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1.
Plant Dis ; 2024 Jun 20.
Article in English | MEDLINE | ID: mdl-38902883

ABSTRACT

The Fusarium head blight (FHB) caused by Fusarium graminearum is a serious fungal disease that can dramatically impact wheat production. At present, control is mainly achieved by the use of chemical fungicides. Hexaconazole (IUPAC name: 2-(2,4-dichlorophenyl)-1-(1,2,4-triazol-1-yl)hexan-2-ol) is a widely used triazole fungicide, but the sensitivity of F. graminearum to this compound has yet to be established. The current study found that the EC50 values of 83 field isolates of F. graminearum ranged between 0.06 and 4.33 µg/mL, with an average EC50 of 0.78 µg/mL. Assessment of four hexaconazole-resistant laboratory mutants of F. graminearum revealed that their mycelial growth, and pathogenicity were reduced compared to their parental isolates, and that asexual reproduction was reduced by resistance to hexaconazole. Meanwhile, the mutants appeared to be more sensitive to abiotic stress associated with SDS, and H2O2, while their tolerance of high concentration of Congo red, and Na+ and K+ increased. Molecular analysis revealed numerous point mutations in the FgCYP51 target genes that resulted in amino acid substitutions, including L92P and N123S in FgCYP51A, as well as M331V, F62L, Q252R, A412V, and V488A in FgCYP51B, and S28L, S256A, V307A, D287G and R515I in FgCYP51C, three of which (S28L, S256A, and V307A) were conserved in all of the resistant mutants. Furthermore, the expression of the FgCYP51 genes in resistant strains was found to be significantly (p < 0.05) reduced compared to their sensitive parental isolates. Positive cross-resistance was found between hexaconazole and metconazole and flutriafol, as well as with the diarylamine fungicide fluazinam, but not with propiconazole, and the phenylpyrrole fungicide fludioxonil, or with tebuconazole, which actually exhibited negative cross-resistance. These results provide valuable insight into resistant mechanisms to triazole fungicides in F. graminearum, as well as the appropriate selection of fungicide combinations for the control of FHB to ensure optimal wheat production.

2.
Pharmacol Res ; 197: 106953, 2023 Nov.
Article in English | MEDLINE | ID: mdl-37804925

ABSTRACT

Cardiometabolic multimorbidity (CMM) is an increasingly significant global public health concern. It encompasses the coexistence of multiple cardiometabolic diseases, including hypertension, stroke, heart disease, atherosclerosis, and T2DM. A crucial component to the development of CMM is the disruption of endothelial homeostasis. Therefore, therapies targeting endothelial cells through multi-targeted and multi-pathway approaches hold promise for preventing and treatment of CMM. Curcumin, a widely used dietary supplement derived from the golden spice Carcuma longa, has demonstrated remarkable potential in treatment of CMM through its interaction with endothelial cells. Numerous studies have identified various molecular targets of curcumin (such as NF-κB/PI3K/AKT, MAPK/NF-κB/IL-1ß, HO-1, NOs, VEGF, ICAM-1 and ROS). These findings highlight the efficacy of curcumin as a therapeutic agent against CMM through the regulation of endothelial function. It is worth noting that there is a close relationship between the progression of CMM and endothelial damage, characterized by oxidative stress, inflammation, abnormal NO bioavailability and cell adhesion. This paper provides a comprehensive review of curcumin, including its availability, pharmacokinetics, pharmaceutics, and therapeutic application in treatment of CMM, as well as the challenges and future prospects for its clinical translation. In summary, curcumin shows promise as a potential treatment option for CMM, particularly due to its ability to target endothelial cells. It represents a novel and natural lead compound that may offer significant therapeutic benefits in the management of CMM.


Subject(s)
Atherosclerosis , Curcumin , Humans , Endothelial Cells , Curcumin/pharmacology , Curcumin/therapeutic use , Multimorbidity , NF-kappa B , Phosphatidylinositol 3-Kinases , Spices
3.
BMC Anesthesiol ; 23(1): 233, 2023 07 11.
Article in English | MEDLINE | ID: mdl-37434138

