Phytochemical Analysis最新文献

Background: Alzheimer's disease (AD) is one of the most common forms of dementia among the elderly in the world. With the increase of human life expectancy, its incidence is also increasing year by year. Tacrine (TAC) is the first acetylcholine inhibitor approved for the treatment of AD. Although TAC has obvious anti-AD activity, it was eventually delisted due to acute liver injury caused by its strong hepatotoxicity. Rosmarinic acid (RA) has shown good activity in both neuroprotection and hepatoprotection.

Purpose and study design: In this study, the combination of RA and TAC was explored, and a high dose of d-galactose was used to build an AD mouse model, which was given at the same time for 4 weeks in order to alleviate TAC hepatotoxicity and enhance the intervention of AD in mice through RA. In particular, we pay attention to the key role of Aβ and microglia in the pathogenesis of AD, so we evaluate the ability of RA combined with TAC in alleviating chronic neuroinflammation induced by Aβ plaque in the brain of AD mice and enhancing the ability of microglia to clear Aβ plaque.

Results: The results show that the combination of RA and TAC has the best intervention effect on AD compared with the single use of the two drugs, and it is basically positively correlated with RA dose. RA + TAC significantly improved body weight, organ index, and behavioral state of AD mice. Further analysis showed that RA + TAC enhanced the antioxidant level of hippocampus and serum of AD mice, alleviated the pathological damage of hippocampus, significantly improved cholinergic system, reduced the expression levels of AB plaque and neurotoxic Aβ1-41 and Aβ1-42 in the brain, and significantly increased the level of neuroprotective protein trigger receptor expressed on myeloid cells 2 (TREM2), which mediated the phagocytosis of microglia. More importantly, the combination therapy of RA and TAC decreased the expression of M1 microglia marker (ionized calcium-binding adapter molecule 1 [Iba-1]), increased the expression of M2 microglia marker Arg-1, and promoted the release of anti-inflammatory compounds. In addition, RA + TAC also inhibited the mRNA expression of TLR4 and NF-κB related to neuroinflammation. In the aspect of liver function, RA reduced cell death mediated by Caspase-3 by regulating the expression of bcl-2/bax, alleviated TAC-induced liver injury in mice, and made the serum indexes of ALT, AST, ALP, TBIL, and γ-GT reflecting liver function closer to the normal range.

Conclusion: The combination of RA and TAC shows the potential to reduce the hepatotoxicity of TAC and is expected to enhance its therapeutic effect on AD.

Introduction: Lavender (Lavandula angustifolia) is valued in the food and pharmaceutical industries for its unique aroma, owing to oxygenated monoterpenoids such as linalool, linalyl acetate, lavandulyl acetate, 1,8-cineole, and terpinene-4-ol, which contribute to the quality of lavender essential oil (LEO). It is rich in flavonoids and phenolics like rosmarinic acid. LEO and phenolic yields depend on agronomic attributes, processing techniques, and extraction methods.

Objectives: This review aims to provide a comprehensive overview of the newly developed technologies and their optimization parameters to maximize oil yield, aroma quality, and phenolic content.

Methods: Related sufficient evidence has been collected from prominent scientific databases, including PubMed, Web of Science, ScienceDirect, and Google Scholar. Data concerning the phytochemistry, biological impacts, agricultural aspects, and processing approaches of Lavender were collected and assessed.

Results: The diverse aspects of LEO production, including agricultural factors, climatic conditions, and processing techniques, are reviewed to identify the optimal parameters. Furthermore, technologies including GC/MS, HPLC/MS, and IR highlight the relevance of metabolomics in lavender quality control and analysis. In addition, lavender's anti-inflammatory, antioxidant, and enzyme-inhibiting properties are highlighted.

