Active Ingredient Content Research Articles

Effect of fermentation on the constituents in the branches and leaves of Taxus media and non-small cell lung cancer

IntroductionNon-small cell lung cancer (NSCLC) is a prominent lung cancer disease worldwide. Currently, commonly used methods, such as surgery and radiotherapy, have significant side effects. Traditional Chinese medicine (TCM) has become a research hotspot because of its safe and effective characteristics. The branches and leaves of Taxus media are abundant in antitumor active compounds, and there has been no research conducted as yet regarding its anti–lung cancer molecular mechanism.ObjectiveThe aim of this study is to investigate the antitumor activity of two samples before and after fermentation of T. media, and to research the molecular mechanism of its inhibitory effect on NSCLC.MethodsThe chemical composition of pre-fermentation T. media (TM) and post-fermentation T. media qu (TMQ) were investigated using UHPLC-Q-Qrbitrap HRMS and high-performance liquid chromatography (HPLC). The anti-lung cancer activities of TM and TMQ were compared using an A549-induced tumor mouse model. An enzyme-linked immunosorbent assay (ELISA), hematoxylin and eosin (H&E) staining, immunohistochemistry, and immunofluorescence were used to determine the of TMQ mechanism of action.ResultsThe results indicated that TM and TMQ contained 83 compounds, consisting primarily of flavonoids, organic acids, and taxanes. Both taxanes and flavonoids in TMQ were higher than that in TM. Both TM and TMQ effectively inhibited the tumor growth in non-small cell lung cancer (NSCLC), and the inhibition rate was greater in TMQ (57.24%) than in TM (49.62%). TMQ administration downregulated the tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and the glutathione (GSH) level and upregulated interferon-γ (IFN-γ), reactive oxygen species (ROS), and malondialdehyde (MDA) levels in the serum of tumor mice. TMQ treatment also increased the protein expression of Bax, Caspase-3, and Beclin-1 in tumor tissues. In contrast, the bcl-2, PI3K, Ki67, ULK1, and mTOR protein levels were suppressed by TMQ. Protein assay analyses reemphasized the superior antitumor effect of TMQ over TM. These cumulative findings demonstrated that the mechanism of action of TMQ was closely related to the activation of transcriptional misregulation in the cancer pathway that inhibited the cholinergic synaptic, AMPK, and PI3K/Akt/mTOR signaling pathways.ConclusionThis study demonstrated that fermentation increased the active ingredient contents and antitumor effects of T. media. In addition, post-fermentation TMQ was superior to TM as a herbal medicine for NSCLC treatment.

Wuzi-Yanzong-Wan Prevents the Defect of Cell-Cell Junctions between Sertoli-Germ Cells by Up-Regulating the Expression of TAp73.

The TAp73 gene is an anti-cancer gene that also affects the junction between Sertoli and germ cells. Inhibition of this gene causes infertility in male mice. Our previous research proved that Wuzi-Yanzong-Wan (WZYZW) can protect spermatogenesis and maturation by preventing TAp73 inhibition. This study aimed to investigate the effect of drug-containing serum of WZYZW on the defect of cell-cell junctions in the Sertoli-germ cells co-culture system in vitro. LC-HRMS was used to analyze the content of active ingredients in WZYZWmedicated serum. Then, primary extraction and co-culture of germ cells and Sertoli cells were carried out. Co-cultured cells were added with PFT-α to induce the TAp73 inhibition model, with WZYZW-medicated serum at 2.5%, 5%, and 10% treated in parallel. Sloughing of germ cells from Sertoli cells was calculated. Transmission electron microscopy (TEM), Immunofluorescence, qRT-PCR, and western blot methods were employed. The drug-containing serum of WZYZW contained schisandrin, hyperoside, geniposidic acid, ellagic acid, and quercetin. Using TEM assay, we observed restoration of the desmosomelike (Des), tight junctions (TJ), and basal ectoplasmic specialization (ES) structure following WZYZW treatment. WZYZW caused inhibition of peptidase and protease inhibitors (tissue inhibitor of metalloproteinase-1 (TIMP1), Serpina3n) by immunofluorescence analysis. Western blot and qRT-PCR analysis revealed that WZYZW was able to ameliorate the expressions of peptidase and protease inhibitors and cell adhesion factors, such as TAp73, TIMP1, Serpina3n, Desmocollin-3, N-cadherin, and Nectin-2. WZYZW-medicated serum could prevent the defect of cell-cell junctions between Sertoli-germ cells co-culture system in vitro by up-regulating the expression of TAp73.

