Your browser doesn't support javascript.
Show: 20 | 50 | 100
Results 1 - 20 de 168
Filter
1.
Front Chem ; 10: 892554, 2022.
Article in English | MEDLINE | ID: mdl-35601554

ABSTRACT

We previously reported that the structural modifications of pentacyclic triterpenoids including oleanolic acid resulted in enhanced hyaluronidase inhibitory activity but whether this applies to other pentacyclic triterpenoids such as betulinic acid (BA) is unknown. Herein, we synthesized BA derivatives with an α,ß-unsaturated ketene moiety and evaluated for their: 1) hyaluronidase inhibitory activity and, 2) anti-inflammatory effects against lipopolysaccharides (LPS) induced inflammation. Compared to BA, the BA derivatives exerted improved anti-hyaluronidase activity (26.3%-72.8% vs. 22.6%) and anti-inflammatory effects by reducing nitrite production in BV2 cells (3.9%-46.8% vs. 3.4%) and RAW264.7 cells (22.7%-49.2% vs. 20.4%). BA derivatives inhibited LPS-induced production of pro-inflammatory cytokines in THP-1 cells (15.2%-22.4%). BA derivatives also exerted promising anti-inflammatory effects against hyaluronic acid fragment induced nitrite production (8.6%-35.6%) in THP-1 cells. BA derivatives showed augmented anti-hyaluronidase and anti-inflammatory effects but further biological evaluations using in vivo models are warranted to confirm their efficacy.

2.
RSC Adv ; 8(5): 2768-2776, 2018 Jan 09.
Article in English | MEDLINE | ID: mdl-35541462

ABSTRACT

Prostate cancer (PCa) is a common cancer among males and a leading cause of cancer deaths. Docetaxel (DOC) was recommended in guidelines as the first first-line drug of PCa; however, treatment with high doses of DOC ultimately results in resistance. This study examined the proliferation, viability, and apoptosis of VCaP cells evaluated by the MTT assay, trypan blue exclusion assay, and morphological assessments to investigate the effects and mechanisms of action by impressic acid (E12-1) or acankoreanogein (E13-1), isolated from Acanthopanax trifoliatus (L.) Merr., in combination with DOC in VCaP PCa cells. The research, which also contained cell migration, was examined under a light microscope. Nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) activity was assessed by the luciferase reporter assay. Finally, the expression of B-cell lymphoma 2 (Bcl-2), NF-κB, phosphorylated Akt (p-Akt), phosphorylated signal transducer and activator of transcription 3 (p-Stat 3), phosphorylated c-Jun N-terminal kinase (p-JNK), and extracellular signal-related protein kinases 1 and 2 in VCaP cells was evaluated by western blotting. The result is combination of DOC with E12-1 or E13-1 which synergistically inhibited growth, induced apoptosis, and reduced migration of VCaP cells compared with treatment with DOC, E12-1, or E13-1 alone. The potential molecular mechanisms were related to significant decreases in the expression of NF-κB, Bcl-2, p-Stat 3, p-JNK, and p-Akt in VCaP cells. DOC combined with E12-1 or E13-1 may be an effective approach for inhibiting the growth and apoptosis of PCa cells, thus making it possible to reduce the dose of DOC in patients with PCa who experience systemic toxicity.

3.
RSC Adv ; 8(36): 20222-20227, 2018 May 30.
Article in English | MEDLINE | ID: mdl-35541662

ABSTRACT

A symmetric ligand is synthesized composed of a core N-methylpyridinium scaffold and two para-substituted benzyl groups through a flexible ethylene bridge to form a novel three-ring-conjugated system. The ligand system was found to have only weak background fluorescent signal in aqueous or physiological conditions and exhibited strong fluorescent signal enhancement targeting at telo21 G-quadruplex structure rather than other types of nucleic acids. The comparison study with two terminal groups (-N(CH3)2 versus -SCH3) indicates that the stimulated signal enhancement of specific binding is probably attributed to the hydrogen-bonding interactions through the amino groups in the G-quartets. The docking result illuminates the experimental observation that the ligand system showed only weak fluorescent signals in aqueous or physiological conditions while exhibiting a strong fluorescent signal upon binding to the telo21 G-quadruplex structure (binding energy: -6.2 kcal mol-1).