Conclusions: Metabolomic analyses offer comprehensive insights into the biochemical composition of lavender, allowing researchers to identify metabolites linked to favorable agricultural traits, disease resistance, optimized oil extraction, superior quality attributes, and potential nutraceutical value; these data-driven findings guide targeted breeding, cultivation strategies, and product development. Lavender (L. angustifolia) is widely recognized for its aroma and health-promoting compounds, including monoterpenoids and phenolics like rosmarinic acid. Essential oil yield and quality depend on cultivation methods and extraction techniques. This review evaluates recent technological advances to optimize oil production, aroma, and phenolic content, using metabolomics techniques to comprehensively analyze lavender constituents. This comprehensive profiling reveals lavender's defensive mechanisms by linking its constituents to considerable health benefits. The findings help improve lavender quality and use in health and well-being.

Introduction: Postmenopausal osteoporosis, a skeletal disorder induced by estrogen deficiency, is commonly addressed in clinical practice through the use of Cuscutae semen and its compound formulations, owing to their significant therapeutic efficacy.

Objective: This study sought to systematically identify bioactive compounds present in Cuscutae semen that interact with estrogen receptor β (ESR2) using Affinity Ultrafiltration combined with Ultra-Performance Liquid Chromatography-Quadrupole-Orbitrap Mass Spectrometry (UPLC-QE-Orbitrap-MS) to find possible therapy options for PMOP.

Methods: The Cuscutae semen extract was fractionated using a C18 column to obtain fractions based on distinct polarity. Preliminary evaluation of anti-osteoporotic activity was conducted in MC3T3-E1 cells by assessing osteoprotegerin (OPG) expression. Affinity Ultrafiltration integrated with UPLC-QE-Orbitrap-MS was utilized to screen for ligands binding to ESR2, followed by molecular docking to validate the interaction mechanisms. The osteogenic effects of the identified compounds were further confirmed through CCK-8 proliferation assays, OPG quantification, and alkaline phosphatase (ALP) activity analysis.

Results: The fraction of Cuscutae semen extract eluted with 100% methanol exhibited significant anti-osteoporotic activity. Three flavonoids-Astragalin, Isorhamnetin, and Quercitrin-that interact with ESR2 were successfully identified. In vitro validation demonstrated the efficacy of these compounds.

Conclusion: This study presents a comprehensive strategy that integrates Affinity Ultrafiltration, UPLC-QE-Orbitrap-MS, and bioactivity validation to efficiently identify ESR2-targeted postmenopausal osteoporosis compounds in Cuscutae Semen. The findings offer both theoretical and empirical foundations for the development of innovative therapeutics for postmenopausal osteoporosis.

Background: Uncariae Ramulus cum Uncis (URCU) is a widely used traditional Chinese medicine (TCM) for treating neurodegenerative disorders. The Chinese Pharmacopeia recognizes five Uncaria species as authorized botanical sources of URCU; however, there is currently no established quality control method for individual species. Furthermore, significant variations in the chemical profiles among these species have been reported.

Objective: Chemical analysis methods were established to evaluate the five species in terms of chemical profile and resource availability, as to determine which species should be preferred as the official source(s).

Method: Ten batches of URCU sample were collected from various regions of China for each of the five species of URCU. Among five species, only UR can be obtained from herbal medicine market, whereas the other four species were sourced from the wild. All samples identities were confirmed by herbarium specimen authentication, morphological identification, and microscopic identification. Twelve alkaloids were identified in the five species, and a UPLC-DAD assay method targeting six marker alkaloids was developed and validated.

Results: Only UR and UM demonstrated the most stable chemical profiles and agreement with published literature. UR mainly contains corynoxeine, isocorynoxeine, rhynchophylline, and isorhynchophylline, whereas corynoxine, corynoxine B, rhynchophylline, and isorhynchophylline dominate in UM.

Conclusion: This study comprehensively evaluated the chemical variations among the five officially recognized URCU species using a UPLC-DAD method. It brings important implications for quality control and standardization of URCU. Considering chemical stability and supply availability, UR is recommended as the sole botanical source for URCU.

Introduction: The roots of Lindera aggregata (Sims) Kosterm named "Wuyao" in Chinese, showed significant antidiabetic bioactivity detected by the insulin resistance HepG2 cells. However, efficient identification of the new antidiabetic compounds has been lacking.