Near Infrared Spectroscopy (NIRS) Model Based on Transfer Learning

This study compares three transfer learning strategies for adapting convolutional neural network (CNN) models in near-infrared spectroscopy to new instruments. Strategy 1 freezes pre-trained weights except for the output layer; Strategy 2 fine-tunes all weights with new data; Strategy 3 adds new fully connected layers to the pre-trained model. Using tablet spectra to predict active pharmaceutical ingredient content, results show that fine-tuning all network weights (Strategy 2) yields the best performance. The study also finds that moderate training sample sizes balance model accuracy and resource expenditure. Transfer learning is effective for near-infrared model transfer.

Shading Impairs Mycorrhizal Benefits on Plant Growth, Leaf Gas Exchange, and Active Ingredients in Polygonum cuspidatum

Polygonum cuspidatum, an important medicinal plant, often experiences shading from surrounding vegetation during its growth phase, raising questions about the impact of such conditions on the functionality of arbuscular mycorrhizal fungi. This study investigated the effects of an arbuscular mycorrhizal fungus (Funneliformis mosseae) on the growth, leaf gas exchange, and concentrations of active ingredient concentrations in leaves and roots of P. cuspidatum under shading (with a 72% shading rate) conditions. A nine-week shading intervention significantly suppressed root colonization by F. mosseae and the formation of soil mycorrhizal mycelium. Shading significantly inhibited the above-ground growth performance, biomass production, leaf photosynthetic rate, transpiration rate, stomatal conductance, and intercellular CO2 concentration, while F. mosseae significantly increased these variables in the absence of shading. Plant height, leaf biomass, stem biomass, leaf photosynthetic rate, transpiration rate, and stomatal conductance were all decreased by F. mosseae when the plants were shaded. The shading treatment also significantly diminished the concentrations of active components measured in both leaves and roots. Under no-shading conditions, F. mosseae significantly boosted the concentrations of polydatin, resveratrol, aloe-emodin, emodin, chrysophanol, and physcion in roots, as well as the concentrations of polydatin and chrysophanol in leaves. Conversely, in the presence of shading, F. mosseae distinctly reduced these active ingredient levels in roots, followed by an increase in leaf polydatin and chrysophanol concentrations. In summary, shading substantially impaired the mycorrhizal benefits on plant growth, leaf gas exchange, and root active ingredients in P. cuspidatum, highlighting the importance of sufficient light to maximize mycorrhizal contributions.

Application of terahertz time-domain spectroscopy and chemometrics-based crested porcupine algorithm in identification of different medicinal parts of Angelica sinensis

ObjectiveAngelica sinensis is one of the commonly used Chinese herbal medicine in traditional Chinese medicine clinic, exhibits different pharmacological characteristics due to variations in the content of active ingredients in its head, body, and tail. Therefore, research on the identification methods of different medicinal parts of Angelica sinensis is of great practical significance. Terahertz Time-Domain Spectroscopy (THz-TDS) technology is widely used in the field of nondestructive testing because of its unique electromagnetic wave characteristics. This study explores the feasibility of combining THz-TDS with chemometrics to identify different medicinal parts of Angelica sinensis. MethodsBy comparing the spectral response characteristics of different parts of Angelica sinensis to various optical parameters, the absorption coefficient spectrum in the 0.6–3.0 THz range was selected, and three types of feature extraction algorithms, namely, joint Competitive Adaptive Reweighted Sampling (CARS), Uninformative Variable Elimination (UVE), and Successive Projections Algorithm (SPA), were used to establish the classification models of Extreme Learning Machine (ELM), Random Forest (RF), and Support Vector Machine (SVM) in turn, and optimize the models by using the crown porcupine algorithm (Crested Porcupine Optimizer (CPO) to optimize the model. ResultsThe research results indicate that the CPO optimizer significantly improved the classification accuracy of the models, with the accuracy of the ELM, RF, and SVM models increasing by 4.36%, 1.11%, and 12.22%, respectively. The SPA-CPO-SVM model exhibited the best overall performance, achieving accuracies of 96.11% and 97.96% on the prediction and training sets, respectively, while the number of input features was only 5% of the total feature set. ConclusionThe results show that the fully joint feature extraction strategy and optimization algorithm can play a powerful synergistic effect in model construction, confirming the feasibility of THz-TDS technology to correctly identify different medicinal parts of Angelica sinensis, and providing an important reference for the application of terahertz technology in the identification of Chinese herbal medicines.

