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1.
Opt Lett ; 48(2): 379-382, 2023 Jan 15.
Article in English | MEDLINE | ID: mdl-36638462

ABSTRACT

We propose an absorption intensity heartbeat modulation-averaged shifted histogram (AIHM-ASH) method for estimating human heart rate (HR) using color videos of lip image sequences. When heartbeat occurs, AIHM is generated. Based on the AIHM, HR signals can be demodulated by computing the instantaneous HR modulation depth that presents the relative red blood cell (RBC) concentration from the green channel image of the RGB color video. In addition, the ASH algorithm further suppresses the background tissue and vein signals, and increases the signal-to-noise ratio (SNR). The experimental results for flow phantoms, chicken embryos, and human lips validated the proposed method's optimal estimation conditions and effectiveness, where the accuracy and root mean square error (RMSE) were 99.23% and 0.8 bpm, respectively. The proposed HR estimation method has significant potential to advance health monitoring and disease prevention via conventional color video cameras installed in public places.


Subject(s)
Algorithms , Chick Embryo , Humans , Animals , Heart Rate/physiology , Signal-To-Noise Ratio , Color
2.
Opt Lett ; 47(22): 5837-5840, 2022 Nov 15.
Article in English | MEDLINE | ID: mdl-37219116

ABSTRACT

We propose a multi-mode optical imaging method to retrieve the 2D and 3D spatial structures of the preheating, reaction, and recombination zones of an axisymmetric steady flame. In the proposed method, an infrared camera, a visible light monochromatic camera, and a polarization camera are triggered synchronously to capture 2D flame images, and their corresponding 3D images are reconstructed by combining different projection position images. The results of the experiments conducted indicate that the infrared and visible light images represent the flame preheating and flame reaction zones, respectively. The polarized image can be obtained by computing the degree of linear polarization (DOLP) of raw images captured by the polarization camera. We discover that the highlighted regions in the DOLP images lie outside the infrared and visible light zones; they are insensitive to the flame reaction and have different spatial structures for different fuels. We deduce that the combustion product particles cause endogenic polarized scattering, and that the DOLP images represent the flame recombination zone. This study focuses on the combustion mechanisms, such as the formation of combustion products and quantitative flame composition and structure.

3.
Biomed Chromatogr ; 34(8): e4865, 2020 Aug.
Article in English | MEDLINE | ID: mdl-32330321

ABSTRACT

The aerial parts of Dracocephalum moldavica L. are extensively used in traditional ethnic medicines in China as a remedy for cardiovascular and cerebrovascular damage. However, the chemical composition and the accumulation of main secondary metabolites of D. moldavica in different natural environments remain unclear. This study aimed to conduct a qualitative and quantitative analysis of the main secondary metabolites to explore the quality variation of D. moldavica in markets. The evaluation of space-time accumulation of main secondary metabolites in D. moldavica was carried out during different growth periods and in different geographical locations. A total of 35 ingredients were detected and 24 identified, including 21 flavonoids, two phenolic acids and one coumarin by UPLC-QTOF-MS method. Furthermore, a simple and convenient HPLC method was successfully developed for the simultaneous determination of lutelin-7-O-glucuronide and tilianin and rosmarinic acid in D. moldavica. The results of space-time accumulation analysis showed the distinct variation of secondary metabolites of D. moldavica with the growth period and geographical location. Finally, the current study provided a meaningful and useful approach for comprehensively evaluating the quality of D. moldavica.


Subject(s)
Chromatography, High Pressure Liquid/methods , Lamiaceae/chemistry , Lamiaceae/metabolism , Mass Spectrometry/methods , Phytochemicals/analysis , Coumarins/analysis , Coumarins/chemistry , Coumarins/metabolism , Hydroxybenzoates/analysis , Hydroxybenzoates/chemistry , Hydroxybenzoates/metabolism , Limit of Detection , Linear Models , Phytochemicals/chemistry , Phytochemicals/metabolism , Plant Extracts/chemistry , Plant Structures/chemistry , Plant Structures/metabolism , Reproducibility of Results
4.
Biomed Chromatogr ; 33(12): e4690, 2019 Dec.
Article in English | MEDLINE | ID: mdl-31452234

