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1.
BMC Plant Biol ; 24(1): 284, 2024 Apr 16.
Article in English | MEDLINE | ID: mdl-38627650

ABSTRACT

BACKGROUND: Lipids found in plant seeds are essential for controlling seed dormancy, dispersal, and defenses against biotic and abiotic stress. Additionally, these lipids provide nutrition and energy and are therefore important to the human diet as edible oils. Acer truncatum, which belongs to the Aceaceae family, is widely cultivated around the world for its ornamental value. Further because its seed oil is rich in unsaturated fatty acids (UFAs)- i.e. α-linolenic acid (ALA) and nervonic acid (NA)- and because it has been validated as a new food resource in China, the importance of A. truncatum has greatly risen. However, it remains unknown how UFAs are biosynthesized during the growth season, to what extent environmental factors impact their content, and what areas are potentially optimal for their production. RESULTS: In this study, transcriptome and metabolome of A. truncatum seeds at three representative developmental stages was used to find the accumulation patterns of all major FAs. Cumulatively, 966 metabolites and 87,343 unigenes were detected; the differential expressed unigenes and metabolites were compared between stages as follows: stage 1 vs. 2, stage 1 vs. 3, and stage 2 vs. 3 seeds, respectively. Moreover, 13 fatty acid desaturases (FADs) and 20 ß-ketoacyl-CoA synthases (KCSs) were identified, among which the expression level of FAD3 (Cluster-7222.41455) and KCS20 (Cluster-7222.40643) were consistent with the metabolic results of ALA and NA, respectively. Upon analysis of the geographical origin-affected diversity from 17 various locations, we found significant variation in phenotypes and UFA content. Notably, in this study we found that 7 bioclimatic variables showed considerable influence on FAs contents in A. truncatum seeds oil, suggesting their significance as critical environmental parameters. Ultimately, we developed a model for potentially ecological suitable regions in China. CONCLUSION: This study provides a comprehensive understanding of the relationship between metabolome and transcriptome in A. truncatum at various developmental stages of seeds and a new strategy to enhance seed FA content, especially ALA and NA. This is particularly significant in meeting the increasing demands for high-quality edible oil for human consumption. The study offers a scientific basis for A. truncatum's novel utilization as a woody vegetable oil rather than an ornamental plant, potentially expanding its cultivation worldwide.


Subject(s)
Acer , Transcriptome , Humans , Gene Expression Profiling , Acer/genetics , Acer/metabolism , Fatty Acids, Unsaturated/metabolism , Seeds , Metabolome , Plant Oils/metabolism
2.
Zhongguo Zhong Yao Za Zhi ; 49(1): 251-267, 2024 Jan.
Article in Chinese | MEDLINE | ID: mdl-38403358

ABSTRACT

This study aims to evaluate the efficacy and safety of Chinese medicine injection in the treatment of acute heart failure. PubMed, Cochrane Library, EMbase, Web of Science, CNKI, VIP, Wanfang, and SinoMed were searched for the randomized controlled trial(RCT) of Chinese medicine injection combined with conventional western medicines in the treatment of acute heart failure with the time interval from the inception to July 10, 2023. Two researchers independently screened the literature, extracted data, and evaluated the risk of bias in the included studies. Stata 15.1 was used to perform network Meta-analysis. A total of 117 RCTs were included, involving 10 529 patients and 7 Chinese medicine injections: Shenfu Injection, Shenmai Injection, Danhong Injection, Puera-rin Injection, Xinmailong Injection, Shengmai Injection, and Yiqi Fumai Injection. Network Meta-analysis yielded the following results.(1) In terms of improving the total response rate, the surface under the cumulative ranking curve(SUCRA) ranking was Shengmai Injection + conventional western medicine > Danhong Injection + conventional western medicine > Shenmai Injection + conventio-nal western medicine > Shenfu Injection + conventional western medicine > Xinmailong Injection + conventional western medicine > Yiqi Fumai Injection + conventional western medicine > Puerarin Injection + conventional western medicine > conventional western medicine.(2)In terms of reducing brain natriuretic peptide(BNP), the SUCRA ranking was Danhong Injection + conventional western medicine > Xinmailong Injection + conventional western medicine > Yiqi Fumai Injection + conventional western medicine > Shenfu Injection + conventional western medicine > Shenmai Injection + conventional western medicine > Puerarin Injection + conventional wes-tern medicine > Shengmai Injection + conventional western medicine > conventional western medicine.(3)In terms of reducing N-terminal pro-brain natriuretic peptide(NT-proBNP), the SUCRA ranking was Shenmai Injection + conventional western medicine > Yiqi Fumai Injection + conventional western medicine > Xinmailong Injection + conventional western medicine > Shengmai Injection + conventional western medicine > Shenfu Injection + conventional western medicine > Puerarin Injection + conventional western medicine > Danhong Injection + conventional western medicine > conventional western medicine.(4) In terms of improving the left ventricular ejection fraction(LVEF), the SUCRA ranking was Shenmai Injection + conventional western medicine > Xinmailong Injection + conventional western medicine > Shenfu Injection + conventional western medicine > Yiqi Fumai Injection + conventional western medicine > Puerarin Injection + conventional western medicine > Danhong Injection + conventional western medicine > Shengmai Injection + conventional western medicine > conventional western medicine.(5) In terms of decreasing the left ventricular end-diastolic diameter(LVEDD), the SUCRA ranking was Shenmai Injection + conventional western medicine > Shenfu Injection + conventional western medicine=Xinmailong Injection + conventional western medicine > Shengmai Injection + conventional western medicine > Yiqi Fumai Injection + conventional western medicine > conventional western medicine > Puerarin Injection + conventional western medicine.(6) In terms of increasing the 6-min walk trail(6MWT), the SUCRA ranking was Xinmailong Injection + conventional western medicine > Shenfu Injection + conventional western medicine > Shenmai Injection + conventional western medicine > Yiqi Fumai Injection + conventional western medicine > conventional western medicine.(7) In terms of reducing the Minnesota heart failure quality of life scale(MLHFQ) scores, the SUCRA ranking was Xinmailong Injection + conventional western medicine > Shenmai Injection + conventional western medicine > Shenfu Injection + conventional western medicine > conventional western medicine.(8)In terms of safety, the group of Chinese medicine injection combined with conventional western medicine had lower incidence of adverse reactions than the control group. The current evidence shows that combining Chinese medicine injection with conventional western medicine treatment can improve the therapeutic effect on acute heart failure, with high safety. Due to the limited number and quality of included studies, the above conclusions need to be verified by more high-quality studies.


