Search Results (40)

Fritillaria thunbergii Miq., a medicinal plant rich in steroidal alkaloids, produces bulbs that clear heat, resolve phlegm, and detoxify. However, excessive yield-oriented cultivation has reduced the number of F. thunbergii plants that meet commercial standards. This study explored the effects of potassium application and shading on the bulb biomass and medicinal substance content of F. thunbergii. Shading increased the active ingredient content in bulbs by approximately 20.71% but reduced biomass by approximately 17.24%. Fertilization with different potassium concentrations under shading (K1S–K3S) alleviated shading-induced biomass reduction and increased active ingredient accumulation, with the K2S and K3S groups yielding significantly better results than the K1S group. Pharmacological experiments showed that the K2S group exerted the best antitussive, expectorant, and anti-inflammatory effects. Metabolome analysis showed that compared with those in the controls, peiminine, peimine, imperialine, solasodine, and cyclopamine were the most abundant steroidal alkaloids under K2S treatment. Transcriptome analysis identified key genes and biosynthetic pathways for major steroidal alkaloids, namely, farnesyl pyrophosphate synthase (FtFPS) involved in steroidal alkaloid biosynthesis. Transcription factor analysis revealed that nine transcription factors predominantly expressed under the K2S treatment might regulate steroidal alkaloid biosynthesis. Furthermore, FtFPS was identified as a hub gene in the co-expression network and was verified to catalyze the biosynthesis of farnesyl pyrophosphate. The interaction between FtFPS and FtAP2/ERF was verified through yeast two-hybrid experiments. These findings offer new insights into the steroidal alkaloid biosynthesis mechanism triggered in F. thunbergii by potassium application and shading, supporting ecological strategies to enhance steroidal alkaloid levels in this species. Full article

Objective: This study was conducted to validate the involvement of the PAR2-PKC-TRPA1 pathway in cough hypersensitivity (CHS) development. Methods: Guinea pigs were divided into a blank control, a citric acid-induced enhanced cough model, and drug intervention groups. The effects of the drugs on capsaicin-induced cough responsiveness in a cough model were observed. The effects of individual and combined treatments (including PAR2 agonists, TRPA1 agonists, PAR2 antagonists, TRPA1 antagonists, PKC agonists, and PKC antagonists) on PAR2, phospho-PKC (pPKC), and TRPA1 expression in bronchial tissues and the vagus ganglion (jugular and nodose) in the cough model and control groups were assessed. Additionally, whole-cell patch-clamp recordings were conducted to evaluate the effects of the drugs on vagus ganglion neuron electrophysiological activity. Results: ① Both PAR2 antagonists and TRPA1 antagonists significantly reduced cough frequency in guinea pigs with a cough, and the PAR2 antagonist inhibited coughing induced by the TRPA1 agonist. ② Western blotting and multiplex immunohistochemistry (mIHC) indicated that PAR2, pPKCα, PKCα, and TRPA1 expression in bronchial and vagus ganglion tissues was elevated in the cough model compared with the control, with TRPA1 expression being regulated by PAR2 and PKC being involved in this regulatory process. ③ Whole-cell patch-clamp recordings demonstrated that TRPA1 agonists induced an inward current in nodose ganglion neurons, which was further amplified by PAR2 agonists; this amplification effect was blocked by PKC antagonist. Additionally, PAR2 antagonists inhibited the inward current induced by TRPA1 agonists. ④ At various concentrations, including the optimal antitussive concentration, PAR2 antagonists did not significantly affect pulse amplitude, arterial oxygen saturation, heart rate, body temperature, or respiratory rate in guinea pigs. Conclusion: PAR2 regulates TRPA1 through PKC in cough syndrome (CHS) pathogenesis, making targeting PAR2 a safe and effective therapeutic strategy for CHS. Full article

Pinelliae Rhizoma (PR), a highly esteemed traditional Chinese medicinal herb, is widely applied in clinical settings due to its diverse pharmacological effects, including antitussive, expectorant, antiemetic, sedative-hypnotic, and antitumor activities. Pinellia ternata exhibits morphological variation in its leaves, with types resembling peach, bamboo, and willow leaves. However, the chemical composition differences among the corresponding rhizomes of these leaf phenotypes remain unelucidated. This pioneering research employed Matrix-Assisted Laser Desorption/Ionization Mass Spectrometry Imaging (MALDI-MSI) to conduct the in situ identification and spatial profiling of 35 PR metabolites in PR, comprising 12 alkaloids, 4 organic acids, 12 amino acids, 5 flavonoids, 1 sterol, and 1 anthraquinone. Our findings revealed distinct spatial distribution patterns of secondary metabolites within the rhizome tissues of varying leaf types. Orthogonal Partial Least Squares Discriminant Analysis (OPLS-DA) effectively differentiated between rhizomes associated with different leaf morphologies. Furthermore, this study identified five potential differential biomarkers—methylophiopogonanone B, inosine, cytidine, adenine, and leucine/isoleucine—that elucidate the biochemical distinctions among leaf types. The precise tissue-specific localization of these secondary metabolites offers compelling insights into the specialized accumulation of bioactive compounds in medicinal plants, thereby enhancing our comprehension of PR’s therapeutic potential. Full article