ABSTRACT

Traditionally, pomegranate (Punica granatum L.) has been consumed as fresh fruit or as pomegranate juice. Pomegranate peel, the dried husk of P· granatum, is an important herbal medicine for treating diarrhea, hemostasis and insect-induced abdominal pain in China. However, the quality control methods for pomegranate peel remain unsatisfactory. In this work, a new HPLC-based qualitative and quantitative method for quality control of pomegranate peel was developed and validated for the simultaneous determination of polyphenols and triterpenes (including punicalagins A and B, ellagic acid, oleanolic acid and ursolic acid) by solvent extraction and ratio blending method in tandem with wavelength switching. The average recoveries were 98.07-100.61% with relative standard deviation no more than 4.27%. In addition, the fingerprint analysis was conducted to interpret the consistency of the quality test. Thirteen characteristic peaks were selected to evaluate the similarities of 16 batches of pomegranate peel. The similarities of samples were all more than 0.80, indicating that the samples from different areas of China were consistent. The results demonstrated that quantitative analysis and the HPLC fingerprint as a characteristic distinguishing method combining similarity evaluation can be successfully used to assess the quality and to identify the authenticity of pomegranate peel.


Subject(s)
Lythraceae/chemistry , Plant Extracts/analysis , Polyphenols/analysis , Triterpenes/analysis , Chromatography, High Pressure Liquid/methods , Fruit/chemistry , Limit of Detection , Linear Models , Reproducibility of Results
5.
Molecules ; 24(7)2019 Apr 11.
Article in English | MEDLINE | ID: mdl-30978991

ABSTRACT

Harmine (HAR) is a beta-carboline alkaloid widely distributed in nature. It exhibits psychopharmacological effects of improving learning and memory. However, excessive dose of HAR can cause central tremor toxicity, which may be related to the glutamate system. Memantine (MEM) is a non-competitive N-methyl-d-aspartate receptor antagonist. It can be used for the treatment of Alzheimer's disease and also can block the neurotoxicity caused by glutamate. Therefore, combination of HAR and MEM would be meaningful and the pharmacokinetics investigation of HAR and MEM in combination is necessary. A ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method was established and validated for the simultaneous quantitative determination of MEM, HAR and harmol (HOL), a main metabolite of HAR, in rat plasma after oral administration of HAR and MEM in combination (5.0 mg/kg of MEM combined with 20.0, 40.0, 80.0 mg/kg of HAR). The contents of HAR and HOL were determined after oral administration of HAR (20.0, 40.0 and 80.0 mg/kg), and the content of MEM was determined after oral administration of MEM (5.0 mg/kg). Blood samples were collected from each rat at 0 (pre-dose), 0.08, 0.17, 0.25, 0.33, 0.50, 0.75, 1.0, 2.0, 4.0, 8.0, 12.0 and 24.0 h after administration. The maximum peak concentration (Cmax) of MEM was obviously decreased, and the area under the plasma concentration versus time curve from zero to time t (AUC(0-t)) and mean residence time (MRT) were significantly increased after combination with HAR. The Cmax and AUC(0-t) of HAR and its metabolite HOL were increased after combination with MEM. These findings suggested that co-administration of HAR and MEM could extend their residence time in rats, and then might increase the efficacy for treatment of Alzheimer's disease. Therefore, this study will provide a basis for the rational combined application of HAR and MEM.


Subject(s)
Harmine/chemistry , Memantine/chemistry , Pharmacokinetics , Receptors, N-Methyl-D-Aspartate/chemistry , Cholinesterase Inhibitors/chemistry , Cholinesterase Inhibitors/pharmacokinetics , Drug Interactions , Harmine/pharmacokinetics , Humans , Memantine/pharmacokinetics , Receptors, N-Methyl-D-Aspartate/antagonists & inhibitors
6.
Biomed Chromatogr ; 32(11): e4341, 2018 Nov.
Article in English | MEDLINE | ID: mdl-30007052

ABSTRACT

Gentiana Macrophylla Radix (GMR) is officially used as traditional Chinese medicine, but easily confused with Gentianae Radix et Rhizoma (GRR) and adulterants. This study aimed to establish an HPLC method for qualitative and quantitative analysis of GMR based on characteristic components, anofinic acid and its derivatives. HPLC analysis was performed on a C18 column with gradient elution using acetonitrile and 0.1% phosphoric acid as mobile phase, and detected at 240 nm by conventional methodology validation. For fingerprint analysis, RSDs of relative retention times and relative peak areas of the characteristic peaks were within 0-1.10 and 0-4.08%, respectively. For determination of 2-methoxyanofinic acid, the calibration curve showed good linearity (R2 > 0.9999) within the test range. The RSDs of precision, repeatability and stability test did not exceed 2.46, 0.83 and 1.11%, respectively. The average recoveries were between 95.08 and 103.05% with RSDs ≤2.29%. The results showed that there was no significant difference among the four species of GMR, but there were significant differences among GMR, GRR and spurious breeds by principal component analysis and hierarchical cluster analysis. Anofinic acid and its derivatives, as the characteristic markers, could be used for the identification and quality control of GMR.