Subject(s)
Drugs, Chinese Herbal , Heart Failure , Humans , Drugs, Chinese Herbal/therapeutic use , Heart Failure/drug therapy , Medicine, Chinese Traditional , Natriuretic Peptide, Brain , Network Meta-Analysis , Quality of Life , Stroke Volume , Ventricular Function, Left , Randomized Controlled Trials as Topic
3.
Zhen Ci Yan Jiu ; 48(8): 818-24, 2023 Aug 25.
Article in Chinese | MEDLINE | ID: mdl-37614141

ABSTRACT

OBJECTIVE: To observe the effect of electroacupuncture (EA) at "Zhongwan" (CV12), "Tianshu" (ST25) and "Shangjuxu" (ST37) (an acupoint prescription "Changbingfang" for treatment of intestinal disorders) on autophagy and expression of AMPK/mTOR signaling pathway in rats with ulcerative colitis (UC), so as to explore its mechanism underlying improvement of UC. METHODS: Thirty-two male SD rats were randomly divided into control, model, medication and EA groups, with 8 rats in each group. The UC model was established by free drinking of 5% dextran sulfate sodium salt solution for 7 days. EA stimulation (10 Hz/50 Hz) was delivered to CV12, ST25 and ST37 for 20 min, once a day for 3 consecutive days. Rats of the medication group received gavage of mesalazine suspension (200 mg/kg) once a day, 3 times in total. The rats' general conditions were recorded for calculating the disease activity index (DAI) score (0-4 points). Histomorphological changes of colon were observed via HE staining. The levels of serum interleukin 6 (IL-6), tumor necrosis factor-α (TNF-α) and IL-10 were measured by ELISA. The mRNA expressions of LC3B and p62 were tested by fluorescence quantitative PCR. Western blot was used to detect the expression levels of LC3B, p62 and AMPK/mTOR pathway related proteins in colon tissues. RESULTS: Compared with the control group, the DAI score, contents of serum IL-6 and TNF-α, the expression levels of p62 protein and mRNA, ratio of p-mTOR/mTOR were significantly increased (P<0.01); while the content of serum IL-10, the expression levels of LC3B mRNA, ratio of LC3BⅡ/LC3BⅠ and p-AMPK/AMPK were decreased (P<0.01, P<0.05) in the model group. Relevant to the model group, modeling-induced increases of DAI score, serum IL-6, TNF-α and IL-10 contents, expressions of p62 protein and mRNA, LC3B mRNA, ratio of p-mTOR/mTOR, LC3BⅡ/LC3BⅠ and p-AMPK/AMPK were reversed in both medication and EA groups (P<0.01, P<0.05). The effect of EA was apparently superior to that of mesalazine in up-regulating ratio of LC3BⅡ/LC3BⅠ and p-AMPK/AMPK, p62 mRNA expression (P<0.01, P<0.05), and in down-regulating ratio of p-mTOR/mTOR (P<0.05). H.E. staining showed severe damage of the colonic mucosal barrier with infiltration of a large number of inflammatory cells in the model group, which was milder in medication and EA groups. CONCLUSION: EA of acupoint recipe "Changbingfang" can improve the symptoms in UC rats, which may be related to its functions in promoting colonic autophagy, increasing AMPK phosphorylation level, and decreasing mTOR phosphorylation level.