Anthriscus sylvestris (L.) Hoffm. (Apiaceae), commonly known as wild chervil, has gained scientific interest owing to its diverse phytochemical profile and potential therapeutic applications. The plant, despite being categorized as a noxious weed, is traditionally used in treating various conditions like headaches, dressing wounds, and as a tonic, antitussive, antipyretic, analgesic, and diuretic. Its pharmacological importance stems from containing diverse bioactive lignans, especially aryltetralins and dibenzylbutyrolactones. One of the main compounds of A. sylvestris, deoxypodophyllotoxin, among its wide-ranging effects, including antitumor, antiproliferative, antiplatelet aggregation, antiviral, anti-inflammatory, and insecticidal properties, serves as a pivotal precursor to epipodophyllotoxin, crucial in the semisynthesis of cytostatic agents like etoposide and teniposide. The main starting compound for these anticancer medicines was podophyllotoxin, intensively isolated from Sinopodophyllum hexandrum, now listed as an endangered species due to overexploitation. Since new species are being investigated as potential sources, A. sylvestris emerges as a highly promising candidate owing to its abundant lignan content. This review summarizes the current knowledge on A. sylvestris, investigating its biological and morphological characteristics, and pharmacological properties. Emphasizing the biological activities and structure–activity relationship, this review underscores its therapeutic potential, thus encouraging further exploration and utilization of this valuable plant resource. Full article

Levodropropizine is a non-narcotic, non-centrally acting antitussive that inhibits the cough reflex triggered by neuropeptides. Despite the active clinical application of levodropropizine, the exploration of its inter-individual pharmacokinetic diversity and of factors that can interpret it is lacking. The purpose of this study was to explore effective covariates associated with variation in the pharmacokinetics of levodropropizine within the population and to perform an interpretation of covariate correlations from a therapeutic perspective. The results of a levodropropizine clinical trial conducted on 40 healthy Korean men were used in this pharmacokinetic analysis, and the calculated pharmacokinetic and physiochemical parameters were screened for effective correlations between factors through heatmap and linear regression analysis. Along with basic compartmental modeling, a correlation analysis was performed between the model-estimated parameter values and the discovered effective candidate covariates for levodropropizine, and the degree of toxicity and safety during the clinical trial of levodropropizine was quantitatively monitored, targeting the hepatotoxicity screening panel. As a result, eosinophil level and body surface area (BSA) were explored as significant (p-value < 0.05) physiochemical parameters associated with the pharmacokinetic diversity of levodropropizine. Specifically, it was confirmed that as eosinophil level and BSA increased, levodropropizine plasma exposure increased and decreased, respectively. Interestingly, changes in an individual’s plasma exposure to levodropropizine depending on eosinophil levels could be interpreted as a therapeutic advantage based on pharmacokinetic benefits linked to the clinical indications for levodropropizine. This study presents effective candidate covariates that can explain the inter-individual pharmacokinetic variability of levodropropizine and provides a useful perspective on the first-line choice of levodropropizine in the treatment of inflammatory respiratory diseases. Full article

Noscapine is a naturally occurring alkaloid isolated from Papaver somniferum, commonly known as opium poppy or bread seed poppy. It edges over other opioids as it lacks addictive, sedative or euphoric effects. This review chronicles the saga of endeavours with noscapine, from modest efforts in the mid-1950s to its present anticancer potential and futuristic hope in combating COVID-19. We comprehensively searched for publications including noscapine- and noscapinoid-relevant keywords in different electronic databases such as PubMed, Google Scholars, Elsevier, Springer Link and Science Direct up to June 2023. We excluded those in a language other than English. Noscapine has long been used as an antitussive and suppresses coughing by reducing the activity of the cough centre in the brain. A great number of water-soluble noscapine analogues have been found to be impressive microtubule-interfering agents with a superior antiproliferative activity, inhibiting the proliferation of cancer cell lines with more potency than noscapine and bromo-noscapine. With enhanced drug delivery systems, noscapine has exerted significant therapeutic efficacy in animal models of Parkinson’s disease, polycystic ovary syndrome, multiple sclerosis and other disorders. Furthermore, the merit of noscapine in crossing the blood–brain barrier makes it a putative candidate agent against neurodegenerative and psychiatric diseases. Its long safety record, widespread availability and ease of administration make it an ideal candidate for fighting several life-threatening conditions. Recent promising docking studies onnoscapine with main protease (Mpro) of SARS-CoV-2 paves the way for combinatorial drug therapy with anti-viral drugs and is hopeful in fighting and triumphing over any future COVID-19 pandemic. Full article

