INDUSTRIAL CROPS AND PRODUCTS
·
2023
·
IF 5.9
Zehao Wang,Ru Zhao,Hongfei Gao,Yang Yang,Xinyu Yang,Huiyan Gu,Lei Yang,Xiaonan Zhang,Tingting Liu
One of the most significant sources of commercial camphor oil is the essential oil of Cinnamomum burmannii (Nees et T. Nees) Blume leaves, which has been manufactured using a variety of distillation techniques, including hydrodistillation and microwave-assisted hydrodistillation. In this study, we employed solvent-free microwave extraction (SFME) to recover hydrosol and essential oil from fresh C. burmannii leaves that had undergone screw extrusion. An optimum yield of 12.35 ± 0.62 mL/kg DW of essential oil was obtained by optimizing the major SFME contributing parameters using a face-centered central composite design (FCCCD). By using SFME, the influence of microwave irradiation power on the yield and quality of the essential oil of fresh leaves of C. burmannii was examined. With the aid of first- and second-order kinetic equations, SFME was contrasted with hydrodistillation and dry distillation. A total of 32 components were detected in the essential oil, and 22 components were detected in the hydrosol obtained by SFME under the optimized conditions. The main components of the essential oil were 1,8-cineole (21.67%), borneol (17.37%) and α -terpineol (7.45%), in descending order, and the main components of the hydrosol were trans -2-hydroxycinnamic acid (21.45%), borneol (22.07%), 1,8-cineole (13.65%) and α -terpineol (11.93%). 1,8-Cineole and borneol were the two components with the highest influence on hierarchical clustering, according to principal component analysis and heatmap analysis. Moreover, box-whisker plots were used to determine and compare the inhibitory activities of the essential oil and its three primary constituents against pancreatic lipase . The outcomes demonstrated that 1,8-cineole played a critical role in the essential oil's ability to inhibit pancreatic lipase, and they also demonstrated a positive correlation between the concentration and the amount of inhibition activity.
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Asian Journal of Pharmaceutical Sciences
·
2023
·
IF 10.2
Xin Shen,Zhixiang Cui,Yidan Wei,Yingnan Huo,Duo Yu,Xin Zhang,Shirui Mao
The number of people with Alzheimer's disease (AD) is increasing annually, with the nidus mainly concentrated in the cortex and hippocampus. Despite of numerous efforts, effective treatment of AD is still facing great challenges due to the blood brain barrier (BBB) and limited drug distribution in the AD nidus sites. Thus, in this study, using vinpocetine (VIN) as a model drug, the objective is to explore the feasibility of tackling the above bottleneck via intranasal drug delivery in combination with a brain guider, borneol (BOR), using nanoemulsion (NE) as the carrier. First of all, the NE were prepared and characterized. In vivo behavior of the NE after intranasal administration was investigated. Influence of BOR dose, BOR administration route on drug brain targeting behavior was evaluated, and the influence of BOR addition on drug brain subregion distribution was probed. It was demonstrated that all the NE had comparable size and similar retention behavior after intranasal delivery. Compared to intravenous injection, improved brain targeting effect was observed by intranasal route, and drug targeting index (DTI) of the VIN NE group was 154.1%, with the nose-to-brain direct transport percentage (DTP) 35.1%. Especially, remarkably enhanced brain distribution was achieved after BOR addition in the NE, with the extent depending on BOR dose. VIN brain concentration was the highest in the VIN-1-BOR-NE group at BOR dose of 1 mg/kg, with the DTI reaching 596.1% and the DTP increased to 83.1%. BOR could exert better nose to brain delivery when administrated together with the drug via intranasal route. Notably, BOR can remarkably enhance drug distribution in both hippocampus and cortex, the nidus areas of AD. In conclusion, in combination with intranasal delivery and the intrinsic brain guiding effect of BOR, drug distribution not only in the brain but also in the cortex and hippocampus can be enhanced significantly, providing the perquisite for improved therapeutic efficacy of AD.