ABSTRACT

BACKGROUND: This investigation aimed to evaluate the impact of continuous pericapsular nerve group (PENG) block and continuous fascia iliac compartment block (FICB) on postoperative pain following total hip arthroplasty (THA). METHODS: This prospective, randomized, and controlled trial recruited a cohort of fifty-seven patients with unilateral femoral neck fractures from Xi'an Aerospace General Hospital in northwest China between July 2020 and November 2021. These patients were randomly assigned to two groups: the continuous PENG block group (PENG group, n = 29) and the continuous FICB group (FICB group, n = 28). Under ultrasound guidance, PENG block and FICB procedures were performed prior to spinal anesthesia, utilizing 20 ml of 0.25% ropivacaine for PENG block and 30 ml of 0.25% ropivacaine for FICB. Subsequently, a catheter was inserted. All study participants received a standardized postoperative multimodal analgesic regimen, including intravenous administration of 30 mg Ketorolac tromethamine every eight hours and patient-controlled neural analgesia (PCNA) after surgery. Numerical rating scale (NRS) scores at rest and during exercise were recorded at various time points: prior to block (T0), 30 min post-blockade (T1), and 6 h (T2), 12 h (T3), 24 h (T4), and 48 h (T5) postoperatively. Additional data collected encompassed postoperative quadriceps muscle strength, the time of initial ambulation after surgery, the number of effective PCNA activations, rescue analgesia requirements, and occurrences of adverse events (such as nausea and vomiting, hematoma, infection, catheter detachment, or displacement) within 48 h following surgery. RESULTS: In the PENG group, the resting NRS pain scores exhibited lower values at T1, T4, and T5 than those at T0. Furthermore, exercise NRS pain scores at T1-T5 were lower in the PENG group than in the FICB group. Similarly, during the same postoperative period, the PENG group demonstrated enhanced quadriceps strength on the affected side compared to the FICB group. Additionally, the PENG group displayed earlier postoperative ambulation and reduced occurrences of effective PCNA activations and rescue analgesia requirements compared to the FICB group. CONCLUSION: Continuous PENG block exhibited superior analgesic efficacy after THA compared to continuous FICB, promoting recovery of quadriceps strength on the affected side and facilitating early postoperative ambulation. TRIAL REGISTRATION: This clinical trial was registered in the China Clinical Trials Center ( http://www.chictr.org.cn ) on 20/07/2020, with the registration number ChiCTR2000034821.


Subject(s)
Arthroplasty, Replacement, Hip , Quadriceps Muscle , Humans , Pain Management , Arthroplasty, Replacement, Hip/adverse effects , Femoral Nerve , Proliferating Cell Nuclear Antigen , Prospective Studies , Ropivacaine , Fascia , Analgesia, Patient-Controlled , Pain
4.
Molecules ; 28(23)2023 Nov 28.
Article in English | MEDLINE | ID: mdl-38067553

ABSTRACT

Seahorse is a valuable marine-animal drug widely used in traditional Chinese medicine (TCM), and which was first documented in the "Ben Cao Jing Ji Zhu" during the Liang Dynasty. Hippocampus kelloggi (HK) is the most common seahorse species in the medicinal material market and is one of the genuine sources of medicinal seahorse documented in the Chinese pharmacopeia. It is mainly cultivated in the Shandong, Fujian, and Guangxi Provinces in China. However, pseudo-HK, represented by Hippocampus ingens (HI) due to its similar appearance and traits, is often found in the market, compromising the safety and efficacy of clinical use. Currently, there is a lack of reliable methods for identifying these species based on their chemical composition. In this study, we employed, for the first time, a strategy combining gas chromatography-mass spectrometry (GC-MS) fingerprints and chemical patterns in order to identify HK and HI; it is also the first metabolomic study to date of HI as to chemical components. The obtained results revealed remarkable similarities in the chemical fingerprints, while significant differences were also observed. By employing hierarchical cluster analysis (HCA) and principal component analysis (PCA), based on the relative contents of their characteristic peaks, all 34 samples were successfully differentiated according to their species of origin, with samples from the same species forming distinct clusters. Moreover, nonadecanoic acid and behenic acid were exclusively detected in HK samples, further distinguishing them from HI samples. Additionally, the relative contents of lauric acid, tetradecanoic acid, pentadecanoic acid, n-hexadecanoic acid, palmitoleic acid, margaric acid, oleic acid, fenozan acid, eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA) exhibited significant differences between HK and HI (p < 0.0001), as determined by an unpaired t-test. Orthogonal partial least squares discriminant analysis (OPLS-DA) identified seven components (DHA, EPA, n-hexadecanoic acid, tetradecanoic acid, palmitoleic acid, octadecanoic acid, and margaric acid) with high discriminatory value (VIP value > 1). Thus, nonadecanoic acid, behenic acid, and these seven compounds can be utilized as chemical markers for distinguishing HK from HI. In conclusion, our study successfully developed a combined strategy of GC-MS fingerprinting and chemical pattern recognition for the identification of HK and HI, and we also discovered chemical markers that can directly differentiate between the two species. This study can provide a foundation for the authentication of Hippocampus and holds significant importance for the conservation of wild seahorse resources.


Subject(s)
Smegmamorpha , Animals , Gas Chromatography-Mass Spectrometry , Myristic Acid , China , Cluster Analysis , Chromatography, High Pressure Liquid/methods , Principal Component Analysis
5.
Molecules ; 28(5)2023 Feb 27.
Article in English | MEDLINE | ID: mdl-36903461