Subject(s)
Colitis, Ulcerative , Electroacupuncture , Male , Animals , Rats , Rats, Sprague-Dawley , Colitis, Ulcerative/genetics , Colitis, Ulcerative/therapy , AMP-Activated Protein Kinases/genetics , Interleukin-10 , Mesalamine , Interleukin-6 , Tumor Necrosis Factor-alpha/genetics , Signal Transduction , TOR Serine-Threonine Kinases/genetics , RNA, Messenger , Autophagy
4.
Clin Transl Med ; 13(8): e1359, 2023 08.
Article in English | MEDLINE | ID: mdl-37537731

ABSTRACT

BACKGROUND: N6 -methyladenosine (m6A) is of great importance in renal physiology and disease progression, but its function and mechanism in renal fibrosis remain to be comprehensively and extensively explored. Hence, this study will explore the function and potential mechanism of critical regulator-mediated m6A modification during renal fibrosis and thereby explore promising anti-renal fibrosis agents. METHODS: Renal tissues from humans and mice as well as HK-2 cells were used as research subjects. The profiles of m6A modification and regulators in renal fibrosis were analysed at the protein and RNA levels using Western blotting, quantitative real-time polymerase chain reaction and other methods. Methylation RNA immunoprecipitation sequencing and RNA sequencing coupled with methyltransferase-like 3 (METTL3) conditional knockout were used to explore the function of METTL3 and potential targets. Gene silencing and overexpression combined with RNA immunoprecipitation were performed to investigate the underlying mechanism by which METTL3 regulates the Ena/VASP-like (EVL) m6A modification that promotes renal fibrosis. Molecular docking and virtual screening with in vitro and in vivo experiments were applied to screen promising traditional Chinese medicine (TCM) monomers and explore their mechanism of regulating the METTL3/EVL m6A axis and anti-renal fibrosis. RESULTS: METTL3 and m6A modifications were hyperactivated in both the tubular region of fibrotic kidneys and HK-2 cells. Upregulated METTL3 enhanced the m6A modification of EVL mRNA to improve its stability and expression in an insulin-like growth factor 2 mRNA-binding protein 2 (IGF2BP2)-dependent manner. Highly expressed EVL binding to Smad7 abrogated the Smad7-induced suppression of transforming growth factor-ß (TGF-ß1)/Smad3 signal transduction, which conversely facilitated renal fibrosis progression. Molecular docking and virtual screening based on the structure of METTL3 identified a TCM monomer named isoforsythiaside, which inhibited METTL3 activity together with the METTL3/EVL m6A axis to exert anti-renal fibrosis effects. CONCLUSIONS: Collectively, the overactivated METTL3/EVL m6A axis is a potential target for renal fibrosis therapy, and the pharmacological inhibition of METTL3 activity by isoforsythiaside suggests that it is a promising anti-renal fibrosis agent.


Subject(s)
Methyltransferases , RNA , Animals , Humans , Mice , Fibrosis , Methyltransferases/genetics , Methyltransferases/metabolism , Molecular Docking Simulation , RNA, Messenger/genetics , RNA-Binding Proteins
5.
Front Psychiatry ; 14: 1144989, 2023.
Article in English | MEDLINE | ID: mdl-37496685

ABSTRACT

Mindfulness training among patients with major depressive disorder (MDD) reduces symptoms, prevents relapse, improves prognosis, and is more efficient for those with a high level of trait mindfulness. Upon hospital admission, 126 MDD patients completed the Beck Depression Inventory (BDI), World Health Organization Quality of Life Brief, Five-Factor Mindfulness Questionnaire (FFMQ), and the Rumination Response Scale (RRS). The 65 patients that scored less than the median of all subjects on the FFMQ were placed into the low mindfulness level (LML) group. The other 61 patients were placed in the high mindfulness level (HML) group. All facet scores were statistically different between the mental health assessment scores of the HML and LML groups except for RRS brooding and FFMQ nonjudgement. Trait mindfulness level exhibited a negative and bidirectional association with MDD severity primarily through the facets of description and aware actions. Trait mindfulness was also related positively with age primarily through the facets of nonreactivity and nonjudgement. Being married is positively associated with trait mindfulness levels primarily through the facet of observation and by an associated increase in perceived quality of life. Mindfulness training prior to MDD diagnosis also associates positively with trait mindfulness level. Hospitalized MDD patients should have their trait mindfulness levels characterized to predict treatment efficiency, help establish a prognosis, and identify mindfulness-related therapeutic targets.