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Frontiers in Pharmacology
·
2023
·
IF 5.6
Fanchang Wu,Mingjun Huang,Xue Zuo,Ruiye Xie,Jinman Liu,Junyu Ke,Weirong Li,Qi Wang,Yong Liang
Alzheimer’s disease (AD) poses a significant threat to the global elderly population. Traditional Chinese medicine (TCM) has been widely utilized in the treatment of AD. Osthole, a bioactive ingredient classified as an “emperor” in many TCM formulas, has been demonstrated to effectively alleviate AD symptoms. However, its low bioavailability in the brain has limited its clinical application. This study aimed to increase the intracerebral bioavailability of osthole by using borneol as a “courier,” based on the classical “Emperor–Minister–Assistant–Courier” model, and to investigate the enhanced pharmacological performance of osthole on AD. Results indicated that a suitable in situ thermosensitive gel matrix for intranasal administration mixed with osthole and borneol consists of P407 at 20%, P188 at 7%, and PEG300 at 6%. The concentration of osthole in the cerebrospinal fluid increased almost tenfold after intranasal administration of osthole/borneol compared to oral administration. Mechanisms showed that borneol as a “courier” opened up intercellular space and loosened the tight junctions of the nasal mucosa by suppressing ZO-1 and occludin expression, thereby expediting the nose-to-brain route and guiding osthole as “emperor” to its target in the brain. Osthole assisted by borneol demonstrated significantly improved efficiency in suppressing cleaved caspase-3 expression, increasing the Bcl-2/Bax ratio, improving T-SOD and catalase expression, reducing malondialdehyde levels, inhibiting neuron apoptosis, and decreasing Aβ levels by inhibiting BACE1 expression to alleviate cognitive impairment in APP/PS1 mice compared to osthole alone. Overall, our study demonstrated that the intracerebral bioavailability of osthole profoundly improved with intranasal administration of osthole/borneol and provided a wider application of TCM for AD treatment with higher intracerebral bioavailability.
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Heritage Science
·
2022
·Vol. 10
·期 1
·1-12
·
IF 2.843
Liu Zhen,Liu Kun
Chinese ink has very special significance for presentation of artistic effects and preservation of works of art; however, wasted nonrenewable resources, potential toxicity, and complex and inefficient production technologies have limited the development of inks for traditional Chinese culture. Herein, environmentally friendly, practical and antibacterial Chinese ink was prepared by facile heating-stirring of gelatin and the natural polysaccharide chitosan. The internal composition, viscosity, morphology, particle size and antibacterial properties of the ink were characterized by Fourier transform-infrared spectroscopy, X-ray photoelectron spectroscopy, scanning electron microscopy and bacteriostatic zone tests. The results showed that commercial ink (CM) spread easily on Xuan paper and led to imperfect artwork, while the chitosan and gelatin ink (CG) showed good adhesion and stability on Xuan paper. Based on this study, we believe that the good performance of CG ink should be attributed to restrictions arising from its internal chitosan and gelatin network, which restrict diffusion. Finally, the author used CG ink to display traditional Chinese calligraphy and landscape painting and believes that it has significant application prospects and will be used in large-scale production.