ABSTRACT

The rhizome of Atractylodes lancea (RAL) is a well-known Chinese herbal medicine (CHM) that has been applied in clinical settings for thousands of years. In the past two decades, cultivated RAL has gradually replaced wild RAL and become mainstream in clinical practice. The quality of CHM is significantly influenced by its geographical origin. To date, limited studies have compared the composition of cultivated RAL from different geographical origins. As essential oil is the primary active component of RAL, a strategy combining gas chromatography-mass spectrometry (GC-MS) and chemical pattern recognition was first applied to compare the essential oil of RAL (RALO) from different regions in China. Total ion chromatography (TIC) revealed that RALO from different origins had a similar composition; however, the relative content of the main compounds varied significantly. In addition, 26 samples obtained from various regions were divided into three categories by hierarchical cluster analysis (HCA) and principal component analysis (PCA). Combined with the geographical location and chemical composition analysis, the producing regions of RAL were classified into three areas. The main compounds of RALO vary depending on the production areas. Furthermore, a one-way analysis of variance (ANOVA) revealed that there were significant differences in six compounds, including modephene, caryophyllene, γ-elemene, atractylon, hinesol, and atractylodin, between the three areas. Hinesol, atractylon, and ß-eudesmol were selected as the potential markers for distinguishing different areas by orthogonal partial least squares discriminant analysis (OPLS-DA). In conclusion, by combining GC-MS with chemical pattern recognition analysis, this research has identified the chemical variations across various producing areas and developed an effective method for geographic origin tracking of cultivated RAL based on essential oils.


Subject(s)
Atractylodes , Oils, Volatile , Oils, Volatile/chemistry , Gas Chromatography-Mass Spectrometry , Atractylodes/chemistry , Rhizome/chemistry
6.
Pharmacol Res ; 175: 106002, 2022 01.
Article in English | MEDLINE | ID: mdl-34826599

ABSTRACT

Obesity, is an increasingly global public health problem associated complications. However, the proven anti-obesity agents are inefficient with adverse side effects; hence attention is being paid to novel drugs from natural resources to manage obesity and obesity-related diseases. Nuciferine (NF) is a high-quality aporphine alkaloid present in lotus leaf. Unlike the chemical drugs, NF elicits anti-obesity, anti-dyslipidemia, anti-hyperglycemic, anti-hypouricemic, anti-inflammatory, and anti-tumor effects, and affinity to neural receptors, and protection against obesity-related diseases. The underlying mechanism of NF includes the regulation of targeted molecules and pathways related to metabolism, inflammation, and cancer and modulation of Ca2+ flux, gut microbiota, and ferroptosis. Besides, the clinical application, availability, pharmacokinetics, pharmaceutics, and security of NF have been established, highlighting the potential of developing NF as an anti-obesity agent. Therefore, this review provides a comprehensive summarization, which sheds light on future research in NF.


Subject(s)
Anti-Obesity Agents/therapeutic use , Aporphines/therapeutic use , Lotus , Obesity/drug therapy , Animals , Anti-Obesity Agents/pharmacology , Aporphines/pharmacology , Humans , Obesity/complications , Obesity/metabolism , Plant Leaves
7.
Crit Rev Food Sci Nutr ; : 1-31, 2022 Sep 08.
Article in English | MEDLINE | ID: mdl-36073729

ABSTRACT

Non-communicable diseases (NCDs) are a global epidemic with diverse pathogenesis. Among them, oxidative stress and inflammation are the most fundamental co-morbid features. Therefore, multi-targets and multi-pathways therapies with significant anti-oxidant and anti-inflammatory activities are potential effective measures for preventing and treating NCDs. The flavonol glycoside compound hyperoside (Hyp) is widely found in a variety of fruits, vegetables, beverages, and medicinal plants and has various health benefits, especially excellent anti-oxidant and anti-inflammatory properties targeting nuclear factor erythroid 2-related factor 2 (Nrf2) and nuclear factor-κB (NF-κB) signaling pathways. In this review, we summarize the pathogenesis associated with oxidative stress and inflammation in NCDs and the biological activity and therapeutic potential of Hyp. Our findings reveal that the anti-oxidant and anti-inflammatory activities regulated by Hyp are associated with numerous biological mechanisms, including positive regulation of mitochondrial function, apoptosis, autophagy, and higher-level biological damage activities. Hyp is thought to be beneficial against organ injuries, cancer, depression, diabetes, and osteoporosis, and is a potent anti-NCDs agent. Additionally, the sources, bioavailability, pharmacy, and safety of Hyp have been established, highlighting the potential to develop Hyp into dietary supplements and nutraceuticals.