Tissue-specific chemical expression and quantitative analysis of bioactive components of Moutan Cortex by laser-microdissection combined with UPLC-Q-Orbitrap-MS technique

Moutan Cortex, is the root bark of Paeonia suffruticosa Andrews, which is classified into three specifications according to whether or not it is peeled and cored: Liandanpi, Guadanpi and whole root. In this study, the cork layer, cortex, phloem and xylem of P. suffruticosa fresh root were precisely separated by laser microdissection technique. UPLC-Q-Orbitrap-MS and UPLC-QQQ-MS techniques were used to analyse the differences in the chemical composition of different tissue parts of P. suffruticosa fresh root and Liandanpi, and to determine the optimal processing method of P. suffruticosa root. As a result, a total of 90 compounds were characterised, among which the cork layer had more types and higher contents of chemical constituents, and the xylem had fewer types and lower contents of chemical constituents. The proportion of xylem is larger, while the type and content of active ingredients is smaller. Therefore, the processing method of removing the wood core and retaining the cork bark can be used in the processing of Moutan Cortex. In this study, laser microdissection and ultra performance liquid chromatography-mass spectrometry were used to provide a theoretical basis for optimising the processing method of Moutan Cortex to enhance its pharmacological effects.

Transport, pollution, and health risk of heavy metals in “soil-medicinal and edible plant-human” system: A case study of farmland around the Beiya mining area in Yunnan, China

Heavy metals (HMs) pose a significant threat to soil quality, plant growth, and human health. However, the impacts (transport, pollution, and health risk) of HMs in medicinal and edible plants with rich value growing in high background soil for a long time remain unclear. So the effects of HMs on the “soil-medicinal and edible plant-human” system were comprehensively studied. Houttuynia cordata Thunb. (HCT) and growing soil were collected from the farmland around Beiya mining area located in Three Parallel Rivers of Yunnan Protected Areas, China. The transport, pollution, and health risks of HMs in the system were investigated by determining the content of active ingredients, HMs, and physicochemical properties in HCT and soil. The results of comprehensive analysis using various measurement and analysis methods showed that Zn, Cu, Mn, and Co in soil could affect the contents of available nutrients (available P (AP), available K (AK), and organic matter (OM)), while AP, OM, pH, Co, and Fe in soil were closely related to the formation of HCT quality. Cr and Fe had the strongest transport capacity in stems and leaves of HCT, respectively. Furthermore, it is worth noting that Cr, Pb, and Cu had caused serious pollution to HCT in the area. Pb and Cu are tolerable levels for human health and may pose a carcinogenic risk. Our study demonstrates that HCT is expected to be a marker of heavy metal pollution in the area and provides a scientific basis for making effective regulations on HMs control and scientific planting.

A Novel Protection and Repair Skincare Regimen Shows Efficacy for Improving Environmental Skin Aging.

Skin aging is accelerated by environmental exposures including solar radiation and pollutants. Thus, protecting skin from environmental exposure and repairing ensuing damage is essential for keeping skin healthy and appearing youthful. To evaluate the clinical benefits of a novel skincare regimen designed to provide comprehensive environmental protection in the daytime and repair environmentally damaged skin at night. Thirty participants, including males and females, with mild-to-moderate extrinsic aging, were enrolled in a 12-week single-site study. Participants used the regimen (The Essential Six, RATIONALE, Victoria, Australia) comprised of 3 products to protect the skin in the morning and 3 products to repair the skin at night. Participants were seen at baseline and evaluated for efficacy and tolerability at weeks 2, 6, and 12. Non-invasive measurements to evaluate hydration, transepidermal water loss, skin tone, and elasticity were conducted. The dermatologist investigator noted across-the-board improvement in all evaluated parameters, except deep wrinkles. By week 12, there were statistically significant (P<0.001) improvements in radiance (43%), tactile roughness (48%), visual roughness (44%), firmness (32%), clarity/even skin tone (21%), and overall appearance (29%). Fine lines improved 16% at week 12 (P=0.002). Participant self-assessment revealed statistically significant and progressive improvement in all evaluated parameters over time. No tolerability issues were identified by the investigator, while a small number of participants reported mild stinging and some dryness that resolved over time. This was likely due to the high concentration of active ingredients found in this regimen. Corneometry revealed improved skin hydration of 28% as early as week 2. The data presented confirms that this novel protection and repair regimen improves the appearance of environmentally aged skin. J Drugs Dermatol. 2024;23(10):866-872. doi:10.36849/JDD.8274.