4.
RSC Adv ; 8(41): 22931, 2018 Jun 21.
Article in English | MEDLINE | ID: mdl-35543993

ABSTRACT

[This corrects the article DOI: 10.1039/C8RA03833C.].

5.
Trans R Soc Trop Med Hyg ; 2022 May 11.
Article in English | MEDLINE | ID: mdl-35543271

ABSTRACT

BACKGROUND: Mother-to-child transmission (MTCT) is the main cause of hepatitis B virus (HBV) infections in China. However, there is a paucity of information on seroprevalence and mutations in HBV surface genes among pregnant women in Huzhou, China. METHODS: In this retrospective cross-sectional study, serum markers of 31 681 pregnant women were collected and analysed. The surface genes were amplified and directly sequenced. Mutations in the major hydrophilic region (MHR) were analysed in 171 randomly selected subjects. RESULTS: The seroprevalence of HBV infection was 3.32% (1053/31 681). The predominant HBV genotypes were B (57.4%) and C (42.6%). Pregnant women ≥30 y of age exhibited a higher hepatitis B surface antigen-positive rate than those <30 y of age. MHR mutations were found in 42.6% (72/169) of the subjects, several of which were escape mutations. The mutational frequencies in the a-determinant and first loop (AA124-137) were higher in genotype C than genotype B. Pregnant women with MHR mutations showed increased alanine transaminase, aspartate transaminase and gamma-glutamyl transpeptidase levels and decreased HBV loads. CONCLUSIONS: The HBV seroprevalence among pregnant women in Huzhou was intermediate. MHR mutations occur and the risk of MTCT still persists. Therefore, early screening, intervention and care for HBV-infected pregnant women should be strengthened to minimize or prevent MTCT of HBV.

6.
RSC Adv ; 9(52): 30134-30138, 2019 Sep 23.
Article in English | MEDLINE | ID: mdl-35530243

ABSTRACT

In this study, we demonstrate an Ir(iii)-catalyzed thioether directed alkenylation of arene C-H bonds under mild reaction conditions. The selectivity for mono- or di-alkenylation is controlled by the concentration of alkene and oxidant loading. Various functional groups are tolerated, and moderate to good yields of alkenylated products are achieved.

7.
Bioorg Chem ; 122: 105714, 2022 05.
Article in English | MEDLINE | ID: mdl-35276603

ABSTRACT

18ß-glycyrrhetinic acid (GA) is a well-known natural compound of oleanane-type triterpene and is found possessing antimicrobial and anti-inflammatory properties. Nonetheless, its relatively low bioactivity restricts its potential in pharmaceutical applications. To maximize the potential use of this natural herbal compound as antimicrobial and anti-inflammatory agents, the rational modification of GA to enhance its pharmacological activity with low toxicity and to understand the mechanism of action is critically essential. We reported herein the design and synthesis of a series of new GA derivatives. The antimicrobial activities of these new compounds were evaluated by inhibition zone test and minimum inhibitory concentration (MIC) assay. In addition, the anti-inflammatory activity was evaluated by LPS induced BV2 cells inflammation model and 12-O-tetradecanoyl phorbol-13-acetate (TPA) induced ear inflammation mice model. It was found that the derivatives functionalized with a di-substituted phenyl group at the 2-position of GA generally displayed high antimicrobial activity against Gram-positive bacteria (MIC down to 2.5 µM) and potent anti-inflammatory effects (inhibition of NO production up to 55%, comparable to dexamethasone). The in vitro and in vivo results also showed that GA-O-02 and GA-O-06 exert their anti-inflammatory activities through downregulation of NO, pro-inflammatory cytokines and chemokines (IL-1ß, IL-6, IL-12, TNF-α, MCP-1 and MIP-1α) and upregulation of anti-inflammatory cytokines (IL-10). The anti-inflammatory mechanism may involve the inhibition of NF-κB, MAPKs and PI3K/Akt related inflammatory signaling pathways and activation of Nrf2/HO-1 signaling pathway. The results demonstrated that GA-O-02 and GA-O-06 possess great application potential as potent antimicrobial and anti-inflammatory agents.