8.
J Nanobiotechnology ; 20(1): 137, 2022 Mar 15.
Article in English | MEDLINE | ID: mdl-35292036

ABSTRACT

BACKGROUND: Most intravenously administered drug-loaded nanoparticles are taken up by liver Kupffer cells, and only a small portion can accumulate at the tumor, resulting in an unsatisfactory therapeutic efficacy and side effects for chemotherapeutic agents. Tumor-targeted drug delivery proves to be the best way to solve this problem; however, the complex synthesis, or surface modification process, together with the astonishing high cost make its clinical translation nearly impossible. METHODS: Referring to Ouyang's work and over-threshold dosing theory in general, blank PEGylated liposomes (PEG-Lipo) were prepared and used as tumor delivery enhancers to determine whether they could significantly enhance the tumor accumulation and in vivo antitumor efficacy of co-injected liposomal ACGs (PEG-ACGs-Lipo), a naturally resourced chemotherapeutic. Here, the phospholipid dose was used as an indicator of the number of liposomes particles with similar particle sizes, and the liposomes was labelled with DiR, a near-red fluorescent probe, to trace their in vivo biodistribution. Two mouse models, 4T1-bearing and U87-bearing, were employed for in vivo examination. RESULTS: PEG-Lipo and PEG-ACGs-Lipo had similar diameters. At a low-threshold dose (12 mg/kg equivalent phospholipids), PEG-Lipo was mainly distributed in the liver rather than in the tumor, with the relative tumor targeting index (RTTI) being ~ 0.38 at 72 h after administration. When over-threshold was administered (50 mg/kg or 80 mg/kg of equivalent phospholipids), a much higher and quicker drug accumulation in tumors and a much lower drug accumulation in the liver were observed, with the RTTI increasing to ~ 0.9. The in vivo antitumor study in 4T1 tumor-bearing mice showed that, compared to PEG-ACGs-Lipo alone (2.25 mg/kg phospholipids), the co-injection of a large dose of blank PEG-Lipo (50 mg/kg of phospholipids) significantly reduced the tumor volume of the mice by 22.6% (P < 0.05) and enhanced the RTTI from 0.41 to 1.34. The intravenous injection of a low drug loading content (LDLC) of liposomal ACGs (the same dose of ACGs at 50 mg/kg of equivalent phospholipids) achieved a similar tumor inhibition rate (TIR) to that of co-injection. In the U87 MG tumor-bearing mouse model, co-injection of the enhancer also significantly promoted the TIR (83.32% vs. 66.80%, P < 0.05) and survival time of PEG-ACGs-Lipo. CONCLUSION: An over-threshold dosing strategy proved to be a simple and feasible way to enhance the tumor delivery and antitumor efficacy of nanomedicines and was benefited to benefit their clinical result, especially for liposomal drugs.


Subject(s)
Antineoplastic Agents , Neoplasms , Animals , Antineoplastic Agents/pharmacology , Drug Delivery Systems , Liposomes/pharmacology , Mice , Neoplasms/drug therapy , Tissue Distribution
9.
Molecules ; 27(16)2022 08 21.
Article in English | MEDLINE | ID: mdl-36014563

ABSTRACT

Ligustici Rhizoma et Radix (LReR) is the dried rhizomes and roots of Ligusticum sinese Oliv. (LS) or Ligusticum jeholense Nakai et Kitag. (LJ). However, in the market, LS and LJ are frequently confused with each other. Since the volatile oils are both the main active components and quality control indicators of LReR, a strategy combining gas chromatography-mass spectrometry (GC-MS) and chemical pattern recognition (CPR) was used to compare the volatile components of LJ and LS. Total ion chromatography (TIC) revealed that phthalides (i.e., neocnidilide) and phenylpropanoids (i.e., myristicin) could be thought of as the most critical components in the volatile oils of LJ and LS, respectively. In addition, the chemical components of the volatile oils in LJ and LS were successfully distinguished by hierarchical cluster analysis (HCA) and principal component analysis (PCA). Moreover, two quality markers, including myristicin and neocnidilide, with a very high discriminative value for the classification of LJ and LS, were found by orthogonal partial least squares discriminant analysis (OPLS-DA). The relative contents of myristicin and neocnidilide were 10.86 ± 6.18% and 26.43 ± 19.63% for LJ, and 47.43 ± 12.66% and 2.87 ± 2.31% for LS. In conclusion, this research has developed an effective approach to discriminating LJ and LS based on volatile oils by combining GC-MS with chemical pattern recognition analysis.


Subject(s)
Drugs, Chinese Herbal , Ligusticum , Oils, Volatile , Drugs, Chinese Herbal/chemistry , Gas Chromatography-Mass Spectrometry/methods , Ligusticum/chemistry , Oils, Volatile/chemistry , Rhizome/chemistry
10.
Nanotechnology ; 32(30)2021 May 07.
Article in English | MEDLINE | ID: mdl-33862617

ABSTRACT

To improve the therapeutic efficacy of anticancer agents and extend their application, mussel-inspired chemical modifications have attracted considerable attention. Surface modification based on polydopamine (PDA) has been a facile and versatile method to immobilize biomolecules on substrates for targeted drug delivery. To better analyze pharmaceutical differences between PDA-based surface modification and traditional synthesis methods, we prepared two kinds of folate (FA)-targeted nanoparticles (NPs) loaded with paclitaxel (PTX). The resultant PTX-PDA-FA NPs and PTX-FA NPs represented PDA and synthesis strategies, respectively. PTX-PDA-FA NPs and PTX-FA NPs have been characterized. The particle size of PTX-PDA-FA NPs was smaller than that of PTX-FA NPs. The two kinds of NPs both exhibited long-rod morphology, good colloidal stability and sustained slow drug release. Cytotoxicityin vitrowas evaluated, and antitumor efficacy was investigated against 4T1 tumor-bearing mice. The tumor targeting therapeutic index of PTX-PDA-FA NPs and PTX-FA NPs showed equivalent superior specificity compared to nontargeted groups, which indicated that FA successfully attached to the surface of NPs by the PDA method and that the antitumor effect was equivalent to that of FA-modified NPs prepared by the chemical synthesis method. These results further indicated that PDA, as a simple and effective chemical surface modification platform, could be developed and applied in targeted delivery systems.


