin 3-dioxygenase (F3H), leucoanthocyanidin dioxygenase(ANS), and flavonol synthase (FLS) play critical roles in regulating the formation of flavonols and anthocyanidin. Based on the gene expression analysis of the carotenoid and flavonoid pathways, and determinations of the pigments, we speculate that the high expression of PSY and CrtZ ensures the production of adequate levels of carotenoids, while the expression of CHS, FLS ensures the production of flavonols. The golden yellow color is then the result of the accumulation of carotenoids and flavonol glucosides in the petals. This study of the mechanism of color formation in golden camellia points the way to breeding strategies that exploit gene technology approaches to increase the content of carotenoids and flavonol glucosides and to decrease anthocyanidin synthesis.

14.
Front Plant Sci ; 7: 1956, 2016.
Article in English | MEDLINE | ID: mdl-28082999

ABSTRACT

Correct identification of medicinal plant ingredients is essential for their safe use and for the regulation of herbal drug supply chain. Loop-mediated isothermal amplification (LAMP) is a recently developed approach to identify herbal medicine species. This novel molecular biology technique enables timely and accurate testing, especially in settings where infrastructures to support polymerase chain reaction facilities are lacking. Studies that used this method have altered our view on the extent and complexity of herbal medicine identification. In this review, we give an introduction into LAMP analysis, covers the basic principles and important aspects in the development of LAMP analysis method. Then we presented a critical review of the application of LAMP-based methods in detecting and identifying raw medicinal plant materials and their processed products. We also provide a practical standard operating procedure (SOP) for the utilization of the LAMP protocol in herbal authentication, and consider the prospects of LAMP technology in the future developments of herbal medicine identification and the challenges associated with its application.

15.
Carbohydr Polym ; 114: 514-520, 2014 Dec 19.
Article in English | MEDLINE | ID: mdl-25263921

ABSTRACT

Mo (VI)-imprinted chitosan (CTS)/triethanolamine (TEA) gel beads (Mo (VI)-ICTGBs) (ICTGBs=imprinted chitosan triethanolamine gel beads) were prepared by using ion-imprinted technology, in which TEA and molybdate solution were used in coagulation bath. The spectrum of FT-IR implies that bonding are formed between TEA and the primary hydroxyl of CTS, and ion gel reaction happen between CTS and molybdate; XRD patterns also prove the change among CTS, TEA and molybdate. SEM images and N2 adsorption show that the surface area increases obviously after eluting Mo (VI) ions. The adsorption isotherm of Mo (VI)-ICTGBs imply that the adsorption process is according with Freundlich model. Adsorption kinetics suggests that the pseudo-second order adsorption mechanism is predominant for this adsorbent system of Mo (VI)-ICTGBs. The Mo (VI)-ICTGBs show high adsorption capacity and good selectivity for Mo (VI) anions in the coexistence system at pH=6.0. The Mo (VI)-ICTGBs have a good application prospect, because it is with a simple and rapid technique and good durance.


Subject(s)
Chitosan/chemistry , Ethanolamines/chemistry , Molybdenum/chemistry , Adsorption
16.
J Biosci ; 38(3): 593-604, 2013 Sep.
Article in English | MEDLINE | ID: mdl-23938391

ABSTRACT

The flavonoids metabolic pathway plays central roles in floral coloration, in which anthocyanins and flavonols are derived from common precursors, dihydroflavonols. Flavonol synthase (FLS) catalyses dihydroflavonols into flavonols, which presents a key branch of anthocyanins biosynthesis. The yellow flower of Camellia nitidissima Chi. is a unique feature within the genus Camellia, which makes it a precious resource for breeding yellow camellia varieties. In this work, we characterized the secondary metabolites of pigments during floral development of C. nitidissima and revealed that accumulation of flavonols correlates with floral coloration. We first isolated CnFLS1 and showed that it is a FLS of C. nitidissima by gene family analysis. Second, expression analysis during floral development and different floral organs indicated that the expression level of CnFLS1 was regulated by developmental cues, which was in agreement with the accumulating pattern of flavonols. Furthermore, over-expression of CnFLS1 in Nicotiana tabacum altered floral colour into white or light yellow, and metabolic analysis showed significant increasing of flavonols and reducing of anthocyanins in transgenic plants. Our work suggested CnFLS1 plays critical roles in yellow colour pigmentation and is potentially a key point of genetic engineering toward colour modification in Camellia.