Subject(s)
Glycyrrhetinic Acid , Phosphatidylinositol 3-Kinases , Animals , Anti-Bacterial Agents , Anti-Inflammatory Agents/pharmacology , Anti-Inflammatory Agents/therapeutic use , Glycyrrhetinic Acid/analogs & derivatives , Glycyrrhetinic Acid/pharmacology , Mice
8.
Food Funct ; 13(6): 3258-3270, 2022 Mar 21.
Article in English | MEDLINE | ID: mdl-35234233

ABSTRACT

Diabetic nephropathy (DN) is the most important cause of middle and late-stage chronic kidney disease. Green tea polypeptides are extracted from tea pomace, and exhibit various pharmacological effects. In this study, we analyzed the reno-protective effects of green tea peptides in diabetic db/db mice, and explored the underlying mechanisms. Peptide treatment for 5 weeks significantly reduced the blood glucose levels and other indices of diabetes, and alleviated renal injury measured in terms of blood creatinine, urea nitrogen and urinary albumin/urinary creatinine levels. Mechanistically, the green tea peptides downregulated p-Smad2/3, α-SMA, ZO-1 and vimentin proteins in the kidney tissues, and elevated Smad7. Thus, green tea peptides inhibited the deposition of ECM proteins by suppressing excessive activation of the TGF-ß/Smad signaling pathway and reducing fibronectin levels. On the other hand, tea peptides ameliorated renal injury by inhibiting the production of inflammatory factors (iNOS and TNF-α) by suppressing the NF-κB signaling pathway. In addition, we confirmed the inhibitory effect of green tea peptides on the TGF-ß/Smad signaling pathway in TGF-ß1-stimulated HK-2 cells. Therefore, tea peptides can be considered as an effective candidate for alleviating DN.


Subject(s)
Diabetic Nephropathies/drug therapy , Peptides/therapeutic use , Smad Proteins/metabolism , Tea/chemistry , Transforming Growth Factor beta/metabolism , Animals , Cell Line , Down-Regulation , Humans , Kidney/drug effects , Kidney/metabolism , Male , Mice , Mice, Inbred C57BL , Peptides/administration & dosage , Signal Transduction
9.
J Agric Food Chem ; 70(10): 3162-3171, 2022 Mar 16.
Article in English | MEDLINE | ID: mdl-35230106

ABSTRACT

5-Demethylated polymethoxyflavones (5-OH PMFs) are the most unique monodemethylated PMFs with relatively low polarities and are proved to possess better anticancer and anti-inflammatory effects than their respective permethoxylated ones. However, their detailed in vivo metabolic fates have not been fully studied. 5-Demethylsinensetin (5-OH Sin), being one of the 5-demethylated citrus PMFs, was used in the present research to investigate its biotransformation in pharmacokinetics and excretion in rats. The results showed that 5-OH Sin was mostly accumulated in the large intestine, indicating its poor absorption in the small intestine. In addition, 5,3'-didemethylsinensetin and 5,4'-didemethylsinensetin were identified as two dominated metabolites of 5-OH Sin, and the C-3' position of 5-OH Sin was more facile to be demethylated in systemic circulation. Moreover, other than demethylation reactions, the methylation transformation of 5-OH Sin and its metabolites were also observed and quantified, suggesting that the bidirectional biotransformation between 5-OH Sin and its parent compound, Sin, occurred under in vivo conditions.