Subject(s)
Drug Delivery Systems , Indoles/chemistry , Nanoparticles/chemistry , Polymers/chemistry , Animals , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Antineoplastic Agents/therapeutic use , Cell Line, Tumor , Cell Survival/drug effects , Drug Liberation , Drug Stability , Folic Acid/chemistry , Mice , Paclitaxel/chemistry , Paclitaxel/pharmacology , Paclitaxel/therapeutic use , Particle Size , Surface Properties , Xenograft Model Antitumor Assays
11.
Bioorg Chem ; 107: 104523, 2021 02.
Article in English | MEDLINE | ID: mdl-33339668

ABSTRACT

Chuanxiongdiolides R4-R6 (1-3), three novel phthalide dimers featuring two classes of unreported monomeric units (ligustilide/senkyunolide A and ligustilide/neocnidilide) with an unprecedented linkage style (3a,7'/7a,7'a), were isolated from the aerial parts of Ligusticum chuanxiong, together with three pairs of enantiomeric phthalide dimers [(-)/(+)-4a/4b, 5a/5b, and 6a/6b]. The bioassays revealed that compounds 1, 3, 4, 5, and 6 showed significant vasodilation effects, and the mechanism may be attributed to Cav1.2 activation blockade. Based on the established compounds library, the structure activity relationship of the phthalides was proposed. Our findings afford possible leads for developing new vasodilator against cardiovascular and cerebrovascular diseases such as hypertension and ischemic stroke.


Subject(s)
Benzofurans/pharmacology , Heterocyclic Compounds, Bridged-Ring/pharmacology , Ligusticum/chemistry , Vasodilator Agents/pharmacology , Animals , Benzofurans/chemistry , Benzofurans/isolation & purification , Benzofurans/metabolism , Calcium Channel Blockers/chemistry , Calcium Channel Blockers/isolation & purification , Calcium Channel Blockers/metabolism , Calcium Channel Blockers/pharmacology , Calcium Channels, L-Type/metabolism , HEK293 Cells , Heterocyclic Compounds, Bridged-Ring/chemical synthesis , Heterocyclic Compounds, Bridged-Ring/isolation & purification , Heterocyclic Compounds, Bridged-Ring/metabolism , Humans , Molecular Docking Simulation , Molecular Structure , Plant Components, Aerial/chemistry , Protein Binding , Rabbits , Rats, Sprague-Dawley , Stereoisomerism , Structure-Activity Relationship , Vasodilator Agents/chemistry , Vasodilator Agents/isolation & purification , Vasodilator Agents/metabolism
12.
Mol Pharm ; 17(4): 1205-1214, 2020 04 06.
Article in English | MEDLINE | ID: mdl-32073273

ABSTRACT

The composition of amphiphilic nanocarriers can affect the antitumor efficacy of drug-loaded nanoparticles and should be researched systematically. In this paper, to study the influence of hydrophobic chains, an amphiphilic copolymer (PEG45PCL17) and hydrophilic PEG (PEG45) were utilized as nanocarriers to prepare docetaxel-loaded nanoparticles (DTX/PEG45PCL17 nanoparticles and DTX/PEG45 nanoparticles) through an antisolvent precipitation method. The two DTX nanoparticles presented a similar drug loading content of approximately 60% and a sheet-like morphology. During the preparation procedure, the drug loading content affected the morphology of DTX nanoparticles, and the nanocarrier composition influenced the particle size. Compared with DTX/PEG45 nanoparticles, DTX/PEG45PCL17 nanoparticles showed a smaller mean diameter and better in vitro and in vivo antitumor activity. The cytotoxicity of DTX/PEG45PCL17 nanoparticles against 4T1 cells was 1.31 µg mL-1, 3.4-fold lower than that of DTX/PEG45 nanoparticles. More importantly, DTX/PEG45PCL17 nanoparticles showed significantly higher antitumor activity in vivo, with an inhibition rate over 80%, 1.5-fold higher than that of DTX/PEG45 nanoparticles. Based on these results, antitumor activity appears to be significantly affected by the particle size, which was determined by the composition of the nanocarrier. In summary, to improve antitumor efficacy, the amphiphilic structure should be considered and optimized in the design of nanocarriers.