Subject(s)
Benzopyrans/analysis , Chromatography, High Pressure Liquid/methods , Drugs, Chinese Herbal/analysis , Benzopyrans/chemistry , Cluster Analysis , Drugs, Chinese Herbal/chemistry , Linear Models , Principal Component Analysis , Reproducibility of Results , Sensitivity and Specificity
7.
Nanomedicine ; 12(1): 235-44, 2016 Jan.
Article in English | MEDLINE | ID: mdl-26393884

ABSTRACT

Microwave-induced thermoacoustic imaging (TAI) can map the microwave absorption distribution of targets, which depends on the electrical and magnetic properties. Although carbon nanotubes (CNTs) with good electrical properties have been used as TAI contrast agents, the negligible magnetic absorption hinders its application for sensitive detection. In order to exploit CNTs with electrical and magnetic absorption properties as agent of TAI, the ferromagnetic material-filled multi-walled CNTs (MMWCNTs) are investigated. In this study, the folic acid conjugated plain multiwalled CNTs (MWCNTs) and MMWCNTs were injected through the tail-vein of mice separately, and TAI and magnetic resonance imaging (MRI) were performed. The results show the MMWCNTs can clearly image the size and edge of the tumor with the TAI contrast enhancement of 67% and T2 signal intensity decrease of four fifths compared to MWCNTs. This study demonstrated the hybrid particles have the potential to be a high-sensitive contrast agent for accurate tumor detection. From the Clinical Editor: Novel imaging modalities are emerging. Microwave-induced thermoacoustic imaging (TAI) relies on the absorption distribution of microwave of targets. In this article the authors investigate the use of ferromagnetic material-filled multi-walled CNTs as contrast agents for both TAI and MRI in an in-vivo model for tumors. The positive findings would imply that the application of dual-modality probe could provide more accurate imaging for the clinical setting.


Subject(s)
Iron/chemistry , Magnetic Resonance Imaging/methods , Multimodal Imaging/methods , Nanotubes, Carbon/chemistry , Neoplasms, Experimental/pathology , Thermography/methods , Animals , Contrast Media/chemical synthesis , Elasticity Imaging Techniques/methods , Female , Folic Acid/chemistry , Folic Acid/pharmacokinetics , Magnetite Nanoparticles/chemistry , Mice , Mice, Inbred BALB C , Microwaves , Nanotubes, Carbon/ultrastructure , Neoplasms, Experimental/metabolism , Reproducibility of Results , Sensitivity and Specificity
8.
Ultrason Imaging ; 38(4): 276-84, 2016 07.
Article in English | MEDLINE | ID: mdl-26294659

ABSTRACT

To receive the information necessary for imaging, traditional microwave-induced thermoacoustic imaging systems (MITISs) use a type of circular-scanning mode using single or arc detectors. However, the use of MITISs for body scanning is complicated by restrictions in space and imaging time. A linear-array detector, the most widely used transducer in medical ultrasound imaging systems for body scanning, is a possible alternative to MITISs for scanning biological tissues, such as from the breast or limbs. In this paper, a handheld MITIS, based on a linear-array detector and a multiple data acquisition system, is described, and the capacity of the system is explored experimentally. First, the vertical and lateral resolution of the system is discussed. Next, real-time imaging of a moving object, obtained with an image capture rate of 20 frame/s, is described. Finally, a phantom experiment is detailed, investigating the overall imaging capability. The results show that this system achieves rapid scanning with a large field of view. The system has the obvious advantages of being handheld, not using coupled fluids, and achieving real-time imaging with a large field of view, which make this MITIS more suitable for clinical applications.