Subject(s)
Citrus , Flavones , Animals , Biotransformation , Citrus/metabolism , Demethylation , Flavones/metabolism , Methylation , Rats
10.
PLoS One ; 17(2): e0264194, 2022.
Article in English | MEDLINE | ID: mdl-35192646

ABSTRACT

Physical and chemical methods for generating rat models of enteritis have been established; however, antibiotic induction has rarely been used for this purpose. The present study aimed to establish and evaluate a rat model of inflammatory bowel disease (IBD) using antibiotics. A total of 84 Sprague-Dawley (SD) rats were divided into the following groups, according to the dosage and method of administration of the antibiotics: A, control; B, low-dose clindamycin; C, medium-dose clindamycin; D, high-dose clindamycin; E, low-dose clindamycin, ampicillin and streptomycin; F, medium-dose clindamycin, ampicillin and streptomycin; and G, high-dose clindamycin, ampicillin and streptomycin. Antibiotic administration was stopped on day 7; the modeling period covered days 1-7, and the recovery period covered days 8-15. Half of the animals were dissected on day 11, with the remaining animals dissected on day 15. Food and water intake, body weight and fecal weight were recorded. Intestinal flora was analyzed via microbial culture and quantitative PCR. The content of TNF-α, IL1-ß, IL-6 and C-reactive protein (CRP) was assessed in abdominal aorta blood. Colonic and rectal tissues were examined pathologically via hematoxylin-eosin staining to assess leukocyte infiltration and intestinal mucosal changes as indicators of inflammation. Rat weight, food intake, water intake and 2-h fecal weight were significantly different across the experimental groups (P = 0.040, P = 0.016, P<0.001 and P = 0.009, respectively). Microbial cultures revealed no significant differences between group A and B,C (P = 0.546,0.872) but significant differences betwenn group A and the other experimental groups (all P<0.001). Furthermore, significant differences in the levels of Bacteroides, Faecalibacterium prausnitzii and Dialister invisus on day 4 between groups A, C and F (P = 0.033, P = 0.025 and P = 0.034, respectively). Significant differences were detected in the levels of TNF-α, IL1-ß, IL-6 and CRP between the groups (all P<0.001). The colonic and rectal pathological inflammation scores of the experimental groups were significantly different compared with group A (B vs. A, P = 0.002; others, all P<0.001). These findings indicated that an antibiotic-induced IBD model was successfully established in SD rats; this animal model may serve as a useful model for clinical IBD research.


Subject(s)
Anti-Bacterial Agents/toxicity , Disease Models, Animal , Inflammatory Bowel Diseases/physiopathology , Animals , C-Reactive Protein/metabolism , Female , Inflammatory Bowel Diseases/etiology , Inflammatory Bowel Diseases/metabolism , Interleukins/metabolism , Rats , Rats, Sprague-Dawley , Tumor Necrosis Factor-alpha/metabolism
11.
J Ethnopharmacol ; 290: 115119, 2022 May 23.
Article in English | MEDLINE | ID: mdl-35182669

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Several Amomum species are commonly used in food as flavoring agents and traditional Chinese medicine to treat inflammation-related diseases. AIM OF THE STUDY: This study aims to investigate the protective effects of Chinese herbal medicines, including six Amomum Roxb. essential oils (AEOs), against acute lung injury (ALI) induced by lipopolysaccharide (LPS) in mice. MATERIALS AND METHODS: The compositions of AEOs were analyzed using gas chromatography - mass spectrometry. RAW264.7 cells were treated with AEOS (0-100 µg/mL) and stimulated with LPS. C57 mice received AEOs (100 mg/kg) via atomization system for seven consecutive days, and then, intratracheal instillation of LPS was applied to establish an in vivo model of acute lung injury. RESULTS: We identified three AEOs demonstrating anti-inflammatory effects and amelioration of LPS-induced lung tissue pathological damage. Furthermore, we found that these AEOs reduced lung wet/dry weight ratios and protein concentrations in the bronchoalveolar lavage fluid of mice with LPS-induced ALI. Additionally, AEOs reduced the levels of malondialdehyde, TNF-α, IL-6, and IL-1ß but increased the levels of superoxide dismutase and catalase in lung tissue, alveolar lavage fluid, and serum samples. We also found that these three AEOs affected proteins related to the TLR4/Myd88/NF-κB pathway. CONCLUSIONS: In summary, our findings revealed that AEOs ameliorate inflammatory and oxidative stress in mice with ALI through the TLR4/Myd88/NF-κB pathway.