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CIENCIA RURAL
·
2022
·
IF 0.901
Liu Zhenyi,Wang Jing,Yin Meijuan,Liu Mengsheng,Gao Weijuan
The Eucalyptus plant releases allelopathic chemicals into the environment mostly through the essential oils volatilized from the leaves. This study discussed the composition of the leaf oils of few seven-year-old varieties like Eucalyptus pellita (E. pel), Eucalyptus camaldulensis (E. cama), Eucalyptus grandis (E. gra), Eucalyptus dunni (E. dun), Eucalyptus saligna (E. sal), and E. grandis × E. urophylla (E. gra×E. uro) and three-year-old E. grandis × E. urophylla (E. gra × E. uro (three)). It determined the allelopathic mechanism and the types of chemical components playing the leading role. Essential oil was obtained by hydrodistillation and analyzed by the Gas Chromatography-Mass Spectrometry (GC-MS) method. In order to determine the effect of allelopathy, seed germination experiments were carried out at different concentrations (10-100 mL/L) of the E. Gra × E. uro leaf oil (EO) and the major components. The wheat seeds germinated by adding 1,8-cineole were used to determine the activity of α-amylase. Moreover, the mRNA expression of α-amylase in seeds was studied. The major chemical class in the essential oil was oxygenated monoterpene; 1,8-cineole (20.2-67.5%) displayed the highest content. Other substances that were high in content and ubiquitous included α-pinene (0.3-21.8%), α-terpineol (0.44-19.24%), and borneol (0.81-3.05%). The four chemical constituents and EO influenced the germination and growth of the three plants. Among them, 1,8-cineole exhibited the strongest inhibitory effect. The α-amylase activity of the 1,8-cineole-treated wheat seeds had decreased significantly. Molecular evidence suggested that 1,8-cineole decreased the α-amylase gene (AMY) expression.
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MOLECULES
·
2022
·Vol. 27
·期 3
·1115
·
IF 4.927
Huijuan Li,Xinghui Song,Huiru Li,Lifei Zhu,Shengbo Cao,Jifeng Liu
Two undescribed ether derivatives of sesquiterpenes, 1-ethoxycaryolane-1, 9β-diol (1) and 2-ethoxyclovane-2β, 9α-diol (3), and one new monoterpene glycoside, p-menthane-1α,2α,8-triol-4-O-β-D-glucoside (5), were obtained, together with eight known compounds from the stems and leaves ofI. simonsii. Their structures were elucidated by spectroscopic methods. Compounds1–11were evaluated for their potency againstStaphylococcus aureusand clinical methicillin-resistantS. aureus(MRSA). Among them, compound3was weakly active againstS. aureus(MIC = 128 μg/mL), and compounds6and7exhibited good antibacterial activity againstS. aureusand MRSA (MICs = 2–8 µg/mL). A primary mechanism study revealed that compounds6and7could kill bacteria by destroying bacterial cell membranes. Moreover, compounds6and7were not susceptible to drug resistance development.Keywords:Illicium simonsii;sesquiterpene;monoterpene;antibacterial;MRSA
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TREES-STRUCTURE AND FUNCTION
·
2021
·Vol. 36
·期 2
·711-721
·
IF 2.529
Xu Chenyi,Ma Yuandan,Tian Zhengfeng,Luo Qingyun,Zheng Tiefeng,Wang Bin,Zuo Zhaojiang
Key message The four chemotypes of adult C. camphora released different monoterpenes which protected these plants against high temperature by lowering ROS levels and maintaining photosynthetic abilities. Abstract High temperature seriously impacts plant growth and development, and terpenes are believed to improve plant thermotolerance through indoor experiments using seedlings. To uncover the actual protection effects of monoterpenes on outdoor adult plants, we investigated the monoterpene emissions, reactive oxygen species (ROS) metabolism, and photosynthetic abilities in four chemotypes of adult Cinnamomum camphora that were blocked monoterpene synthesis by fosmidomycin (Fos) under high temperature in summer (the mean highest temperature at about 38.2 °C). Eucalyptol (EuL), linalool (Lnl), borneol (BeL), and camphor (CmR) chemotypes of C. camphora released an abundance of monoterpenes, with eucalyptol, linalool, endo-borneol, and camphor as the typical monoterpene, respectively. When the four chemotypes of C. camphora were treated with Fos, their monoterpene emission was inhibited remarkably, with disappearance of some monoterpenes. In that case, the content of O 2 − , H 2 O 2 , and thiobarbituric acid reactive substance (TBARS) in the four chemotypes of C. camphora significantly increased although antioxidant enzyme activities remarkably increased, and the photosynthetic abilities significantly decreased by declining the quantum production and electron transport in photosystem II and increasing the dissipation of absorbed light energy. Among the four chemotypes, monoterpenes might play the maximum roles in CmR lowering ROS levels and in EuL maintaining photosynthesis. It can be speculated that monoterpenes can protect adult C. camphora against high temperature by lowering ROS levels and maintaining photosynthetic abilities.