Phytochemical Analysis and Antioxidant Activities of Various Extracts from the Aerial Part of Anemone baicalensis Turcz.: In Vitro and In Vivo Studies.

Anemone baicalensis Turcz., a botanical species with a rich historical background in traditional medicine for detoxification and insecticidal applications, possesses a vast, yet largely unexplored, therapeutic potential. This study primarily focused on conducting a qualitative phytochemical analysis of the plant, determining the active ingredient content and antioxidant activity of various solvent extracts. The qualitative phytochemical analysis revealed the presence of 12 different types of phytochemicals within the plant. Utilizing ultraviolet-visible spectrophotometry, we identified 11 active ingredients in 4 solvent extracts. Notably, the methanol extract was found to contain high concentrations of total carbohydrate, total monoterpenoid, total phenolic, total tannin, and total triterpenoid. In the antioxidant experiment, the methanol extract demonstrated superior scavenging abilities against 1,1-diphenyl-2-picrylhydrazyl radical, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonicacid) diammonium salt, superoxide anion radical, and hydrogen peroxide, outperforming other extracts in chelation experiments aimed at reducing iron and metal ions. Consequently, the methanol extract was selected for further investigation. Subsequent ultrahigh-performance liquid chromatography-electrospray ionization-quadrupole-time of flight-mass spectrometry analysis revealed that the methanol extract contained 39 compounds, primarily phenolic compounds and triterpenoid saponins. Three stability assessments confirmed the extract's stability under high temperatures, varying pH levels, and simulated gastrointestinal processes. Additionally, oil stability testing demonstrated its antioxidant capacity in extra virgin olive oil and cold-pressed sunflower seed oil media. An oral acute toxicity experiment conducted on mice not only confirmed the absence of acute toxicity in the methanol extract but also provided a dose reference for subsequent gastric protection experiments. Notably, the methanol extract exhibited significant gastroprotective effects against ethanol-induced gastric lesions in rats, as evidenced by histopathological and biochemical analyses. Specifically, the extract reduced levels of malondialdehyde, alanine aminotransferase, and aspartate aminotransferase while increasing glutathione, nitric oxide, and catalase, indicating its gastroprotective mechanism. These findings suggest that the methanol extract from the aerial part of Anemone baicalensis could be a promising therapeutic agent for conditions associated with oxidative imbalances. They underscore the plant's potential therapeutic benefits and offer valuable insights into its antioxidant properties, thereby broadening our understanding of its medicinal potential.

Discovery of Active Antibacterial Fractions of Different Plant Part Extracts of clove (Syzigium aromaticum) Against Streptococcus mutans

Nowadays, dental cavities caused by Streptococcus mutans are a major focus of research in Indonesia. While several antibiotics are available to combat this bacterium, concerns about antibiotic resistance have prompted researchers to explore natural remedies. Clove (Syzigium aromaticum) is a commonly studied natural remedy against dental cavities and S. mutans. Among the different parts of the clove plant, clove bud is the most widely used against dental cavities or S. mutans, and the potential of other clove parts has not been thoroughly explored. Identifying which parts of the clove plant have higher concentrations of active ingredients and exhibit the strongest antibacterial activity is important. Therefore, this study evaluated the antibacterial activity of three different parts, i.e., leaf, stems, and buds of the clove plant ethanolic extracts against S. mutans. The ethanolic extracts of clove leaf, stems, and buds were prepared using the maceration method with 70% ethanol, and their activity against S. mutans was tested using the disc diffusion method at three different concentrations (10%, 5%, 2.5% b/v). Fractionation was carried out using hexane and water to obtain two fractions: hexane and water fraction. These fractions were then subjected to antibacterial assays. The ethanolic leaf, stems, and bud extracts exhibited varying antibacterial activity levels. The best activity was observed with the 10% clove bud ethanolic extract, which produced an inhibition zone of 20.83 ± 0.77 mm. The leaf and stem extracts showed inhibition zones of 16.38 ± 3.84 mm and 17.95 ± 5.15 mm, respectively. Furthermore, the hexane-soluble fraction of the clove bud displayed the highest activity with an inhibition zone diameter of 23.7 ± 3.21 mm at 10%. This activity was twice as high as ampicillin, used as the positive control. In conclusion, clove bud remains the best source of antibacterial compounds against S. mutans. Fractionation of the bud extract using hexane can significantly enhance its activity. Further investigation should be conducted to optimize the effectiveness of this active fraction for use as an anti-dental caries treatment.