Subject(s)
Acute Lung Injury/pathology , Amomum , Oils, Volatile/pharmacology , Acute Lung Injury/chemically induced , Animals , Bronchoalveolar Lavage Fluid/chemistry , Catalase/drug effects , Cell Survival/drug effects , Disease Models, Animal , Inflammation Mediators/metabolism , Lipopolysaccharides/pharmacology , Lung/drug effects , Male , Membrane Glycoproteins/drug effects , Metabolomics , Mice , Mice, Inbred C57BL , NF-kappa B/drug effects , RAW 264.7 Cells , Random Allocation , Superoxide Dismutase/drug effects , Toll-Like Receptor 4/drug effects
12.
J Enzyme Inhib Med Chem ; 37(1): 451-461, 2022 Dec.
Article in English | MEDLINE | ID: mdl-35012401

ABSTRACT

Different oleanolic acid (OA) oxime ester derivatives (3a-3t) were designed and synthesised to develop inhibitors against α-glucosidase and α-amylase. All the synthesised OA derivatives were evaluated against α-glucosidase and α-amylase in vitro. Among them, compound 3a showed the highest α-glucosidase inhibition with an IC50 of 0.35 µM, which was ∼1900 times stronger than that of acarbose, meanwhile compound 3f exhibited the highest α-amylase inhibitory with an IC50 of 3.80 µM that was ∼26 times higher than that of acarbose. The inhibition kinetic studies showed that the inhibitory mechanism of compounds 3a and 3f were reversible and mixed types towards α-glucosidase and α-amylase, respectively. Molecular docking studies analysed the interaction between compound and two enzymes, respectively. Furthermore, cytotoxicity evaluation assay demonstrated a high level of safety profile of compounds 3a and 3f against 3T3-L1 and HepG2 cells.HighlightsOleanolic acid oxime ester derivatives (3a-3t) were synthesised and screened against α-glucosidase and α-amylase.Compound 3a showed the highest α-glucosidase inhibitory with IC50 of 0.35 µM.Compound 3f presented the highest α-amylase inhibitory with IC50 of 3.80 µM.Kinetic studies and in silico studies analysed the binding between compounds and α-glucosidase or α-amylase.


Subject(s)
Enzyme Inhibitors/pharmacology , Esters/pharmacology , Oleanolic Acid/pharmacology , Oximes/pharmacology , alpha-Amylases/antagonists & inhibitors , alpha-Glucosidases/metabolism , Dose-Response Relationship, Drug , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Esters/chemical synthesis , Esters/chemistry , Humans , Molecular Structure , Oleanolic Acid/chemical synthesis , Oleanolic Acid/chemistry , Oximes/chemical synthesis , Oximes/chemistry , Structure-Activity Relationship , alpha-Amylases/metabolism
13.
J Enzyme Inhib Med Chem ; 37(1): 542-553, 2022 Dec.
Article in English | MEDLINE | ID: mdl-34986722