6.
Nutrients ; 14(20)2022 Oct 14.
Article in English | MEDLINE | ID: mdl-36296987

ABSTRACT

Shortening is mainly derived from the partial hydrogenation of palm oil and widely used in fast food. Food processed with shortening contains high levels of industrial trans fatty acids. Studies have shown that there is a correlation between industrial trans fatty acids, obesity, and depression. However, the regulatory effect of neuronal nitric oxide synthase (nNOS) on depression in obese patients is still unknown. The purpose of this study was to explore mood changes in obese mice fed a high shortening diet, and to determine the regulatory effect of nNOS on depressive-like behaviors in obese mice. We used a high shortening diet-induced obesity mouse model to systematically assess the metabolic response, behavioral changes, prefrontal and hippocampal nNOS protein levels, and the effect of nNOS inhibitors (7-nitroindole) on depression-like behavior in obese mice. Interestingly, obese mice on a 9-week high-shortening diet developed short-term spatial working memory impairment and anxiety-like behavior, and obesity may be a risk factor for cognitive impairment and mood disorders. In animals fed a high shortening diet for 12 weeks, obese mice developed depression-like behavior and had significantly elevated levels of nNOS protein expression in the hippocampus and prefrontal lobe. Administration of the nNOS inhibitor 7-nitroindole could improve depression-like behaviors in obese mice, further suggesting that inhibition of nNOS is helpful for depression associated with obesity.


Subject(s)
Depression , Trans Fatty Acids , Animals , Mice , Nitric Oxide Synthase Type I/metabolism , Mice, Obese , Depression/etiology , Depression/metabolism , Palm Oil/metabolism , Hippocampus/metabolism , Obesity/complications , Obesity/metabolism , Nitric Oxide/metabolism
7.
J Food Sci ; 87(9): 3925-3937, 2022 Sep.
Article in English | MEDLINE | ID: mdl-35904249

ABSTRACT

Acer truncatum seed oil (ATSO) contains abundant unsaturated fatty acids, with significant quantities of nervonic acid (NA, > 5%), which was authenticated as a new food resource in China. For the sake of minimizing animal consumption and the importance of NA for human health, extraction of NA from plants has become a research hotspot. In the present study, three extraction factors were determined to significantly influence the saponification reaction based on single-factor experiments: NaOH dosage, reaction time, and reaction temperature. These three factors were used to further optimize the saponification process through the response surface methodology, and the highest yield of mixed fatty acids was 83.12%. Moreover, the activation energy (40.8228 kJ/mol), the pre-exponential factor [2.568 × 106 m3 /(kmol·min)], and the kinetic equation [rA = kcA cB = 2.568 × 106 ·exp(- 4970 . 1 T ) $\frac{{{\rm{4970}}{\rm{.1}}}}{{\rm{T}}})$ cA cB ] of the ATSO saponification reaction were determined by combining the chemical reaction rate equation of the elementary reaction, the Arrhenius equation, and the NaOH concentration in the substrate. Finally, the mixed fatty acids of ATSO were crystallized by triple-stage low-temperature crystallization, and we achieved 25.05% purity for NA. This study provides a technological basis and strategy for specific fatty acid production from ASTO, as well as other vegetable oils important in the field of food and health supplement products. PRACTICAL APPLICATION: Nervonic acid (NA) is an essential component of neural cells and neural tissue, and it is vital for maintaining the normal work of nerve tissues in organisms and promotes neurodevelopment. NA has traditionally been mainly obtained from shark hunting, which is now restricted due to an international ban on shark fishing. The alternative way to produce NA cheaply and in large quantities is from plant sources. The techniques utilized in this study provide an effective method of NA separation from Acer truncatum seed oil for industrial production.


Subject(s)
Acer , Acer/chemistry , Crystallization , Fatty Acids/analysis , Fatty Acids, Monounsaturated , Humans , Kinetics , Plant Oils/chemistry , Seeds/chemistry , Sodium Hydroxide , Technology
8.
J Nat Prod ; 85(5): 1193-1200, 2022 05 27.
Article in English | MEDLINE | ID: mdl-35512012

ABSTRACT

Eight new phenethoxy derivatives, trichoasperellins A-H (1-8), were isolated from the endophytic fungus Trichoderma asperellum G10 isolated from the medicinal plant Areca catechu L. The structures of these compounds were elucidated from spectroscopic data, J-based configurational analysis, and Mosher's methods. Compounds 1-4 and 6-8 bear one or two multioxidized C7 moieties with the same carbon skeleton. The carbon skeletons of compounds 6-8 are new, all containing three moieties connected via two acetal carbons similar to those of disaccharide glycosides. Compound 4 inhibited nitric oxide production with an IC50 value of 48.3 µM, comparable to that of the positive control indomethacin (IC50, 42.3 µM).