Subject(s)
Antineoplastic Agents/chemistry , Docetaxel/chemistry , Drug Carriers/chemistry , Nanoparticles/chemistry , Animals , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Docetaxel/pharmacology , Female , Hydrophobic and Hydrophilic Interactions , Mice , Mice, Inbred BALB C , Particle Size , Polyethylene Glycols/chemistry , Polymers/chemistry
13.
J Nanobiotechnology ; 18(1): 4, 2020 Jan 06.
Article in English | MEDLINE | ID: mdl-31907045

ABSTRACT

Disulfiram (DSF) has been considered as "Repurposing drug" in cancer therapy in recent years based on its good antitumor efficacy. DSF is traditionally used as an oral drug in the treatment of alcoholism. To overcome its rapid degradation and instability, DSF nanosuspensions (DSF/SPC-NSps) were prepared using soybean lecithin (SPC) as a stabilizer of high drug-loaded content (44.36 ± 1.09%). Comprehensive characterization of the nanosuspensions was performed, and cell cytotoxicity, in vivo antitumor efficacy and biodistribution were studied. DSF/SPC-NSps, having a spherical appearance with particle size of 155 nm, could remain very stable in different physiological media, and sustained release. The in vitro MTT assay indicated that the cytotoxicity of DSF/SPC-NSps was enhanced remarkably compared to free DSF against the 4T1 cell line. The IC50 value decreased by 11-fold (1.23 vs. 13.93 µg/mL, p < 0.01). DSF/SPC-NSps groups administered via intravenous injections exhibited better antitumor efficacy compared to the commercial paclitaxel injection (PTX injection) and had a dose-dependent effect in vivo. Notably, DSF/SPC-NSps exhibited similar antitumor activity following oral administration as PTX administration via injection into a vein. These results suggest that the prepared nanosuspensions can be used as a stable delivery vehicle for disulfiram, which has potential application in breast cancer chemotherapy.


Subject(s)
Antineoplastic Agents/pharmacology , Disulfiram/pharmacology , Glycine max/chemistry , Lecithins/chemistry , Nanoparticles/chemistry , Animals , Calorimetry, Differential Scanning , Cell Line, Tumor , Disulfiram/chemistry , Drug Liberation , Drug Stability , Female , Mice, Inbred BALB C , Nanoparticles/ultrastructure , Particle Size , Static Electricity , Suspensions , Tissue Distribution/drug effects , Treatment Outcome , X-Ray Diffraction
14.
J Sep Sci ; 43(15): 2989-2995, 2020 Aug.
Article in English | MEDLINE | ID: mdl-32419363

ABSTRACT

This study aimed to identify Pheretima aspergillum (Guang-Pheretima) and its adulterants using the cytochrome c oxidase subunit I based deoxyribonucleic acid barcoding technology, and further to evaluate their quality using an optimized high-performance liquid chromatography method. For deoxyribonucleic acid barcoding identification, the Kimura-2-Parameter model was used to analyze genetic distance, and phylogenetic neighbor-joining tree was constructed for species identification of 20 labeled Guang-Pheretima samples. A high-performance liquid chromatography method was developed for the simultaneous determination of seven nucleoside components for quality evaluation. Compared with the GenBank database, 10 samples were identified as real Guang-Pheretima (P. aspergillum), and the others as the adulterants-Metaphire magna. The maximum intraspecific genetic distances of c oxidase subunit I sequence for P. aspergillum were smaller than the minimum interspecific genetic distances between P. aspergillum and M. magna. Ten P. aspergillum and 10 M. magna samples were clearly clustered in the neighbor-joining tree. The contents of seven nucleosides components in P. aspergillum were significantly higher than that in its adulterant-M. magna. The incidence of adulterants for Guang-Pheretima was high (up to 50%) with an alarming quality. This study provided a powerful idea for the quality evaluation of other highly valuable plant- or animal-derived products for safety concerns to avoid misidentification.


Subject(s)
Cyclooxygenase 1/metabolism , DNA/chemistry , Nucleosides/analysis , Oligochaeta/chemistry , Animals , Chromatography, High Pressure Liquid , DNA/metabolism , Nucleosides/genetics , Oligochaeta/genetics , Quality Control
15.
Pharmacol Res ; 142: 176-191, 2019 04.
Article in English | MEDLINE | ID: mdl-30818043

ABSTRACT

As an important component of complementary and alternative medicines, traditional Chinese medicines (TCM) are gaining more and more attentions around the world because of the powerful therapeutic effects and less side effects. However, there are still some doubts about TCM because of the questionable TCM theories and unclear biological active compounds. In recent years, gut microbiota has emerged as an important frontier to understand the development and progress of diseases. Together with this trend, an increasing number of studies have indicated that drug molecules can interact with gut microbiota after oral administration. In this context, more and more studies pertaining to TCM have paid attention to gut microbiota and have yield rich information for understanding TCM. After oral administration, TCM can interact with gut microbiota: (1) TCM can modulate the composition of gut microbiota; (2) TCM can modulate the metabolism of gut microbiota; (3) gut microbiota can transform TCM compounds. During the interactions, two types of metabolites can be produced: gut microbiota metabolites (of food and host origin) and gut microbiota transformed TCM compounds. In this review, we summarized the interactions between TCM and gut microbiota, and the pharmacological effects and features of metabolites produced during interactions between TCM and gut microbiota. Then, focusing on gut microbiota and metabolites, we summarized the aspects in which gut microbiota has facilitated our understanding of TCM. At the end of this review, the outlooks for further research of TCM and gut microbiota were also discussed.