ABSTRACT

Roburic acid (ROB) is a naturally occurred tetracyclic triterpenoid, and the anticancer activity of this compound has not been reported. Docetaxel (DOC) is the first-line chemotherapeutic agent for advanced stage prostate cancer but toxic side effects and drug resistance limit its clinical success. In this study, the potential synergistic anticancer effect and the underlying mechanisms of ROB in combination with DOC on prostate cancer were investigated. The results showed that ROB and DOC in combination synergistically inhibited the growth of prostate cancer cells. The combination also strongly induced apoptosis, and suppressed cell migration, invasion and sphere formation. Mechanistic study showed that the combined effects of ROB and DOC on prostate cancer cells were associated with inhibition of NF-κB activation, down regulation of Bcl-2 and up regulation of Bax. Knockdown of NF-κB by small interfering RNA (siRNA) significantly decreased the combined effect of ROB and DOC. Moreover, we found that esomeprazole (ESOM), a proton pump inhibitor (PPI), strongly enhanced the effectiveness of ROB and DOC on prostate cancer cells in acidic culture medium. Since acidic micro environment is known to impair the efficacy of current anticancer therapies, ESOM combined with ROB and DOC may be an effective approach for improving the treatment of prostate cancer patients.


Subject(s)
Antineoplastic Combined Chemotherapy Protocols/pharmacology , Docetaxel/pharmacology , Prostatic Neoplasms/drug therapy , Antineoplastic Combined Chemotherapy Protocols/chemical synthesis , Antineoplastic Combined Chemotherapy Protocols/chemistry , Cell Proliferation/drug effects , Cell Survival/drug effects , Docetaxel/chemistry , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Esomeprazole/chemistry , Esomeprazole/pharmacology , Humans , Male , Molecular Structure , NF-kappa B/antagonists & inhibitors , NF-kappa B/metabolism , Prostatic Neoplasms/metabolism , Prostatic Neoplasms/pathology , Proto-Oncogene Proteins c-bcl-2/antagonists & inhibitors , Proto-Oncogene Proteins c-bcl-2/metabolism , Structure-Activity Relationship , Tumor Cells, Cultured
14.
Chin J Nat Med ; 19(11): 874-880, 2021 Nov.
Article in English | MEDLINE | ID: mdl-34844726

ABSTRACT

Nine new compounds, including five natural rarely-occurring 2, 3-dihydro-1H-indene derivatives named diaporindenes E-I (1-5), and four new benzophenone analogues named tenellones J-M (6-9) were isolated from the deep-sea sediment-derived fungus Phomopsis lithocarpus FS508. All the structures for these new compounds were fully characterized on the basis of spectroscopic data, NMR spectra, and ECD calculation and single-crystal X-ray diffraction analysis. The potential anti-tumor activities of compounds 1-9 against four tumor cell lines SF-268, MCF-7, HepG-2, and A549 were evaluated using the SRB method. Compound 7 exhibited cytotoxic activity against the SF-268 cell line with an IC50 value of 11.36 µmol·L-1.


Subject(s)
Antineoplastic Agents , Phomopsis , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Crystallography, X-Ray , Fungi , Molecular Structure
15.
Pak J Pharm Sci ; 34(5): 1715-1722, 2021 Sep.
Article in English | MEDLINE | ID: mdl-34803007

ABSTRACT

Ranitidine hydrochloride (RH) resinates were prepared by bath method using a highly acidic cation-exchange resin as the carrier. The drug-resinates combination pattern was characterized by DSC and X-ray diffraction. The influences of the types of the ion-exchange resin, initial RH concentration and the reaction temperature on the process of ion exchange were investigated. Three empirical kinetics models and thermodynamics equations were studied to the ion exchange process under different temperatures. The results showed that RH combined with ion-exchange resin not simple physical mixture but by ion bond, and the rate of ion exchange increased on increasing the initial drug concentration and reducing the temperature the resin. The in vitro drug release test showed that the release process was affected by the kind of countra-ion, ionic strength and temperature. Thermodynamics results showed that the ion exchange reaction between RH and cation-exchange resin was exothermic (ΔHθr,m< <0), and the drug release process could preferably be fitted with the first order equation. In conclusion, RH resinates were prepared by the bath method with strongly acidic cation-exchange (Amberlite® IRP69) with 5 mg/mL RH solution(100mL) stirred at 298K for 1h. Drug release from resinates was fitted with Viswanathan equation, and to achieve obvious sustained-release effect, the RH-resin complex should be further coated with a semipermeable membrane.