A Nondestructive and Rapid Method for the Determination of Triamterene Content by Transmission Raman Spectroscopy Combined with Chemometrics

Background: Triamterene is a potassium-conserving diuretic mainly used in the treatment of edematous diseases. Although there are some methods to measure the content of triamterene, the existing methods have the characteristics of sample destructiveness and low flux, making it difficult to meet the needs of online monitoring. In recent years, transmission Raman spectroscopy (TRS), as a new technology for the determination of drug content, has emerged as being nondestructive and rapid and provides a new method for the determination of triamterene content. Objective: In this study, we used transmission Raman spectroscopy combined with partial least squares (PLS) approaches to establish a six concentration levels model for measuring the content of triamterene. The model was applied to determine whether tablets are commercially available. Method: Firstly, TRS was used to collect the spectra of the principal components and mixed excipients of triamterene, and the feasibility test was carried out. Secondly, six concentration levels were determined by the design of experimental (DOE), and hand-made tablets were prepared to obtain corresponding spectra. The content prediction model was established by the PLS method, and the content of triamterene was determined by high-performance liquid chromatography (HPLC) to correct the model. Finally, the model was applied to the determination of triamterene in commercially available tablets. Results: The results showed that the established model was successfully applied to the determination of triamterene. The values of RMSEC (0.0089783) and RMSECV (0.0097241) of the final model were very low and close to each other. The relative error of 12 hand-made tablets predicted by this model was less than 5% compared with the results determined by HPLC. In addition, in the process of applying the model to the determination of the content of commercially available tablets, the accuracy of the model can be significantly improved by adding the spectrum of commercially available tablets. The corrected model was used to determine the content of triamterene in two commercially available tablets. The results showed that the relative error was less than 5%. Conclusion: We described a new strategy to analyze the content of active pharmaceutical ingredients (API) in triamterene tablets by TRS with PLS. The established model has the advantage of non-destructive and rapid quantitation, which can provide a new method for real-time monitoring of production lines and promote the development of process analytical technology (PAT).

Evavaltion of the Rotundin content of Stephania brachyandra (Diels) gene sources in Thai Nguyen province

The Stephania brachyandra plant, naturally found in Thai Nguyen, is scientifically known as Stephania brachyandra. It belongs to the genus Stephania Lour., family Menispermaceae, order Menispermaceae. This plant is used as a raw material to extract L-tetrahydropalmatine (the active ingredient known as Rotundin) with the chemical formula C21H25NO4. Rotundin is an alkaloid with sedative, sleep-inducing, and memory-reducing effects. The purpose of this study is to evaluate tof Rotundin content in the Stephania brachyandra species and analyze the correlation between the size of the specíe tubers and the content of Rotudin in Stephania brachyandra naturally distributed in Thai Nguyen province. The analysis results show that the content of Rotundin in 160 samples of naturally distributed Stephania brachyandra in Thai Nguyen province ranges from 90.4 to 981 mg/100g. The analysis of the correlation coefficient between tuber diameter and Rotundin content shows a strong relationship between Rotundin content and tuber diameter. This demonstrates diversity in active ingredient content among natural Stephania brachyandra plant samples, thereby confirming their significant potential as a medicinal resource.

Rapid and accurate identification of Gastrodia elata Blume species based on FTIR and NIR spectroscopy combined with chemometric methods

Different varieties of Gastrodia elata Blume (G. elata Bl.) have different qualities and different contents of active ingredients, such as polysaccharide and gastrodin, and it is generally believed that the higher the active ingredients, the better the quality of G. elata Bl. and the stronger the medicinal effects. Therefore, effective identification of G. elata Bl. species is crucial and has important theoretical and practical significance. In this study, first unsupervised PCA and t-SNE are established for data visualisation, follow by traditional machine learning (PLS-DA, OPLS-DA and SVM) models and deep learning (ResNet) models were established based on the fourier transform infrared (FTIR) and near infrared (NIR) spectra data of three G. elata Bl. species. The results show that PLS-DA, OPLS-DA and SVM models require complex preprocessing of spectral data to build stable and reliable models. Compared with traditional machine learning models, ResNet models do not require complex spectral preprocessing, and the training and test sets of ResNet models built based on raw NIR and low-level data fusion (FTIR + NIR) spectra reach 100 % accuracy, the external validation set based on low-level data fusion reaches 100 % accuracy, and the external validation set based on NIR has only one sample classification error and no overfitting.