Subject(s)
Drugs, Chinese Herbal/pharmacology , Gastrointestinal Microbiome/drug effects , Medicine, Chinese Traditional , Animals , Humans
16.
BMC Complement Altern Med ; 19(1): 126, 2019 Jun 11.
Article in English | MEDLINE | ID: mdl-31185967

ABSTRACT

BACKGROUND: Gut microbiota plays a crucial role in the treatment of gastrointestinal (GI) diseases such as chemotherapy-induced diarrhea (CID). Shenzhu Capsule (SZC) is a Chinese herbal formula, which is composed of Renshen (rhizomes of Panax ginseng C. A. Mey.) and Baizhu (rhizomes of Atractylodes macrocephala Koidz.). Many Chinese traditional anti-diarrheal formulae that contain Renshen and Baizhu are capable of effectively alleviating CID. However, the efficacy in vivo and potential mechanism of SZC (the form of compatibility of Renshen and Baizhu) in the treatment of CID had not been elucidated. Here, this study aimed to investigate whether SZC exhibited the anti-diarrheal activity, and whether gut microbiota was involved in the therapeutic effect of SZC on CID. METHODS: High performance liquid chromatography (HPLC), gas chromatography-mass spectrometer (GC-MS) and infrared spectroscopy (IR) analyses were used to characterize the extracted components in SZC. The mice were orally administrated with SZC in a preventive mode on the first 2 days of this experiment, and then intraperitoneally injected with 5-FU (40 mg/kg/d) for 6 days. SZC treatment lasted until the 3rd day after the end of 5-FU chemotherapy. We investigated the effects of SZC on body weights, diarrhea, thymus/spleen indexes, colonic tissues, and gut microbiota. Colonic histology was examined by hematoxylin-eosin (HE) staining. 16S rDNA Amplicon Sequencing was used to analyze the gut microbial structure from fecal samples. RESULTS: SZC significantly increased the body weights and thymus/spleen indexes, alleviated diarrhea, and reversed histopathological changes of colons. In addition, gut microbiota analysis revealed that the overall structure of gut microbiota in CID mice was disturbed, but reversed to the normal state after SZC treatment. At genus level, SZC significantly inhibited the growth of some potential pathogens associated with diarrhea, such as Clostridiumm, Bacteroides, Parabacteroides, Alloprevotella, Acinetobacter and Pseudomonas. CONCLUSIONS: In our study, these data illustrated that SZC inhibited the growth of many potential pathogens during the alleviation of CID. Gut microbial modulation was associated with the anti-diarrheal activity of SZC.


Subject(s)
Atractylodes/chemistry , Diarrhea/prevention & control , Drugs, Chinese Herbal/therapeutic use , Gastrointestinal Microbiome/drug effects , Panax/chemistry , Animals , Antimetabolites, Antineoplastic/adverse effects , Diarrhea/chemically induced , Drug Evaluation, Preclinical , Drugs, Chinese Herbal/chemistry , Drugs, Chinese Herbal/pharmacology , Female , Fluorouracil/adverse effects , Male , Mice , Phytotherapy , Random Allocation , Spleen/drug effects , Thymus Gland/drug effects
17.
Molecules ; 24(9)2019 Apr 28.
Article in English | MEDLINE | ID: mdl-31035329

ABSTRACT

Fructus Amomi (FA) is usually regarded as the dried ripe fruit of Amomum villosum Lour. (FAL) or Amomum villosum Lour. var. xanthioides T. L. Wu et Senjen (FALX.). However, FAL, which always has a much higher price because of its better quality, is often confused with FALX. in the market. As volatile oil is the main constituent of FA, a strategy combining gas chromatography-mass spectrometry (GC-MS) and chemometric approaches was applied to compare the chemical composition of FAL and FALX. The results showed that the oil yield of FAL was significantly higher than that of FALX. Total ion chromatography (TIC) showed that cis-nerolidol existed only in FALX. Bornyl acetate and camphor can be considered the most important volatile components in FAL and FALX., respectively. Moreover, hierarchical cluster analysis (HCA) and principal component analysis (PCA) successfully distinguished the chemical constituents of the volatile oils in FAL and FALX. Additionally, bornyl acetate, α-cadinol, linalool, ß-myrcene, camphor, d-limonene, terpinolene and borneol were selected as the potential markers for discriminating FAL and FALX. by partial least squares discrimination analysis (PLS-DA). In conclusion, this present study has developed a scientific approach to separate FAL and FALX. based on volatile oils, by GC-MS combined with chemometric techniques.