Subject(s)
Ion Exchange Resins , Ranitidine/chemistry , Ranitidine/pharmacokinetics , Calorimetry, Differential Scanning , Drug Liberation , Kinetics , Osmolar Concentration , Temperature , Thermodynamics
16.
J Agric Food Chem ; 69(47): 14143-14150, 2021 Dec 01.
Article in English | MEDLINE | ID: mdl-34797063

ABSTRACT

As one of the major polymethoxyflavones in citrus peels, sinensetin (Sin) has been reported to possess numerous bioactivities. However, its detailed in vivo metabolic fate has not been uncovered yet. In the present study, the possible metabolites of Sin were synthesized, and all five mono-demethylated metabolites were successfully identified via ultraperformance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) analysis in rats fed with 100 mg/(kg·bw) Sin. The excretion and pharmacokinetic studies were then carried out to quantitatively investigate their variation in content with time in urine, feces, and plasma samples. Results showed that 4'-demethylsinensetin, 6-demethylsinensetin, and 3'-demethylsinensetin were the three most abundant metabolites generated in the above-mentioned biological samples. In addition, the total amount of Sin with its metabolites showed a significantly higher content in urine than in feces, indicating that Sin may be easily absorbed in the small intestine.


Subject(s)
Tandem Mass Spectrometry , Animals , Biotransformation , Chromatography, High Pressure Liquid , Chromatography, Liquid , Feces , Flavonoids , Rats
17.
Int J Food Sci Nutr ; : 1-11, 2021 Oct 31.
Article in English | MEDLINE | ID: mdl-34719319

ABSTRACT

Oleuropein (OLE) and hydroxytyrosol (HT) are dietary polyphenols with skin beneficial effects but their effects on skin-ageing-related enzymes are not clear. Herein, we evaluated their inhibitory effects on elastase and collagenase. OLE and HT (62.5-1 000 µM) showed moderate anti-elastase and anti-collagenase effects (5.1-26.3%, 5.8-12.2% and 12.6-31.0%, 11.6-31.9% inhibition, respectively). Combinations of OLE and HT (1:1 ratio) exerted synergistic inhibitory effects on elastase, which were supported by their combination index (CI), kinetic assay and computational docking. Moreover, HT (100 µM) reduced hydrogen peroxide (H2O2)-induced cytotoxicity and reactive oxygen species (ROS) in human dermal fibroblast cells by 21.8 and 15.2%, respectively. In addition, combinations of OLE and HT (6.25/6.25-100/100 µM) exerted synergistic cytoprotective effects by reducing ROS levels by 7.6-37.3% with CIs of 0.17-0.44, respectively. The findings from this study support the cosmeceutical activities of OLE and HT but further research is warranted to evaluate their anti-skin-ageing effects using in vivo models.

18.
Nanomaterials (Basel) ; 11(10)2021 Sep 22.
Article in English | MEDLINE | ID: mdl-34684916

ABSTRACT

Rare Earth Upconversion nanoparticles (UCNPs) are a type of material that emits high-energy photons by absorbing two or more low-energy photons caused by the anti-stokes process. It can emit ultraviolet (UV) visible light or near-infrared (NIR) luminescence upon NIR light excitation. Due to its excellent physical and chemical properties, including exceptional optical stability, narrow emission band, enormous Anti-Stokes spectral shift, high light penetration in biological tissues, long luminescent lifetime, and a high signal-to-noise ratio, it shows a prodigious application potential for bio-imaging and photodynamic therapy. This paper will briefly introduce the physical mechanism of upconversion luminescence (UCL) and focus on their research progress and achievements in bio-imaging, bio-detection, and photodynamic therapy.