Subject(s)
Hypocreales , Trichoderma , Anti-Inflammatory Agents/chemistry , Anti-Inflammatory Agents/pharmacology , Areca , Carbon , Molecular Structure , Trichoderma/chemistry
9.
Mar Pollut Bull ; 178: 113572, 2022 May.
Article in English | MEDLINE | ID: mdl-35381462

ABSTRACT

Since 1990s, harmful algal blooms (HABs) of Kareniaceae, primarily caused by species of Karenia and Karlodinium and rarely by Takayama species, have been substantially increasing in frequency and duration in the coastal waters of China. In this study, we recorded a bloom of high abundance of T. acrotrocha in the Haizhou Bay, the Yellow Sea in September 2020, which is the first record of a Takayama bloom in the temperate coastal waters of China. We found that high concentrations of DON and DOP accelerated the proliferation of T. acrotrocha in the Haizhou Bay. Intensive mariculture, and terrestrial nitrogen and phosphorus input may be responsible for the eutrophication in the Haizhou Bay featuring high concentrations of DON and DOP, and high DIN/DIP ratios. The results suggested that, under ocean warming, the HABs of Kareniaceae are becoming increasingly dominant in eutrophic temperate coasts with intensive mariculture activities.


Subject(s)
Dinoflagellida , Phosphorus , Bays , Dinoflagellida/physiology , Dissolved Organic Matter , Harmful Algal Bloom
10.
Molecules ; 27(4)2022 Feb 16.
Article in English | MEDLINE | ID: mdl-35209113

ABSTRACT

Acer truncatum Bunge is now widely cultivated throughout the world. Fatty acid synthase (FAS) is a potential target in the treatment of both obesity and cancer. Only a few FAS inhibitors have been reported. In this study, the inhibitory effect of A. truncatum seed coat (ESA) on FAS and the inhibition mechanisms were investigated using a FAS activity assay and an enzyme kinetics study. The main chemicals of ESA were analyzed with UPLC-MS/MS. The effects of ESA on 3T3-L1 adipocyte differentiation and lipid accumulation were investigated using Oil red O staining. We first identified seven main compounds (quinic acid, malic acid, gentisic acid, procyanidin dimer, procyanidin trimer, catechin, and quercetin) from 50% ethanol extracts of seed coats of A. truncatum (ESAs), which were then found to inhibit 3T3-L1 adipocyte differentiation at the concentration of 50 µg/mL. ESA obviously reduced the visible triglyceride droplets accumulation, and dramatically decreased the number of the adipocytes at a comparatively high concentration. It is suggested that the effects are due to the inhibition of FAS by ESA; FAS activity is inhibited by ESA at a half inhibition concentration (IC50) of 0.57 µg/mL, which is lower than that of classically known FAS inhibitors. Meanwhile, ESA displayed different inhibition kinetics and reacting sites for FAS. These results provide new clues for the development of novel products for obesity treatment and a scientific basis for the full use of byproducts for future industrial production of vegetable oil.


Subject(s)
Acer/chemistry , Cell Differentiation/drug effects , Lipid Metabolism/drug effects , Plant Extracts/chemistry , Plant Extracts/pharmacology , Seeds/chemistry , Adipocytes/drug effects , Animals , Chromatography, High Pressure Liquid , Enzyme Activation/drug effects , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Fatty Acid Synthases/metabolism , Mice , Molecular Structure , Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization , Tandem Mass Spectrometry
11.
Food Funct ; 13(2): 846-856, 2022 Jan 24.
Article in English | MEDLINE | ID: mdl-34989366

ABSTRACT

Tree peonies are well-known horticultural and medicinal plants. The tree peony seeds, as emerging woody oil crops, recently have attracted great attention for their metabolites and bioactivities. In this study, the phytochemicals isolated from tree peony seed coats were systematically investigated. Seven polyphenolics were separated and prepared, mainly belonging to resveratrol derivatives. There was a great variation in the seed coat polyphenolic content among eight Paeonia species, and the contents of the resveratrol trimers and dimers were significantly higher in the seed coats of Paeonia ostii than other species. Based on the HPLC fingerprint characteristics and chemometric analysis, a clear discrimination among Paeonia plants was found, including the composition patterns and contents of the constituents. Moreover, the characteristic phytochemicals (vateriferol and trans-ε-viniferin) could significantly reduce the starch-mediated levels of postprandial blood glucose in diabetic/normal mice. In addition, in vitro enzyme tests showed that the two compounds could effectively and competitively inhibit α-glucosidase, with the IC50 values of 3.01 and 7.75 µM, respectively, indicating that vateriferol and trans-ε-viniferin could be therapeutic potential agents for hyperglycemia and diabetes mellitus.