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INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2023
·
IF 5.8
Chuanhui Teng,Wei Lv,Yuqin Chen,Linfeng Liu,Jiaqing Yin,Shengnan Li,Zhiyi Min,Qi Zhang,Weichong He,Kunfang Ma,Xinrui Li,Xiang Cao,Hongliang Xin
Since ischemic stroke occurs by a combination of multiple mechanisms, therapies that modulate multiple mechanisms are required for its treatment. The combination of edaravone (EDA) and borneol can significantly ameliorate the symptoms of neurological deficits in cerebral ischemia–reperfusion model in rats. In this study, the solubility of borneol and edaravone was improved by hydroxypropyl-β-cyclodextrin and PEG 400 . Furthermore, a nasal temperature-sensitive hydrogel containing both edaravone and borneol inclusion complex (EDA-BP TSG S ) was developed to overcome the obstacles of ischemic stroke treatment including the obstruction of the blood–brain barrier (BBB) and the unavailability and untimely of intravenous injection. The effectiveness of the thermosensitive hydrogel was investigated in transient middle cerebral artery occlusion/reperfusion model rats (MCAO/R). The results showed that EDA-BP TSG S could significantly alleviate the symptoms of neurological deficits and decrease the cerebral infarct area and the degree of brain damage. In summary, nasal EDA-BP TSG S is a secure and effective brain-targeting formulation that may provide a viable option for the clinical prophylaxis and treatment of ischemic stroke.
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DRUG DELIVERY
·
2019
·
IF 3.829
Yujia Zhang,Nan Zhang,Hui Song,He Li,Jin Wen,Xiaochuan Tan,Wensheng Zheng
Gout is a kind of joint disease characterized by the accumulation of monosodium urate (MSU) crystals in the joint and its surrounding tissue, causing persistent hyperuricemia. Colchicine is the first choice of treatment for acute gout attacks. Due to strong toxicity of colchicines oral tablets, there are high fluctuations of blood drug concentration and serious irritation of gastrointestinal tract, and hence a transdermal preparation can help to slow down the blood drug concentration, reduce the frequency of drug taking, and improve the patients' compliance of the drug. The ethosome is a lipid carrier with high concentration of ethanol and has been proved to promote the penetration of drugs into the skin. Borneol (BO) is an excellent penetration enhancer in Chinese medicine, which can promote the entry of drugs into the skin. This paper prepared the borneol-physically-modified colchicine ethosome (COL-bpES) and used the prepared borneol-dioleoyl phosphoethanloamine (BO-DOPE) to prepare borneol-chemically-modified colchicine ethosome (COL-bcES). Compared to the free colchicine aqueous solution (free COL) and normal colchicine ethosome (COL-ES), the borneol-modified colchicine ethosome (COL-bES) demonstrated better drug penetration effect, while the particle size of the COL-bcES was lower than that of the COL-bpES. Toxicity, in vitro diffusion, pharmacokinetics and pharmacodynamics are superior to those of COL-bpES, providing a better delivery system for the treatment of small molecule inflammatory drugs.
研究领域:
药剂学
·
生物医学工程
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Acta Pharmaceutica Sinica B
·
2023
·
IF 14.5
Zinan Zhang,Wenbin Cao,Huanchun Xing,Shuai Guo,Lijuan Huang,Lin Wang,Xin Sui,Kui Lu,Yuan Luo,Yongan Wang,Jun Yang
In the treatment of central nervous system disease, the blood–brain barrier (BBB) is a major obstruction to drug delivery that must be overcome. In this study, we propose a brain-targeted delivery strategy based on selective opening of the BBB. This strategy allows some simple bare nanoparticles to enter the brain when mixed with special opening material; however, the BBB still maintains the ability to completely block molecules from passing through. Based on the screening of BBB opening and matrix delivery materials, we determined that phospholipase A2-catalyzed 1-palmitoyl-2-oleoyl- sn -glycero-3-phosphoserine liposomes can efficiently carry drugs into the brain immediately. At an effective dose, this delivery system is safe, especially with its effect on the BBB being reversible. This mix & act delivery system has a simple structure and rapid preparation, making it a strong potential candidate for drug delivery across the BBB.