19.
Fitoterapia ; 155: 105061, 2021 Nov.
Article in English | MEDLINE | ID: mdl-34673146

ABSTRACT

Clinacanthus nutans Lindau (Family: Acanthaceae) is a medicinal herb widely distributed in the tropic and subtropic areas of Asia. C. nutans is traditionally consumed as vegetable or herbal tea, as well as a folk medicine for anticancer and antifungal activities. However, to date, chemical constituent responsible for observed health beneficial effects of this medicinal plant is not clear. In the current study, 32 compounds (1-32), including three new megastigmanes (1-3) were isolated from the aerial parts of C. nutans. Their structures were elucidated on the basis of comprehensive NMR, MS, and CD spectroscopic data analysis, as well as chemical hydrolysis. Among the isolates, cycloartane triterpenoids (9, 10, and 12) displayed moderate anti-proliferative effects against HepG2 cell growth with IC50 values ranging from 9.12 to 19.89 µM. Data obtained from flow cytometry analysis and western blotting assays revealed that compounds 9 and 12 induced apoptosis of HepG2 cells by modulating the expression of proteins associated to mitochondrial-mediated apoptotic pathway. Furthermore, megastigmanes 1, 2, 7, and 8 enhanced the anti-Candida albicans activity of amphotericin B (AmB), supporting the synergistic effects between megastigmanes and AmB. This is the first report of anticancer and antifungal potential of cycloartane triterpenoids and megastigmanes in C. nutans, which shed useful insights on the relationship between C. nutans's chemical constituent and its beneficial effects to health. Findings from this study support further development of this medicinal plant for potential pharmaceutical applications.


Subject(s)
Acanthaceae/chemistry , Antifungal Agents/pharmacology , Antineoplastic Agents, Phytogenic/pharmacology , Norisoprenoids/pharmacology , Triterpenes/pharmacology , Antifungal Agents/isolation & purification , Antineoplastic Agents, Phytogenic/isolation & purification , Apoptosis/drug effects , Candida albicans/drug effects , China , Hep G2 Cells , Humans , Molecular Structure , Norisoprenoids/isolation & purification , Phytochemicals/isolation & purification , Phytochemicals/pharmacology , Plant Components, Aerial/chemistry , Plants, Medicinal/chemistry , Triterpenes/isolation & purification
20.
Int J Biol Macromol ; 193(Pt A): 71-80, 2021 Dec 15.
Article in English | MEDLINE | ID: mdl-34637817

ABSTRACT

Herein, a TEMPO-oxidized cellulose-grafted-polystyrene hypercrosslinked polymer (TOC-PS-HCP) was synthesized facilely by TEMPO oxidation, grafting copolymerization and post crosslinking route. Based on the structural characterization, it was confirmed that TOC-PS-HCP mainly consisted of polystyrene chain on cellulose and rigid crosslinked bridge. Additionally, the as-prepared TOC-PS-HCP displayed appropriate hydrophobicity (water contact angle = 102.44°) and high specific surface area (SBET = 601.20 m2·g--1), which could efficiently recover ethylbenzene and styrene from PO/SM wastewater. The adsorption experiment was conducted to study the recovery performance for ethylbenzene and styrene in the aqueous phase. The results showed that TOC-PS-HCP could recover ethylbenzene and styrene quickly by adsorption process, and maintain a stable recovery rate both in different aqueous conditions and recycle experiments. The adsorption experiment in the simulated wastewater solution showed that TOC-PS-HCP exhibited the greater affinity for ethylbenzene and styrene than other substrates. Furthermore, a possible mechanism for the efficient recovery of ethylbenzene and styrene was suggested on the basis of experimental and theoretical results, which may be associated with van der Waals force and π-π stacking.


Subject(s)
Cellulose/chemistry , Cyclic N-Oxides/chemistry , Polymers/chemistry , Waste Water/chemistry , Water Purification/methods , Adsorption
SELECTION OF CITATIONS
SEARCH DETAIL