Subject(s)
Blood Glucose/drug effects , Paeonia/chemistry , Resveratrol/analogs & derivatives , Resveratrol/pharmacology , Seeds/chemistry , Animals , Dose-Response Relationship, Drug , Gene Expression Regulation, Enzymologic/drug effects , Glycoside Hydrolase Inhibitors/chemistry , Glycoside Hydrolase Inhibitors/pharmacology , Hypoglycemic Agents/chemistry , Hypoglycemic Agents/pharmacology , Male , Mice , Molecular Docking Simulation , Resveratrol/chemistry , Starch/administration & dosage , alpha-Glucosidases/chemistry , alpha-Glucosidases/metabolism
12.
Zhongguo Zhong Yao Za Zhi ; 46(7): 1783-1789, 2021 Apr.
Article in Chinese | MEDLINE | ID: mdl-33982482

ABSTRACT

Chemical constituents were isolated and purified from fruiting bodies of Ganoderma calidophilum by various column chromatographic techniques, and their chemical structures were identified through combined analysis of physicochemical properties and spectral data. As a result, 11 compounds were isolated and identified as(24E)-lanosta-8,24-dien-3,11-dione-26-al(1), ganoderone A(2), 3-oxo-15α-acetoxy-lanosta-7,9(11), 24-trien-26-oleic acid(3),(23E)-27-nor-lanosta-8,23-diene-3,7,25-trione(4), ganodecanone B(5), ganoderic aldehyde A(6), 11ß-hydroxy-lucidadiol(7), 3,4-dihydroxyacetophenone(8), methyl gentiate(9), ganoleucin C(10), ganotheaecolumol H(11). Among them, compound 1 is a new triterpenoid. The cytotoxic activities of all of the compounds against tumor cell lines were evaluated. The results showed that compounds 1, 3, 4 and 6 showed cytotoxic activity against BEL-7402, with IC_(50) values of 26.55, 11.35, 23.23, 18.66 µmol·L~(-1); compounds 1 and 3-6 showed cytotoxic activity against K562, with IC_(50) values of 5.79, 22.16, 12.16, 35.32, and 5.59 µmol·L~(-1), and compound 4 showed cytotoxic activity against A549, with IC_(50) value of 42.50 µmol·L~(-1).


Subject(s)
Ganoderma , Triterpenes , Cell Line, Tumor , Fruiting Bodies, Fungal , Molecular Structure , Triterpenes/pharmacology
13.
Theranostics ; 11(11): 5464-5490, 2021.
Article in English | MEDLINE | ID: mdl-33859758

ABSTRACT

Hepatocellular carcinoma (HCC) is the most common type of liver cancer and one of the leading causes of cancer-related death worldwide. Advanced HCC displays strong resistance to chemotherapy, and traditional chemotherapy drugs do not achieve satisfactory therapeutic efficacy. Sorafenib is an oral kinase inhibitor that inhibits tumor cell proliferation and angiogenesis and induces cancer cell apoptosis. It also improves the survival rates of patients with advanced liver cancer. However, due to its poor solubility, fast metabolism, and low bioavailability, clinical applications of sorafenib have been substantially restricted. In recent years, various studies have been conducted on the use of nanoparticles to improve drug targeting and therapeutic efficacy in HCC. Moreover, nanoparticles have been extensively explored to improve the therapeutic efficacy of sorafenib, and a variety of nanoparticles, such as polymer, lipid, silica, and metal nanoparticles, have been developed for treating liver cancer. All these new technologies have improved the targeted treatment of HCC by sorafenib and promoted nanomedicines as treatments for HCC. This review provides an overview of hot topics in tumor nanoscience and the latest status of treatments for HCC. It further introduces the current research status of nanoparticle drug delivery systems for treatment of HCC with sorafenib.


Subject(s)
Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , Carcinoma, Hepatocellular/drug therapy , Liver Neoplasms/drug therapy , Nanoparticles/chemistry , Sorafenib/pharmacology , Sorafenib/therapeutic use , Animals , Drug Delivery Systems/methods , Humans
14.
Fitoterapia ; 146: 104708, 2020 Oct.
Article in English | MEDLINE | ID: mdl-32827694

ABSTRACT

Patchouli is a tropical medicinal and spice crop with high economic value, and the endophytic microorganism is also one of its important components and can provide new active compounds with medicinal use. In the present study, four new biphenyl compounds named 3-O-demethylaltenuisol (1), (-)-dialtenuisol (5) and (+)-dialtenuisol (6), and altertoxin VII (9), as well as six known related compounds, were isolated from the patchouli (Pogostemon cablin) endophytic fungus Alternaria sp. PfuH1. The structures of the new compounds were elucidated from spectroscopic data, ECD spectra analysis, and ECD calculations. Compounds 5 and 6 are a pair of dimeric axially chiral enantiomers. Compounds 2, 4, and 9 showed antibacterial activities against S. agalactiae with MIC values of 9.3, 85.3, and 17.3 µg/mL, respectively, and compound 4 also showed weak antibacterial activity against E. coli with MIC value of 128 µg/mL.