Long-Term Treatment for Unspecified Anxiety Disorders with Cannabidiol: A Retrospective Case Series from Real-World Evidence in Colombia

Introduction: Preclinical and clinical evidence has elucidated that cannabis-based medical formulations (CBMFs) may display anxiolytic, antidepressive, and neuroprotective properties. CBMFs are often considered as novel therapeutic anxiolytic agents that can be prescribed as pharmacotherapy for symptomatic domains in anxiety disorders (ADs). Our aim was to explore effectiveness and tolerability of enriched cannabidiol (CBD) oil extract formulations in adults with anxiety symptoms in an outpatient mental health program in Colombia during the COVID-19 pandemic. Methods: We conducted an observational, retrospective, real-world evidence case series from electronic health records at Zerenia Clinic in Bogotá, Colombia between June 2021 and December 2022. Our convenience sample consisted of people searching for CBMFs for the treatment of anxiety symptoms. A cohort of 24 adults was prescribed with enriched CBD in the form of non-sterile oral liquids suspended in sesame seed oil extracts for DSM-5 unspecified anxiety disorder and followed throughout the first year of treatment. CBMFs were prepared by dissolving full-spectrum cannabis extracts in sesame seed oil to a standardized concentration of active ingredients which is CBD-enriched. The oil extract contained 100 mg/mL of CBD and less than 1.9 mg/mL of THC. Primary outcome measures established were the anxiety subscale in the Hospital Anxiety and Depression Scale (HADS-A), and the clinical global impression scale with regard to severity (CGI-S) and improvement (CGI-I) at baseline, 6 months, and 12 months during follow-up. Secondary outcome measures established were HADS depression subscale (HADS-D) and the Epworth Sleepiness Scale (ESS), respectively. Participants also completed the patient-reported outcome measures (PROMs) during each visit throughout the 12-month follow-up. PROMs documented both participantʼs subjective improvement experience and progressive adverse effects. Results: After 6 months of treatment with sublingually administered enriched CBD oil extracts in a median dosage of 100 mg, more than half (54.17%) of the sample continued to report significant anxiety symptoms. After 12 months, only 37.50% persisted with significant anxiety symptoms with a median dose of 120 mg of enriched CBD oil extracts. Similar subjective improvements were reported with regard to sleep disturbances (SDs) as a secondary outcome. At baseline, less than half (46.83%) of the sample reported significant daytime sleepiness. After 6 months of enriched CBD oil extract treatment, less than one third (29.17%) continued to report SDs. At end point, a high proportion of the sample (87.50%) were considered to have normal daytime sleepiness. The cohort showed no clinically relevant depressive symptoms at baseline based on HADS-D scores; therefore, no improvement could be reported throughout the 12-month follow-up. Minimal gender differences with regard to HADS-D scores may be attributed to modifying effects of menopause-related symptoms. No significant adverse drug reactions or deaths were reported during the 12-month follow-up. Conclusions: Further research should determine the long-term efficacy, safety, and appropriate dosages of enriched CBD oil extracts in treating specific ADs rather than broad and unspecified anxiety symptoms. The state of the art of CBMFs for ADs should be warranted by future randomized controlled trials. The next stage for cannabis research should be focused in performing head-to-head trials comparing enriched CBD extracts or capsules versus first-line treatments proven to be effective in ADs.