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SENSORS AND ACTUATORS B-CHEMICAL
·
2023
·
IF 8.4
Shishi Shao,Jiaqiang Zhao,Wei Wang,Hanbing Nie,Yan Jie Li,Xuepeng Zhang,Cheng Zhi Huang,Peng Fei Gao
Host-guest doping room-temperature phosphorescence (RTP) materials have showed excellent potential for ultra-sensitive detection due to its bright luminescence in presence of trace guests. However, the inherent signal fluctuation of solid-state sensors restricts their widespread applications. Herein we constructed a simple internal standard method to overcome the signal fluctuation problem in RTP spectral analysis. Ultralong organic RTP can be obtained by using 1,4-dichlorobenzene (DCB) as a host and trace gaseous NL as a guest through the host-guest doping strategy. In this study, a dual-emission ratiometric phosphorescent probe pyrene (Py)/pentachloropyridine (PCP)-DCB was constructed by using the Py/PCP system fabricated via melt-casting as the reference afterglow and using the DCB as the stimuli-responsive unit of gaseous NL. This probe can be used for visual identification and content detection of NL in commercial mothballs. The ratio of phosphorescence intensity (I485/I595) was linearly related to the mass of added NL (mNL) within the range of 0.05–1.45 mg in this ratiometric RTP platform, and had a low detection limit of 0.012 mg. Furthermore, the NL content of five commercially available mothballs with different NL content was detected by this Py/PCP-DCB platform, and it had good performance compared to the gas chromatography (GC) analysis results.
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ENVIRONMENTAL RESEARCH
·
2023
·
IF 8.3
Tianyu Huang,Meng Lai,Zhenwei Lin,Ruiqi Luo,Xuezheng Xiang,Haozhe Xu,Ning Pan,Zhaojiang Zuo
Cyanobacterial blooms cause serious environmental issues , and plant secondary metabolites are considered as new algaecide for controlling them. Cinnamomum camphora produces a wide spectrum of terpenoids and has 4 main chemotypes, including linalool, camphor , eucalyptol and borneol chemotype. To develop the new cyanobacterial algaecide by using suitable chemotype of Cinnamomum camphora and the main terpenoids, we analyzed the terpenoid composition in the 4 chemotype extracts, evaluated the algicidal effects of the extracts and their typical monoterpenoids on Microcystis aeruginosa , and investigated the algicidal mechanism of the stronger algicidal agents. Among the 4 chemotypes, eucalyptol and borneol chemotype extracts exhibited stronger algicidal effects. In the 4 chemotype extracts, monoterpenoids were the main compounds, of which linalool, camphor, eucalyptol and borneol were the typical components. Among the 4 typical monoterpenoids, eucalyptol and borneol showed stronger algicidal effects, which killed 78.8% and 100% M. aeruginosa cells, respectively, at 1.2 mM after 48 h. In 1.2 mM eucalyptol and borneol treatments, the reactive oxygen species levels markedly increased, and the caspase-3-like activity also raised. With prolonging the treatment time, M. aeruginosa cells gradually shrank and wrinkled, and the cell TUNEL fluorescence intensity and DNA degradation gradually enhanced, indicating that the lethal mechanism is causing apoptosis-like programmed cell death (PCD). Therefore, eucalyptol and borneol chemotype extracts and their typical monoterpenoids have the potential for developing as algaecides to control cyanobacteria through triggering apoptosis-like PCD.
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