Subject(s)
Alternaria/chemistry , Anti-Bacterial Agents/pharmacology , Biphenyl Compounds/pharmacology , Pogostemon/microbiology , Anti-Bacterial Agents/isolation & purification , Biphenyl Compounds/isolation & purification , Cell Line, Tumor , China , Endophytes/chemistry , Escherichia coli/drug effects , Flowers/microbiology , Humans , Microbial Sensitivity Tests , Molecular Structure
15.
J Anim Physiol Anim Nutr (Berl) ; 104(1): 371-378, 2020 Jan.
Article in English | MEDLINE | ID: mdl-31724249

ABSTRACT

In order to investigate the mechanism of genistein (Gen) in the treatment of climacteric syndrome, an in vivo study was performed to investigate the beneficial effects of genistein on the expression of P450 aromatase (P450 arom) and follicle-stimulating hormone receptor (FSHR) in the mouse ovary and uterus. Fifty female ICR mice (45 ± 5g, n = 50), aged 12 months, were divided into the following five groups with 10 animals in each: blank control group (CG), low-dose genistein group (L-Gen), middle-dose genistein group (M-Gen) and high-dose genistein group (H-Gen) (received 15, 30 and 60 mg/kg of genistein, respectively), and oestrogen group (EG; received 0.5 mg/kg diethylstilbestrol). The expression levels of the FSHR protein were determined by an immunohistochemical staining method. The expression of P450 arom, Cytochrome P450 19 (CYP19) and FSHR was quantified by real-time PCR. Immunohistochemical results showed that the expression levels of the FSHR protein in the M-Gen (average stained area: 20.79) and the H-Gen (average stained area: 21.21) groups were significantly stronger than in the CG (average area was 17.24) group (p < .05). The expression levels of CYP19 mRNA and P450 arom were positively correlated with the dose of genistein. Specifically, the relative expression levels in the H-Gen and EG groups were more than 1.5 times higher than in the CG group (p < .05). Genistein played a significant role in regulating aromatase and FSHR gene expression to improve perimenopausal ovarian and uterine function.


Subject(s)
Aromatase/metabolism , Genistein/pharmacology , Menopause , Metabolic Syndrome/drug therapy , Receptors, FSH/metabolism , Animals , Aromatase/genetics , Female , Gene Expression Regulation/drug effects , Mice , Mice, Inbred ICR , Ovary/drug effects , Ovary/metabolism , Receptors, FSH/genetics , Transcriptome
16.
Zhongguo Zhong Yao Za Zhi ; 44(3): 489-494, 2019 Feb.
Article in Chinese | MEDLINE | ID: mdl-30989913

ABSTRACT

Chemical constituents were isolated from the fruiting bodies of Ganoderma australe by various column chromatographic techniques and HPLC method, and their chemical structures were identified through the combined analysis of physicochemical properties and spectral data. Meanwhile, their α-glucosidase inhibitory activity and anti-oxidative ability were evaluated. Seven compounds were isolated from G. australe and were identified as 6-methoxyl-cyclo-(Phe-Ile)(1), applanoxidic acid A methyl ester(2), ergosta-7,22 E-dien-3ß-ol(3), cinnamic acid(4), 5α,8α-epidioxy-(20S,22E,24R)-ergosta-6,22-diene-3ß-ol(5), 1-(3, 4-dihydroxyphenyl) ethanone(6), salicylic acid(7) and benzoic acid(8). Among the compounds, compound 1 was a new cyclic dipeptide. Compound 2 was a new lanosta natural product, and compounds 4, 6, 7 and 8 were obtained from G. australe for the first time. Moreover, compounds 4 and 8 exhibited α-glucosidase inhibitory activity with inhibition rates of 36.8% and 34.7%, and compounds 4, 7 and 8 had a certain activity in DPPH free radical scavenging activity with IC_(50) values of 0.168, 0.458 and 0.170 g·L~(-1), respectively. The DPPH radical scavenging rate of compound 1 was 41.1%.