Subject(s)
Camellia/growth & development , Flavonoids/metabolism , Flowers/growth & development , Oxidoreductases/chemistry , Pigmentation/genetics , Plant Proteins/chemistry , Anthocyanins/biosynthesis , Anthocyanins/genetics , Camellia/genetics , Flavonoids/genetics , Flowers/metabolism , Gene Expression Regulation, Plant , Oxidoreductases/genetics , Plant Proteins/genetics , Plants, Genetically Modified , Nicotiana/genetics , Nicotiana/metabolism
17.
Bioorg Med Chem ; 21(8): 2363-2369, 2013 Apr 15.
Article in English | MEDLINE | ID: mdl-23490151

ABSTRACT

Twenty new acyl thiourea derivatives of podophyllotoxin and 4'-demethylepipodophyllotoxin were prepared and screened for their cytotoxicity against four human tumor cell lines, A-549, DU-145, KB, and KBvin. With IC50 values of 0.098-1.13 µM, compounds 13b, 13c, and 13o displayed much better cytotoxic activity than the control etoposide. Most importantly, 13b and 13o exhibited promising cytotoxicity against the drug resistant tumor cell line KBvin with IC50 values of 0.098 and 0.13 µM, respectively, while etoposide lost activity completely. Structure-activity relationship (SAR) correlations of the new derivatives have been established. Compounds 13b and 13o merit further development as a new generation of epipodophyllotoxin-derived antitumor clinical trial candidates.


Subject(s)
Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Podophyllotoxin/analogs & derivatives , Podophyllotoxin/pharmacology , Antineoplastic Agents/chemical synthesis , Cell Line, Tumor , Drug Screening Assays, Antitumor , Humans , KB Cells , Podophyllotoxin/chemical synthesis , Podophyllotoxin/chemistry , Structure-Activity Relationship , Thiourea/analogs & derivatives , Thiourea/chemical synthesis , Thiourea/chemistry , Thiourea/pharmacology , Topoisomerase II Inhibitors/chemical synthesis , Topoisomerase II Inhibitors/chemistry , Topoisomerase II Inhibitors/pharmacology
18.
Bioorg Med Chem ; 21(5): 1248-56, 2013 Mar 01.
Article in English | MEDLINE | ID: mdl-23369687

ABSTRACT

Two series (14a-d and 21a-h) of novel spin-labeled combretastatin derivatives were synthesized and evaluated for cytotoxicity against four tumor cell lines (K562, SGC-7901, Hela and HepG-2). Simultaneously, a representative compound 21a was selected to investigate the antitumor mechanisms of these synthetic compounds. The results indicated that some of the compounds showed significant cytotoxicity against four tumor cell lines in vitro and were more active than etoposide, a clinically available anticancer drug. Among the newly synthesized compounds, 21a, 21b and 21c displayed the greatest cytotoxicity against three tested tumor cell lines (HEPG-2, BGC-832 and Hela), with IC(50) values ranging from 0.15 to 1.05 µM, compared with values of 0.014-0.403 µM for 3-amino-deoxycombretastatin A-4 (3). In addition, the mechanistic analysis revealed that compound 21a effectively interfered with tubulin dynamics to prevent mitosis in cancer cells, leading to cell cycle arrest and, eventually, dose dependent apoptosis.


Subject(s)
Antineoplastic Agents/chemical synthesis , Bibenzyls/chemistry , Antineoplastic Agents/chemistry , Antineoplastic Agents/toxicity , Apoptosis/drug effects , Bibenzyls/chemical synthesis , Bibenzyls/toxicity , Cell Line, Tumor , Drug Screening Assays, Antitumor , HeLa Cells , Hep G2 Cells , Humans , K562 Cells , Mitosis/drug effects , Spin Labels , Tubulin/chemistry , Tubulin/metabolism , Tubulin Modulators/chemical synthesis , Tubulin Modulators/chemistry , Tubulin Modulators/toxicity
19.
Bioorg Med Chem Lett ; 22(24): 7659-61, 2012 Dec 15.
Article in English | MEDLINE | ID: mdl-23102893

ABSTRACT

New 7-acyl camptothecin derivatives were designed and synthesized from camptothecin in a one-pot reaction through a Minisci type-reaction and were evaluated for cytotoxicity against four tumor cell lines, A-549, DU-145, KB, and KB-vin. All of the new compounds showed significant inhibition of human tumor cell growth, with IC(50) values ranging from 0.01538 to 13.342 µM. Most of the derivatives were more cytotoxic than irinotecan, and the (7a) and 7-propionyl (7b) analogs exhibited the highest cytotoxic activity against the tumor cell lines tested. This compound class merits further development as anticancer clinical trial candidates.