Subject(s)
Image Processing, Computer-Assisted/methods , Transducers , Ultrasonography/instrumentation , Ultrasonography/methods , Microwaves , Phantoms, Imaging
9.
J Biophotonics ; 16(6): e202200370, 2023 06.
Article in English | MEDLINE | ID: mdl-36633529

ABSTRACT

A deep learning model called choroidal vascularity index (CVI)-Net is proposed to automatically segment the choroid layer and its vessels in overall optical coherence tomography (OCT) scans. Clinical parameters are then automatically quantified to determine structural and vascular changes in the choroid with the progression of diabetic retinopathy (DR) severity. The study includes 65 eyes consisting of 34 with proliferative DR (PDR), 17 with nonproliferative DR (NPDR), and 14 healthy controls from two OCT systems. On a dataset of 396 OCT B-scan images with manually annotated ground truths, overall Dice coefficients of 96.6 ± 1.5 and 89.1 ± 3.1 are obtained by CVI-Net for the choroid layer and vessel segmentation, respectively. The mean CVI values among the normal, NPDR, and PDR groups are consistent with reported outcomes. Statistical results indicate that CVI shows a significant negative correlation with DR severity level, and this correlation is independent of changes in other physiological parameters.


Subject(s)
Diabetes Mellitus , Diabetic Retinopathy , Humans , Diabetic Retinopathy/diagnostic imaging , Tomography, Optical Coherence/methods , Choroid/diagnostic imaging , Choroid/blood supply
10.
Biosensors (Basel) ; 11(11)2021 Oct 25.
Article in English | MEDLINE | ID: mdl-34821632

ABSTRACT

Suspended particles play a significant role in aquatic systems. However, existing methods to probe suspended particles have several limitations. In this paper, we present a portable prototype to in situ probe individual particles in aquatic suspensions by simultaneously measuring polarized light scattering and fluorescence, aiming to obtain an effective classification of microplastics and microalgae. Results show that the obtained classification accuracy is significantly higher than that for either of these two methods. The setup also successfully measures submicron particles and discriminates two species of Synechococcus. Our study demonstrates the feasibility of simultaneously measuring polarized light scattering and fluorescence, and the promising capability of our method for further aquatic environmental monitoring.


Subject(s)
Light , Plastics , Environmental Monitoring , Scattering, Radiation , Suspensions
11.
Front Physiol ; 11: 606769, 2020.
Article in English | MEDLINE | ID: mdl-33362581

ABSTRACT

The controversy over the evolution of sex gap in sports stems from the reported that women's performance will 1 day overtake men's in the journal Nature. After debate, the recent studies suggest that the sports sex gap has been stable for a long time, due to insurmountable physiological differences. To find a mathematical model that accurately describes this stable gap, we analyze the best annual records of men and women in 25 events from 1992 to 2017, and find that power-law relationship could be acted as the best choice, with an R-squares as high as 0.999 (p ≤ 0.001). Then, based on the power law model, we use the records of men in 2018 to predict the performance of women in that year and compare them with real records. The results show that the deviation rate of the predicted value is only about 2.08%. As a conclusion, it could be said that there is a constant sex gap in sports, and the records of men and women evolve in parallel. This finding could serve as another quantitative rule in biology.

12.
J Pharm Biomed Anal ; 186: 113232, 2020 Jul 15.
Article in English | MEDLINE | ID: mdl-32229392

ABSTRACT

Zanthoxylum nitidum (Roxb.) DC. (ZN) belongs to the genus Zanthoxylum of Rutaceae and has various chemical ingredients and pharmacologic effects. Alkaloids are its main active constituents responsible for diverse pharmacologic effects, such as anti-tumor, anti-bacterial, anti-inflammatory, and analgesic activities. The chemical and pharmacological effects of ZN are well reported, but the in vivo pharmacokinetic profiles of its main active alkaloids are poorly investigated. This study aims to elucidate the absorbed constituents and pharmacokinetic behavior of main active ingredients in rat plasma after the oral administration of ZN extract. The absorbed constituents in rat plasma were qualitatively analyzed using ultra-high-performance liquid chromatography with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF-MS). Ultra-high-performance liquid chromatography with triple quadrupole mass spectrometry (UPLC-MS/MS) method was developed for the simultaneous determination and pharmacokinetic studies of dihydrochelerythrine (DHCHE), nitidine chloride (NIT), chelerythrine (CHE), sanguinarine (SAN), liriodenine (LIR), skimmianine (SKI), γ-fagarine (FAG), and dictamnine (DIC) in rat plasma. Eighteen prototypes and metabolites were identified according to exact mass, characteristic diagnostic fragment ions, and reference standards. The established UPLC-MS/MS quantitative method met the requirements of FDA for biological analysis methods. Method validation showed that this method has good linearity (r ≥ 0.9910), precision (RSD ≤ 18.63 %), accuracy (88.11 %-117.50 %), and stability. The limit of detection (LOD) could reach 1 ng/mL, and the limit of quantitation could reach 2 ng/mL. The plasma drug concentration of benzophenanthridine alkaloids, such as NIT, CHE, and DHCHE, were still low even after dose differences were deducted. For the furan quinoline alkaloids (such as SKI, FAG, and DIC), only SKI showed high plasma drug concentration, although SKI content comprised only approximately 1/6 of benzophenanthridine alkaloids. This study is the first to simultaneously determine the above-mentioned active alkaloids in rat plasma and would contribute to the comprehensive understanding of in vivo pharmacokinetic behavior on active alkaloids in ZN extract.