Subject(s)
Fruiting Bodies, Fungal/chemistry , Ganoderma/chemistry , Free Radical Scavengers/isolation & purification , Glycoside Hydrolase Inhibitors/isolation & purification , Molecular Structure
17.
Fitoterapia ; 134: 182-187, 2019 Apr.
Article in English | MEDLINE | ID: mdl-30825575

ABSTRACT

Five optically active epoxy-5,6,7,8-tetrahydro-2-(2-phenylethyl)chromone derivatives (1-5) with four chirality centers in the condensed cyclohexene ring were isolated from artificial holing agarwood originating from Aquilaria sinensis (Lour.) Gilg. Their structures were elucidated by spectroscopic techniques (UV, IR, 1D and 2D NMR) and MS analyses. The absolute configuration of 2 was elucidated by TDDFT-ECD calculations and ECD spectra of 1, 3-5 allowed their configurational assignment as well. All of the new compounds contained a condensed oxirane ring, and compound 1 was the only 6,7-epoxy-2-(2-phenylethyl)-5,6,7,8-tetrahydrochromone derivative that has ever been found in agarwood. AChE inhibitory activity was tested for the first time of these new compounds by using modified Ellman's colorimetric method. Compounds 3 and 5 exhibited inhibitory activity against AChE with IC50 value of 441.6, and 155.6 µM, respectively.


Subject(s)
Chromones/pharmacology , Thymelaeaceae/chemistry , Wood/chemistry , China , Cholinesterase Inhibitors/isolation & purification , Cholinesterase Inhibitors/pharmacology , Chromones/isolation & purification , Molecular Structure , Phytochemicals/isolation & purification , Phytochemicals/pharmacology
18.
Phytochemistry ; 159: 208-215, 2019 Mar.
Article in English | MEDLINE | ID: mdl-30634083

ABSTRACT

Twelve undescribed compounds including six phenanthrene derivatives (parviphenanthrines A-F), two stilbene derivatives (parvistilbines A-B), three esters (parviesters A-C), and one sesquiterpenoid (parvidiol A) were isolated from the roots of Stemona parviflora, together with twenty-two known ones. The structures of the undescribed compounds were elucidated based on the analyses of their spectroscopic data. The absolute configuration of parviphenanthrine A was determined by the quantum ECD calculations. Parviphenanthrines A and E, stemanthrene A, stilbostenin E, 4-hydroxy-benzenepropanol-α-benzoate, and (E)-4-hydroxycinnamic acid methyl ester showed nematocidal activity against Meloidogyne incognita with IC50 values of 14.02 ±â€¯0.32, 2.51 ±â€¯0.13, 17.10 ±â€¯0.65, 2.05 ±â€¯0.07, 4.22 ±â€¯0.31, and 1.07 ±â€¯0.05 µM, respectively.


Subject(s)
Antinematodal Agents/pharmacology , Phytochemicals/chemistry , Plant Extracts/pharmacology , Plant Roots/chemistry , Stemonaceae/chemistry , Inhibitory Concentration 50 , Molecular Structure
19.
Molecules ; 23(11)2018 Nov 20.
Article in English | MEDLINE | ID: mdl-30463280

ABSTRACT

Six new phragmalin limonoids, named moluccensin Z1 (1), moluccensin Z2 (2), carapanolide Y (3), tabulalin N (4), chukvelutilide A1 (5), and velutinasin J (6), as well as two known compounds, chukvelutilide A (7) and velutinasin D (8) were isolated from the stems of Chukrasia tabularis A. Juss. The structures of the new compounds 1⁻6 were confirmed by spectroscopic methods, including IR and HRESIMS, as well as 1D and 2D NMR, and by comparisons with the data of known analogues. All compounds were tested for α-glucosidase and acetylcholinesterase inhibitory activities. However, none of the compounds was active against α-glucosidase and acetylcholinesterase in vitro.


Subject(s)
Limonins/isolation & purification , Meliaceae/chemistry , Limonins/chemistry , Molecular Structure , Nuclear Magnetic Resonance, Biomolecular , Plant Extracts/chemistry , Plant Stems/chemistry
20.
Fitoterapia ; 128: 20-25, 2018 Jul.
Article in English | MEDLINE | ID: mdl-29723562

ABSTRACT

Five new amide alkaloids (1-3, 5-6) were isolated from the seeds of Clausena lansium together with one new natural product (4) and four known analogues (7-10). The structures of the new amide alkaloids were elucidated based on a comprehensive spectroscopic data analysis including 1D and 2D NMR as well as HRESIMS, and by comparison with the literature. The bioactivity results showed that compound 8 expressed potent nematicidal activity against Panagrellus redivevus, with IC50 value of 0.12 mM, while compounds 3 and 5 presented moderate nematicidal activity with IC50 values of 2.75 and 3.93 mM, respectively (abamectin as the positive control with IC50 value of 1.05 mM).


Subject(s)
Alkaloids/isolation & purification , Amides/isolation & purification , Anthelmintics/isolation & purification , Clausena/chemistry , Seeds/chemistry , Alkaloids/pharmacology , Amides/pharmacology , Animals , Anthelmintics/pharmacology , Molecular Structure , Tylenchida/drug effects
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