Subject(s)
Antineoplastic Agents/pharmacology , Camptothecin/pharmacology , Drug Design , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Camptothecin/chemical synthesis , Camptothecin/chemistry , Cell Line, Tumor , Cell Proliferation/drug effects , Dose-Response Relationship, Drug , Humans , KB Cells , Molecular Structure , Structure-Activity Relationship
20.
Zhonghua Yi Xue Za Zhi ; 85(17): 1201-4, 2005 May 11.
Article in Chinese | MEDLINE | ID: mdl-16029597

ABSTRACT

OBJECTIVE: To investigate the roles of PTEN (phosphatase and tensin homologue deleted on chromosome ten)/PI3K (phosphatidylinositol 3 kinase) signal transduction pathways in myocardium remodeling in patients with congestive heart failure (CHF). METHODS: A small amount of papillary muscle tissue was collected during mitral valve displacement from 39 patients of mitral valve disease with CHF, 12 cases with grade II, 15 cases with grade III, and 12 cases with grade IV cardiac function. 30 cases of healthy persons and 8 cases of heart donors who died of accident were included as controls. Pathological examination was conducted. Immunoprecitipation was used to assay the protein expression and phosphorylation of PTEN, PI3K and Akt (protein kinase B), and protein expression of alpha-skeletal-actin in myocardial tissues. RESULTS: Typical myocardial remodeling was shown in the myocardial tissues from the valvular heart disease patients with CHF. Hypertrophy was dominant in the myocardial tissues at early stagy of CHF, the myocardial tissues in the end stage of CHF was characterized by disordered alignment of myocytes, discontinuity and dissolving of cardiac fiber, destroyed subcellular organs, and hyperplasia of interstitial tissue. The protein expression of PTEN [absorbance value (A) ratio of PTEN and beta-actin] in control group was 3.29 +/- 0.11, grade II cardiac function was 2.56 +/- 0.19, grade III was 1.52 +/- 0.35, grade IV was 0.91 +/- 0.10, PTEN protein expressions in CHF groups were lower than that of control group and negatively correlated to the levels of cardiac function (P < 0.05 or 0.01). On the contrary, The phosphorylation of PI3K (PI3K/beta-actin) in control group was 0.21 +/- 0.04, grade II cardiac function was 0.52 +/- 0.09, grade III was 1.12 +/- 0.29, grade IV was 1.62 +/- 0.54; The phosphorylation of Akt (Akt/beta-actin) in control group was 0.75 +/- 0.13, grade II cardiac function was 1.21 +/- 0.34, grade III was 2.45 +/- 0.71, grade IV was 3.55 +/- 0.80; The protein expression of alpha-skeletal-actin (alpha-skeletal-actin/beta-actin) in control group was 0.20 +/- 0.03, grade II cardiac function was 0.41 +/- 0.04, grade III was 0.82 +/- 0.09, grade IV was 1.56 +/- 0.11, their expressions in CHF groups were higher than that of control group and positively correlated to the levels of cardiac function (P < 0.05 or 0.01). CONCLUSION: Both the PTEN and PI3K signal pathways are involved in the pathogenesis of myocardial remodeling in CHF patients with valvular heart disease, which play an important role in the pathogenesis of myocardial hypertrophy. PTEN may play a negative regulation role in the process of myocardial remodeling.


Subject(s)
Heart Failure/pathology , PTEN Phosphohydrolase/biosynthesis , Phosphatidylinositol 3-Kinases/biosynthesis , Ventricular Remodeling , Adult , Female , Heart Failure/metabolism , Heart Failure/physiopathology , Humans , Male , Middle Aged , Myocardium/enzymology , PTEN Phosphohydrolase/genetics , Phosphatidylinositol 3-Kinases/genetics , Signal Transduction
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