Subject(s)
Alkaloids/blood , Drugs, Chinese Herbal/pharmacokinetics , Tandem Mass Spectrometry/methods , Zanthoxylum/chemistry , Administration, Oral , Alkaloids/pharmacokinetics , Animals , Chromatography, High Pressure Liquid/methods , Drugs, Chinese Herbal/administration & dosage , Drugs, Chinese Herbal/chemistry , Male , Models, Animal , Rats
13.
Materials (Basel) ; 12(1)2019 Jan 02.
Article in English | MEDLINE | ID: mdl-30609701

ABSTRACT

The setting of cutting variables for precision milling of ceramics is important to both the machined surface quality and material removal rate (MRR). This work specifically aims at the performance of corner radius PCD (polycrystalline diamond) end mill in precision milling of zirconia ceramics with relatively big cutting parameters. The characteristics of the cutting zone in precision milling ceramics with corner radius end mill are analyzed. The relationships between the maximum uncut chip thickness (hmax) and the milling parameters including feed per tooth (fz), axial depth of cut (ap) and tool corner radius (rε) are discussed. Precision milling experiments with exploratory milling parameters that cause uncut chip thickness larger than the critical value were carried out. The material removal mechanism was also analyzed. According to the results, it is advisable to increase fz appropriately during precision milling ZrO2 ceramics with corner radius end mill. There is still a chance to obtain ductile processed surface, as long as the brittle failure area is controlled within a certain range. The appropriate increasing of ap, not only can prevent the brittle damage from affecting the machined surface, but also could increase the MRR. The milling force increases with increasing MRR, but the surface roughness can still be stabilized within a certain range.

14.
Phytomedicine ; 63: 153007, 2019 Oct.
Article in English | MEDLINE | ID: mdl-31301537

ABSTRACT

BACKGROUND: Aerial parts of Peganum harmala Linn is used as a traditional medical herb for treatment of amnesia in Uighur medicine in China. Deoxyvasicine (DVAS) is one of the chief active ingredients in P. harmala, it possesses strong acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities in vitro, but the therapeutic effect and mechanisms on amnesia in vivo are unclear. PURPOSE: The objective of this study was to investigate the improvement effect of DVAS from P. harmala in learning and memory deficits of scopolamine-induced mice and elucidate the underlying mechanisms involved. METHODS: Mice were pretreated with DVAS (5, 15 and 45 mg/kg) and huperzine-A (0.2 mg/kg) by gavage for 7 days, and subsequently were daily intraperitoneally injected with scopolamine (1 mg/kg) to induce learning and memory deficits and behavioral performance was assessed by Morris water maze. To further evaluate the potential mechanisms of DVAS in improving learning and memory capabilities, pathological change, levels of various biochemical markers and protein expressions related to cholinergic system, oxidative stress, and neuroinflammation were examined. RESULTS: The results showed that DVAS could alleviate learning and memory deficits in scopolamine-treated mice. DVAS could regulate cholinergic function by inhibiting AChE and activating choline acetyltransferase (ChAT) activities and protein expressions. DVAS could induce brain-derived neurotrophic factor and protect hippocampal pyramidal cells against neuronal damage. DVAS also enhanced antioxidant defense via increasing the antioxidant enzyme level and activity of glutathione peroxidase, and anti-inflammatory function through suppressing tumor necrosis factor-α. Additionally, DVAS could regulate the neurotransmitters by elevating acetylcholine, 5-hydroxytryptamine, γ-aminobutyric acid and reducing 5-hydroxyindole-3-acetic acid and glutamic acid. CONCLUSION: Results illustrated that DVAS may be a promising candidate compound against amnesia via restoration of cholinergic function, regulating neurotransmitters, attenuating neuroinflammation and oxidative stress.