Antihypertensive mechanism of the medicine food homology compound solution with high ACE inhibition rate based on network pharmacology and molecular docking

Certain instances of medicine food homology (MFH) have an antihypertensive effect, which has a therapeutic effect on hypertension, but their mechanism in treating hypertension and improving blood pressure is still unclear. The objective of this study is to analyze the potential bioactive substances and the hypotensive mechanism by which the MFH compound solution (Hawthorn:Lycium barbarum:Cassia = 4:1:1) with a high angiotensin-converting enzyme (ACE) inhibition rate. This will be achieved through the use of network pharmacology and molecular docking techniques, which will be further validated through experimental testing. The key components in the MFH compound solution were obtained by constructing the component-disease target network, and Gene Ontology (GO) and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis were used to explore the pathways of the MFH compound solution participating in anti-hypertension. The content of the main active ingredients in the MFH compound solution was identified by high-performance liquid chromatography (HPLC). The main active components were quercetin, beta-sitosterol, stigmasterol, kaempferol, and isorhamnetin, while the identified core genes were AKT1 and TP53. Through pathway analysis, the mechanisms of the MFH compound solution against hypertension may be Lipid and atherosclerosis, Calcium signaling pathway, PI3K-AKT signaling pathway, etc. Moreover, the molecular docking of five key compounds and the top five targets verified the reliability of network pharmacology results. HPLC analysis revealed that these five active substances were detected in the MFH compound solution, where kaempferol was the most abundant. This study revealed that the MFH compound exerted a hypotensive effect through multiple targets and pathways.

Multi-Omics Analyses Uncover the Mechanism Underlying Polyploidization-Enhanced Steviol Glycosides Biosynthesis in Stevia rebaudiana.

Stevia rebaudiana (Bertoni) is a valuable sweetener plant whose sweetness primarily derives from steviol glycosides (SGs), especially rebaudioside A (RA). Polyploidization has the potential to enhance the content of active ingredients in medicinal plants, making this strategy a promising avenue for genetic improvement. However, the underlying regulatory mechanisms that contribute to the fluctuating SGs content between autotetraploid and diploid stevia remain unclear. In this study, we employed metabolic analysis to identify 916 differentially accumulated metabolites (DAMs), with the majority, specifically terpenoids, flavonoids, and lipids, exhibiting upregulation due to polyploidization. Notably, the content of stevia's signature metabolite SGs (including RA, steviolbioside, and rebaudioside C), along with their precursor steviol, increased significantly after polyploidization. Furthermore, a comprehensive analysis of the transcriptome and metabolome revealed that the majority of differentially expressed genes (DEGs) involved in the SG-synthesis pathway (ent-KAH, ent-KS1, UGT73E1, UGT74G1, UGT76G1, UGT85C2, and UGT91D2) were upregulated in autotetraploid stevia, and these DEGs exhibited a positive correlation with the polyploidization-enhanced SGs. Additionally, multi-omics network analysis indicated that several transcription factor families (such as five NACs, four WRKYs, three MYBs, eight bHLHs, and three AP2/ERFs), various transporter genes (four ABC transporters, three triose-phosphate transporters, and two sugar efflux transporters for intercellular exchange), as well as microorganisms (including Ceratobasidium and Flavobacterium) were positively correlated with the accumulation of RA and steviol. Overall, our results indicate the presence of a regulatory circuit orchestrated by polyploidization, which recruits beneficial rhizosphere microbes and modulates the expression of genes associated with SG biosynthesis, ultimately enhancing the SG content in stevia. This finding will provide new insights for promoting the propagation and industrial development of stevia.

Non-targeted metabolomics analysis of fermented traditional Chinese medicine and its impact on growth performance, serum biochemistry, and intestinal microbiome of weaned lambs

Fermented traditional Chinese medicines (TCMs) have been identified as a low-cost and promising feed additive to to alleviate weaning stress in young livestock and poultry effectively. This study investigated the impact of probiotic fermentation on the metabolite content of BanQi (Radix Isatidis and Astragalus membranaceus) extract while also examined the effects of both fermented-BanQi (FBQ) and unfermented-BanQi (UBQ) on growth performance, serum biochemistry, intestinal villi, and gut microbiota in weaned lambs. This study demonstrated that compared with UBQ, FBQ contained significantly higher levels of free amino acids (e.g., phenylalanine and isoleucine), short peptides (e.g., Val–Leu–Pro–Val–Pro–Gln and Gly–Leu), and the active ingredients (e.g., vindesine and reserpine) (P < 0.05). The addition of FBQ to the diet significantly increased the final body weight and average daily gain of weaned lambs (P < 0.05). In addition, FBQ significantly increased the total protein level in the serum and the villus length of the jejunum and ileum in lambs, while significantly reduced the levels of aspartate aminotransferase (AST) and urea (P < 0.05). Sequencing of the intestinal flora showed that FBQ improved the diversity of intestinal flora and promoted the enrichment of beneficial bacteria in the lamb intestine, such as Mogibacterium and Butyrivibrio, compared to NC or UBQ groups (P < 0.05). Fermentation with Bacillus subtilis can enhance the content of free amino acids, peptides, and active ingredients in BanQi extract, making it an effective method to improve the efficacy of traditional Chinese medicine. Adding FBQ to the diet can improve the growth performance of weaned lambs, and its mechanism may be related to increasing the height of intestinal villi and increasing the diversity of intestinal flora.