Objective: To develop a guided discovery strategy for new antidiabetic compounds from L. aggregate with activity labeled molecular networking (ALMN).

Methodology: The constructed ALMN could clearly visualize the activities and the structure nodes, which can facilitate the annotation of the active candidates.

Results: Eight new sesquiterpenoids (1-8) were obtained from the roots of Lindera aggregate according to the ALMN workflow showed antidiabetic activity. As for the new compounds, 1 was characteristic of 15-nor-lindenane type, which was reported for the first time, 2 and 3 of aconitane type, 4 of germarane type, 5-8 of eudesmane type sesquiterpenes.

Conclusion: As results indicated, all the eight compounds showed significant antidiabetic effects, which were consistent with the obtained activity annotations by ALMN. The mechanism of the antidiabetic activity for 1-8 were further delved via Akt/GSK3β signal pathway, which can be observed as potential agents against the insulin resistance for the insulin resistance Type II diabetes.

Introduction: Eleutherococcus senticosus, a traditional Chinese medicine, has shown potential in treating glioblastoma (GBM). However, its main active components and mechanisms of action remain unclear.

Objective: This study aimed to evaluate the inhibitory effects of E. senticosus on GBM cell proliferation and migration using in vitro cellular experiments.

Methods: Transcriptome sequencing and metabolome analysis were performed on GBM cells treated with E. senticosus. Network pharmacology and correlation analysis identified the main active components and their targets, which were further verified using molecular biology experiments. Electrophoretic mobility shift assays and molecular docking analyses were used to analyze the binding ability and mechanisms of action of transcription factors and promoters.

Results: E. senticosus significantly inhibited GBM cell proliferation and migration. Treatment with E. senticosus caused significant changes in ferroptosis-related genes and metabolites in GBM cells, significantly reducing the levels of glutathione, an antagonist of ferroptosis, and its synthetic substrates. GPX4, FTH1, and TFR1 were identified as core targets of ferroptosis induction in E. senticosus-induced GBM cells. Quercetin had similar biological effects on GBM cells as E. senticosus and is its main active component. E. senticosus and quercetin changed the binding ability of transcription factors SIX1 and MYBL2 to the promoters of GPX4, FTH1, and TFR1.

Conclusion: E. senticosus changed the binding ability of SIX1, MYBL2, and promoters of target genes via quercetin, which led to changes in the expression of GPX4, FTH1, and TFR1, finally resulting in ferroptosis induction in GBM cells.

Background: Cannabis sativa L. is an annual herbaceous plant in the genus Cannabis of the family Cannabaceae. Hempseed, a traditional Chinese medicine, is the dried and ripe decorticated fruit of C. sativa L. It has a long history of medicinal use and belongs to the category of "both medicine and food." The earliest record of hempseed as food can be found in "The Book of Rites" (Zhou Li), while its medicinal use was first documented in Shennong's Classic of Materia Medica (Shennong Bencao Jing). Hempseed contains rich chemical components, such as fatty acids, cannabinoids, lignin amides, alkaloids, flavonoids, and proteins, among which fatty acids are the most abundant. Hempseed has the effects of moistening the intestines and relieving dryness, invigorating the middle-jiao, and replenishing qi. It is often used for blood deficiency and body fluid deficiency, intestinal dryness, and constipation, and is an important drug for the treatment of functional constipation. Modern medicinal chemistry and pharmacological studies have shown that hempseed semen not only has a significant laxative effect but also possesses pharmacological effects such as anti-inflammation, anti-oxidation, anti-tumor, analgesia, lipid-lowering, and others.

Objectives: At present, the quality standards for hemp kernels have not yet established content control for single or whole components. This not only cannot fully guarantee the quality and safety of medicinal materials but also restricts the improvement of quality standards. We summarize the knowledge in this area with the aim of providing new ideas for the scientific application of cannabis and the integration of modern research and traditional medicine.