Subject(s)
Alkaloids/pharmacology , Cognitive Dysfunction/drug therapy , Hippocampus/drug effects , Quinazolines/pharmacology , Acetylcholine/metabolism , Amnesia/drug therapy , Animals , Antioxidants/metabolism , Brain-Derived Neurotrophic Factor/metabolism , Cholinesterase Inhibitors/pharmacology , Cognitive Dysfunction/chemically induced , Cognitive Dysfunction/metabolism , Male , Memory/drug effects , Memory Disorders/chemically induced , Memory Disorders/drug therapy , Mice, Inbred C57BL , Neurotransmitter Agents/metabolism , Oxidative Stress/drug effects , Peganum/chemistry , Scopolamine/toxicity , Sesquiterpenes/pharmacology
15.
J Ethnopharmacol ; 236: 288-301, 2019 May 23.
Article in English | MEDLINE | ID: mdl-30872168

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Aerial parts of Peganum harmala Linn are a Uighur traditional medicinal herb in China used to treat amnesia, bronchial asthma, and cough. Deoxyvasicine (DVAS), a potent cholinesterase inhibitor exhibiting anti-senile dementia activity, is one of the chief active ingredients in aerial parts of P. harmala and plays a key role in mediating the pharmacological effects of P. harmala. However, the metabolic profiling and in vivo pharmacokinetic characteristics of DVAS still remain unknown. AIM OF THE STUDY: The aim of this present study was to investigate the metabolism and pharmacokinetic properties of DVAS in rats by using ultra-performance liquid chromatography combined with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (UPLC-ESI-QTOF-MS) and ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-ESI-MS/MS) method. MATERIALS AND METHODS: The metabolic profiling of DVAS was evaluated in vitro and in vivo by rat liver microsomes (RLMs) incubation and by rat bio-specimens, such as urine, feces, plasma, and bile, after the oral administration of 45 mg/kg DVAS. An efficient and sensitive UPLC-ESI-MS/MS method was developed and validated to simultaneously determine DVAS and its major four metabolites, namely, vasicine, deoxyvasicinone, vasicinone, and 1,2,3,9-tetrahydropyrrolo[2,1-b]quinazolin-3-ß-D-glucuronide in rat plasma. For pharmacokinetic studies, 32 Sprague-Dawley rats were randomly divided into four groups, namely, intravenous dosage group (2 mg/kg DVAS) and three oral dosage groups (5, 15, and 45 mg/kg DVAS). In addition, the activity of the components in plasma after intravenous administration of DVAS was evaluated by in vitro anti-butyrylcholinesterase (BChE) assays. RESULTS: A total of 23 metabolites were found in RLMs, plasma, urine, feces, and bile by UPLC-ESI-QTOF-MS. The metabolic pathway of DVAS in vivo and in vitro mainly involved hydroxylation, dehydrogenation, acetylation, methylation, glucuronidation, and O-sulphate conjugation, and the C-3 and C-9 sites were the main metabolic soft spots. All 23 metabolites were detected in the urine sample, and 13, 8, 22, and 6 metabolites were identified from rat feces, plasma, bile, and RLMs, respectively. The standard curves of DVAS and four metabolites in rat plasma showed good linearity in the concentration range of 0.82-524.00 ng/mL with acceptable selectivity, precision, accuracy, recovery, and stability. DVAS exhibited linear dose-proportional pharmacokinetics at doses of 5, 15, and 45 mg/kg after oral administration, and the average oral absolute bioavailability of DVAS was 47.46%. The in vitro anti-BChE assays implied that the inhibitive activities were mainly due to the different concentrations of prototype DVAS. CONCLUSIONS: DVAS can be rapidly absorbed and excreted by blood, and it is also extensively metabolized in vivo, and the anti-BChE activity in blood is mainly attributed to DVAS. These findings can lay a foundation for new drug development for DVAS.