Physicochemical properties and volatile compounds of Rosa roxburghii fruit using different drying methods

To enhance the drying quality of Rosa roxburghii fruit, this study examined the effects of four methods: Natural Drying (ND), Hot Air Drying (AD), Heat Pump Drying (PD), and Vacuum Freezing Drying (FD). Fresh R. roxburghii fruit was used to assess drying characteristics, color, microstructure, active ingredient content, antioxidant activity, and volatile substances. Drying times for ND, AD, PD, and FD were 28, 7, 6, and 21 h, respectively, with the rate order PD > AD > FD > ND. AD samples showed superior water-binding capacity, solubility, and highest levels of flavonoids and polyphenols, enhancing antioxidant activity. FD samples had the best color performance and retained more intact cell structures and higher Vitamin C and polysaccharide levels. Volatile compounds were analyzed, revealing 45, 60, 61, and 50 compounds for ND, AD, PD, and FD, respectively. AD proved to be the most efficient method, providing optimal drying time, color, active ingredient content, antioxidant activity, and volatile components. This finding offers valuable guidance for selecting a drying method that preserves the quality of dried R. roxburghii fruit and suits industrial production.

Melanin resistance of heat-processed ginsenosides from Panax ginseng berry treated with citric acid through autophagy pathway

GFRS is the conversion product of Panax ginseng Meyer berry after citric acid heat treatment, which is rich in rare ginsenosides. However, the anti-melanin role of GFRS in the regulation of skin pigmentation and its material basis remains unclear. To compare the anti-melanin activity before and after citric acid heat treatment, we determined the effects of GFS and GFRS on tyrosinase activity and melanin lever under α-MSH stimulation and found the potential anti-melanin effect of GFRS. Further, Western blot and immunofluorescence methods were used to reveal the mechanism by which GFRS detects anti-melanin activity by promoting autophagy flux levels. In zebrafish models, GFRS inhibited endogenous melanin and tyrosinase better than arbutin and promoted the accumulation of autophagy levels in vivo. To determine the material basis of the anti-melanin effect of GFRS, HPLC was used to isolate and prepare 12 ginsenosides from GFRS, and their activity evaluation and structure–activity relationship analysis were performed. The results showed that the inhibitory effect of GFRS on melanin was Rg3 > Rg5 > Rk1 > Rd. Molecular docking showed that their docking fraction with mushroom tyrosinase was significantly better than that of arbutin, but the presence of C-20 glycosylation decreased the anti-melanin activity of Rd. To maximize the content of Rg3, Rg5, and Rk1, we optimized the process by using citric acid heat treatment of ginsenoside Rd and found that citric acid heat treatment at 100°C almost completely transformed Rd and obtained a high content of active ingredients. In summary, our data demonstrated that GFRS exerted anti-melanin effects by inducing autophagy. It was further revealed that Rg3, Rg5, and Rk1, as effective active components, could be enriched by the improved process of converting ginsenoside Rd by citric acid heat treatment.

Ultraselective Macrocycle Membranes for Pharmaceutical Ingredients Separation in Organic Solvents

Separations are core processes in the chemical and pharmaceutical industries. Several steps of fractionation and purification of multicomponent mixtures are required. Membrane technology can operate at fair temperatures, saving energy and processing sensitive compounds. However, breakthroughs require high stability and selectivity beyond those available today. Here, we propose membranes constituted by fully crosslinked crown ethers using interfacial polymerization. The 24 nm-thick nanofilms on robust porous supports exhibit up to 90% higher selectivity than commercially available membranes, with a 90% increase in solvent permeance. The membranes are tested with a complex mixture of structurally diverse solutes containing active pharmaceutical ingredients. The membranes are effective for the total retention and concentration of active pharmaceutical ingredients with molecular weights around 800 g mol–1. The ability to distinguish between smaller molecules in the range between 100 and 370 g mol–1 is confirmed with high separation factors, which could provide a significant advance for the pharmaceutical industry.