Methods: Relevant literature was retrieved from major scientific databases, including PubMed, Web of Science, ScienceDirect, and Google Scholar. The system collected and analyzed information related to the phytochemistry, pharmacological effects, comprehensive utilization, and quality control of hemp seeds.

Results: This article provides a review of the research on traditional Chinese medicine Ma Ren from the aspects of herbal research, phytochemistry, and pharmacology, and emphasizes the latest progress in the comprehensive utilization and quality control of hemp seeds.

Conclusion: Hemp seeds contain various bioactive compounds with broad pharmacological potential. They have shown potential in disease management and prevention and are increasingly being applied in the development of functional health products. At the same time, in the future, we need to strengthen interdisciplinary mechanism analysis, accelerate clinical validation, optimize intelligent manufacturing technology, build a standard system for the entire industry chain, and promote the leapfrog development of hemp seeds from functional raw materials to precision and healthy products.

Neurological disorders impose a significant burden on the healthcare systems. The latest published data by WHO indicated that stroke was the second leading cause of death globally in 2020, with Alzheimer's disease (AD) and other dementias in the seventh position. The treatment of neurological disorders is challenging because of the complex nature of the disease, as well as limited accessibility to this target organ due to several biological barriers. There is a wide range of treatment options for neurological disorders. Small drug molecules, antibodies, and stem cells have been employed for the treatment of neurodegenerative diseases such as AD, but currently, there is no effective treatment for AD. As conventional drugs have not been successful in achieving therapeutic outcomes, natural products such as curcumin, stemming from traditional medicines, have been tested for the treatment of neurodegenerative diseases such as AD. However, this compound has not shown significant therapeutic effects for the treatment of brain diseases, mainly due to rapid clearance from the body. Therefore, phytochemical nanoparticles have been developed. In this review article, the rationale has been provided for the use of nanoparticles for the treatment of neurodegenerative diseases with emphasis on phytochemical nanoparticles.

Quercetin is one of the prestigious bioactive flavonoids found in many fruits, vegetables, and grains, which has attracted considerable attention due to its various pharmacological effects and therapeutic potential. Many researchers isolate and extract it by employing various analytical methods because of its manifold pharmacological profile. This paper provides a comprehensive review of quercetin's biological impacts, emphasizing its anti-inflammatory, antioxidant, anticancer, and antihypertensive effects. There are many formulations available in which quercetin is the main ingredient. Its clinical use is frequently limited by inadequate bioavailability and stability. To tackle these challenges, several drug formulations and delivery methods, including nanoparticles and liposome complexes, have been created to improve absorption and effectiveness. The author also discussed that various analytical methods, like high-performance liquid chromatography, are increasingly being employed to characterize quercetin's molecular properties, bioactivity, and interactions with biological targets and sources from which it is obtained. Additionally, the review gives insight into the synthesis of quercetin, with a description of clinical and preclinical trials as well as patents.

Introduction: Murraya koenigii contains bioactive compounds with antidiabetic and hypolipidemic activities. Considering widespread availability and traditional use of M. koenigii throughout South Asia.

Objectives: The present study was designed to perform qualitative and quantitative analysis of phytochemicals present in curry leaves.

Material and methods: Quantification method was validated according to International Council of Harmonization (ICH) guidelines and was used to analyze seasonal and geographical variability of phytoconstituents in leaf samples collected from different geographical locations across India.

Results: The isolated four carbazole alkaloids, namely, mahanimbine, girinimbine, koenimbine, and koenigicine, from methanolic extract of curry leaves, were quantitatively determined in the leaves of M. koenigii using reverse phase-high performance liquid chromatography equipped with photodiode array detector (RP-HPLC-PDA).

Conclusions: Our study revealed that mahanimbine, koenimbine, and koenigicine content was maximum in sample collected in months of April, June, and October 2020, respectively. The samples procured from Northern Indian regions showed maximum content of carbazole alkaloids. The in vitro biological assays revealed anti-obesogenic potential of carbazole alkaloids in 3T3-L1 adipocytes.