Subject(s)
Alkaloids/pharmacokinetics , Cholinesterase Inhibitors/pharmacokinetics , Peganum/chemistry , Quinazolines/pharmacokinetics , Administration, Intravenous , Administration, Oral , Alkaloids/administration & dosage , Alkaloids/blood , Alkaloids/metabolism , Animals , Butyrylcholinesterase/metabolism , Cholinesterase Inhibitors/administration & dosage , Cholinesterase Inhibitors/blood , Cholinesterase Inhibitors/metabolism , Chromatography, High Pressure Liquid/methods , Enzyme Assays , Female , Male , Medicine, Traditional , Microsomes, Liver , Plant Components, Aerial/chemistry , Quinazolines/administration & dosage , Quinazolines/blood , Quinazolines/metabolism , Rats , Rats, Sprague-Dawley , Spectrometry, Mass, Electrospray Ionization/methods , Tandem Mass Spectrometry/methods
16.
Front Pharmacol ; 9: 346, 2018.
Article in English | MEDLINE | ID: mdl-29755345

ABSTRACT

The analogous ß-carboline alkaloids, harmaline (HAL) and harmine (HAR), possess a variety of biological properties, including acetylcholinesterase (AChE) inhibitory activity, antioxidant, anti-inflammatory, and many others, and have great potential for treating Alzheimer's disease (AD). However, studies have showed that the two compounds have similar structures and in vitro AChE inhibitory activities but with significant difference in bioavailability. The objective of this study was to comparatively investigate the effects of HAL and HAR in memory deficits of scopolamine-induced mice. In the present study, mice were pretreated with HAL (2, 5, and 10 mg/kg), HAR (10, 20, and 30 mg/kg) and donepezil (5 mg/kg) by intragastrically for 7 days, and were daily intraperitoneal injected with scopolamine (1 mg/kg) to induce memory deficits and then subjected to behavioral evaluation by Morris water maze. To further elucidate the underlying mechanisms of HAL and HAR in improving learning and memory, the levels of various biochemical factors and protein expressions related to cholinergic function, oxidative stress, and inflammation were examined. The results showed that HAL and HAR could effectively ameliorate memory deficits in scopolamine-induced mice. Both of them exhibited an enhancement in cholinergic function by inhibiting AChE and inducing choline acetyltransferase (ChAT) activities, and antioxidant defense via increasing the antioxidant enzymes activities of superoxide dismutase and glutathione peroxidase, and reducing maleic diadehyde production, and anti-inflammatory effects through suppressing myeloperoxidase, tumor necrosis factor α, and nitric oxide as well as modulation of critical neurotransmitters such as acetylcholine (ACh), choline (Ch), L-tryptophan (L-Trp), 5-hydroxytryptamine (5-HT), γ-aminobutyric acid (γ-GABA), and L-glutamic acid (L-Glu). Furthermore, the regulations of HAL on cholinergic function, inflammation, and neurotransmitters were more striking than those of HAR, and HAL manifested a comparable antioxidant capacity to HAR. Remarkably, the effective dosage of HAL (2 mg/kg) was far lower than that of HAR (20 mg/kg), which probably due to the evidently differences in the bioavailability and metabolic stability of the two analogs. Taken together, all these results revealed that HAL may be a promising candidate compound with better anti-amnesic effects and pharmacokinetic characteristics for the treatments of AD and related diseases.

17.
Biomaterials ; 75: 163-173, 2016 Jan.
Article in English | MEDLINE | ID: mdl-26513410

ABSTRACT

The ultra-short pulse microwave could excite to the strong thermoacoustic (TA) shock wave and deeply penetrate in the biological tissues. Based on this, we developed a novel deep-seated tumor therapy modality with mitochondria-targeting single wall carbon nanotubes (SWNTs) as microwave absorbing agents, which act efficiently to convert ultra-short microwave energy into TA shock wave and selectively destroy the targeted mitochondria, thereby inducing apoptosis in cancer cells. After the treatment of SWNTs (40 µg/mL) and ultra-short microwave (40 Hz, 1 min), 77.5% of cancer cells were killed and the vast majority were caused by apoptosis that initiates from mitochondrial damage. The orthotopic liver cancer mice were established as deep-seated tumor model to investigate the anti-tumor effect of mitochondria-targeting TA therapy. The results suggested that TA therapy could effectively inhibit the tumor growth without any observable side effects, while it was difficult to achieve with photothermal or photoacoustic therapy. These discoveries implied the potential application of TA therapy in deep-seated tumor models and should be further tested for development into a promising therapeutic modality for cancer treatment.