Subject(s)
Amomum/chemistry , Fruit/chemistry , Gas Chromatography-Mass Spectrometry , Metabolomics , Oils, Volatile/chemistry , Cluster Analysis , Metabolomics/methods
18.
Luminescence ; 32(6): 908-912, 2017 Sep.
Article in English | MEDLINE | ID: mdl-28071869

ABSTRACT

CaSnO3 :Bi3+ blue-emitting phosphor was synthesized using a high-temperature solid-state reaction method in air. The crystal structures and luminescence properties were investigated. A broad emission band peaking at ~448 nm upon excitation at 262 and 308 nm was observed in the range 330-680 nm at room temperature due to 3 P1  â†’ 1 S0 transition of the Bi3+ ion. The chromaticity coordinate was (0.1786, 0.1665). The optimal Bi3+ ion concentration was ~0.6 mol% in CaSnO3 :Bi3+ phosphor. The emission spectrum of CaSnO3 :Bi3+ phosphor showed a blue-shift with increasing temperature from 50 to 300 K due to the influence of temperature on the electron transition of the Bi3+ ion. The emission intensity of CaSnO3 :Bi3+ phosphor may be increased ~1.45 times by co-doping Li+ ions as a charge compensator and fluxing agent. The luminescence mechanism is explained by a configurational coordinate diagram of Bi3+ ion in CaSnO3 :Bi3+ phosphor.


Subject(s)
Bismuth/chemistry , Lithium/chemistry , Luminescent Agents/chemical synthesis , Color , Luminescence , Luminescent Agents/chemistry , Luminescent Measurements
19.
Luminescence ; 30(7): 962-6, 2015 Nov.
Article in English | MEDLINE | ID: mdl-25645573

ABSTRACT

A series of Sr(1-x-y)CayMoO4:xSm(3+) (0 ≤ x ≤ 7 mol% and 0 ≤ y < 1) phosphors was synthesized by a conventional solid-state reaction method in air, and their structural and spectroscopic properties were investigated. The optimal doping concentration of Sm(3+) in SrMoO4:Sm(3+) phosphor is 5 mol%. Under excitation with 275 nm, in Sr(1-x-y)CayMoO4:xSm(3+) (0 ≤ x ≤ 7 mol% and 0 ≤ y < 1) phosphors, the emission band of the host was found to overlap with the excitation bands peaking at ~ 500 nm of Sm(3+) ion, and the energy transfer from MoO4 (2-) group to Sm(3+) ion can also be observed. The International Commission on Illumination (CIE) chromaticity coordinates of Sr(0.95-y)CayMoO4:0.05Sm(3+) phosphors with excitation 275 nm varied systematically from an orange (0.4961, 0.3761) (y = 0) to a white color (0.33, 0.3442) (y = 0.95) with increasing calcium oxide (CaO) concentration. However, Sr(0.95-y)CayMoO4:0.05Sm(3+) phosphors with excitation at 404 nm only showed red emission and the energy transfer between MoO4(2-) group to Sm(3+) ion was not observed. The complex mechanisms of luminescence and energy transfer are discussed by energy level diagrams of MoO4(2-) group and Sm(3+) ion.


Subject(s)
Calcium/chemistry , Luminescence , Molybdenum/chemistry , Oxygen/chemistry , Samarium/chemistry , Strontium/chemistry , Luminescent Measurements , Photochemical Processes , Powder Diffraction
20.
Drug Deliv ; 31(1): 2324716, 2024 Dec.
Article in English | MEDLINE | ID: mdl-38555735

ABSTRACT

Annonaceous acetogenins (ACGs) have potent anti-tumor activity, and the problems of their low solubility, hemolysis, and in vivo delivery have been solved by encapsulation into nanoparticles. However, the high toxicity still limits their application in clinic. In this paper, the co-delivery strategy was tried to enhance the in vivo anti-tumor efficacy and reduce the toxic effects of ACGs. Ginsenoside Rh2, a naturally derived biologically active compound, which was reported to have synergistic effect with paclitaxel, was selected to co-deliver with ACGs. And due to its similarity with cholesterol in chemical structure, the co-loading liposomes, (ACGs + Rh2)-Lipo, were successfully constructed using Rh2 instead of cholesterol as the membrane material. The obtained (ACGs + Rh2)-Lipo and ACGs-Lipo had similar mean particle size (about 80 nm), similar encapsulation efficiency (EE, about 97%) and good stability. The MTS assay indicated that (ACGs + Rh2)-Lipo had stronger toxicity in vitro. In the in vivo study, in contrast to ACGs-Lipo, (ACGs + Rh2)-Lipo demonstrated an improved tumor targetability (3.3-fold in relative tumor targeting index) and significantly enhanced the antitumor efficacy (tumor inhibition rate, 72.9 ± 5.4% vs. 60.5 ± 5.4%, p < .05). The body weight change, liver index, and spleen index of tumor-bearing mice showed that Rh2 can attenuate the side effects of ACGs themselves. In conclusion, (ACGs + Rh2)-Lipo not only alleviated the toxicity of ACGs to the organism, but also enhanced their anti-tumor activity, which is expected to break through their bottleneck.


Subject(s)
Acetogenins , Ginsenosides , Glioma , Mice , Animals , Acetogenins/pharmacology , Acetogenins/chemistry , Liposomes , Glioma/drug therapy , Cholesterol
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