Subject(s)
Hyperthermia, Induced , Microwaves , Nanotubes, Carbon/chemistry , Neoplasms/therapy , Acoustics , Animals , Cell Line, Tumor , Female , Hyperthermia, Induced/adverse effects , Mice, Inbred BALB C , Mitochondria/metabolism , Nanotubes, Carbon/ultrastructure , Xenograft Model Antitumor Assays
18.
IEEE Trans Med Imaging ; 35(3): 839-44, 2016 Mar.
Article in English | MEDLINE | ID: mdl-26552081

ABSTRACT

We report the design of a real-time thermoacoustic (TA) scanner dedicated to imaging deep breast tumors and investigate its imaging performance. The TA imaging system is composed of an ultrashort microwave pulse generator and a ring transducer array with 384 elements. By vertically scanning the transducer array that encircles the breast phantom, we achieve real-time, 3D thermoacoustic imaging (TAI) with an imaging speed of 16.7 frames per second. The stability of the microwave energy and its distribution in the cling-skin acoustic coupling cup are measured. The results indicate that there is a nearly uniform electromagnetic field in each XY-imaging plane. Three plastic tubes filled with salt water are imaged dynamically to evaluate the real-time performance of our system, followed by 3D imaging of an excised breast tumor embedded in a breast phantom. Finally, to demonstrate the potential for clinical applications, the excised breast of a ewe embedded with an ex vivo human breast tumor is imaged clearly with a contrast of about 1:2.8. The high imaging speed, large field of view, and 3D imaging performance of our dedicated TAI system provide the potential for clinical routine breast screening.


Subject(s)
Breast Neoplasms/diagnostic imaging , Breast/diagnostic imaging , Imaging, Three-Dimensional/methods , Microwaves/therapeutic use , Thermography/methods , Animals , Female , Humans , Models, Biological , Phantoms, Imaging , Sheep , Signal Processing, Computer-Assisted
20.
Med Phys ; 41(11): 110701, 2014 Nov.
Article in English | MEDLINE | ID: mdl-25370614

ABSTRACT

PURPOSE: Previous studies demonstrated that thermoacoustic imaging (TAI) has great potential for breast tumor detection. However, large field of view (FOV) imaging remains a long-standing challenge for three-dimensional (3D) breast tumor localization. Here, the authors propose a practical TAI system for noninvasive 3D localization of breast tumors with large FOV through the use of ultrashort microwave pulse (USMP). METHODS: A USMP generator was employed for TAI. The energy density required for quality imaging and the corresponding microwave-to-acoustic conversion efficiency were compared with that of conventional TAI. The microwave energy distribution, imaging depth, resolution, and 3D imaging capabilities were then investigated. Finally, a breast phantom embedded with a laboratory-grown tumor was imaged to evaluate the FOV performance of the USMP TAI system, under a simulated clinical situation. RESULTS: A radiation energy density equivalent to just 1.6%-2.2% of that for conventional submicrosecond microwave TAI was sufficient to obtain a thermoacoustic signal with the required signal-to-noise ratio. This result clearly demonstrated a significantly higher microwave-to-acoustic conversion efficiency of USMP TAI compared to that of conventional TAI. The USMP TAI system achieved 61 mm imaging depth and 12 × 12 cm(2) microwave radiation area. The volumetric image of a copper target measured at depth of 4-6 cm matched well with the actual shape and the resolution reaches 230 µm. The TAI of the breast phantom was precisely localized to an accuracy of 0.1 cm over an 8 × 8 cm(2) FOV. CONCLUSIONS: The experimental results demonstrated that the USMP TAI system offered significant potential for noninvasive clinical detection and 3D localization of deep breast tumors, with low microwave radiation dose and high spatial resolution over a sufficiently large FOV.


Subject(s)
Breast Neoplasms/pathology , Imaging, Three-Dimensional/methods , Acoustics , Algorithms , Breast/pathology , Breast Neoplasms/diagnosis , Computer Simulation , Electromagnetic Radiation , Female , Humans , Image Processing, Computer-Assisted , Microwaves , Phantoms, Imaging , Reproducibility of Results , Signal-To-Noise Ratio
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