The roots of Peucedanum praeruptorum Dunn and Angelica decursiva Franchet et Savatier are designated Zenko, which is a crude drug defined by the Japanese Pharmacopoeia. This crude drug is used as an antitussive and an expectorant and is included in the Kampo formula Jinsoin, which improves cough, fever, and headache. Although the anti-inflammatory effects of this crude drug have been determined, the constituents responsible for this effect remain unknown. To investigate biologically active compounds, rat hepatocytes were used, which produce proinflammatory mediator nitric oxide (NO) in response to proinflammatory cytokine interleukin 1β (IL-1β). A methanol extract of P. praeruptorum roots, which suppressed IL-1β-induced NO production, was fractionated into three crude fractions (ethyl acetate (EtOAc)-soluble, n-butanol-soluble, and water-soluble fractions) based on hydrophobicity. The EtOAc-soluble fraction markedly inhibited NO production. After this fraction was purified, three biologically active compounds were identified as praeruptorins A, B, and E, the contents of which were high. A comparison of their activities indicated that praeruptorin B exhibited the highest potency to inhibit NO production by decreasing inducible NO synthase expression and suppressed the expression of mRNAs encoding proinflammatory cytokines. Collectively, the three praeruptorins may primarily contribute to the anti-inflammatory effects of P. praeruptorum roots. Full article

Sweet mogrosides are not only the primary bioactive ingredient in Siraitia grosvenorii fruits that exhibit anti-tussive properties and expectorate phlegm, but they are also responsible for the fruit’s sweetness. Increasing the content or proportion of sweet mogrosides in Siraitia grosvenorii fruits is significant for improving their quality and industrial production. Post-ripening is an essential step in the post-harvest processing of Siraitia grosvenorii fruits, but the underlying mechanism and condition of post-ripening on Siraitia grosvenorii quality improvement need to be studied systematically. Therefore, this study analyzed the mogroside metabolism in Siraitia grosvenorii fruits under different post-ripening conditions. We further examined the catalytic activity of glycosyltransferase UGT94-289-3 in vitro. The results showed that the post-ripening process of fruits could catalyze the glycosylation of bitter-tasting mogroside IIE and III to form sweet mogrosides containing four to six glucose units. After ripening at 35 °C for two weeks, the content of mogroside V changed significantly, with a maximum increase of 80%, while the increase in mogroside VI was over twice its initial amount. Furthermore, under the suitable catalytic condition, UGT94-289-3 could efficiently convert the mogrosides with less than three glucose units into structurally diverse sweet mogrosides, i.e., with mogroside III as the substrate, 95% of it can converted into sweet mogrosides. These findings suggest that controlling the temperature and related catalytic conditions may activate UGT94-289-3 and promote the accumulation of sweet mogrosides. This study provides an effective method for improving the quality of Siraitia grosvenorii fruits and the accumulation of sweet mogrosides, as well as a new economical, green, and efficient method for producing sweet mogrosides. Full article

Zingiber officinale Roscoe. (ginger) is a widely distributed plant with a long history of cultivation and consumption. Ginger can be used as a spice, condiment, food, nutrition, and as an herb. Significantly, the polysaccharides extracted from ginger show surprising and satisfactory biological activity, which explains the various benefits of ginger on human health, including anti-influenza, anti-colitis, anti-tussive, anti-oxidant, anti-tumor effects. Here, we systematically review the major studies on the extraction and purification of polysaccharides from ginger in recent years, the characterization of their chemical structure, biological activity, and structure–activity relationships, and the applications of ginger polysaccharides in different fields. This article will update and deepen the understanding of ginger polysaccharide and provide a theoretical basis for its further research and application in human health and product development. Full article

Adansonia digitata L. fruit, also known as baobab, has been used traditionally throughout the world for its medicinal properties. Ethnopharmacological uses of various plant parts have been reported for hydration, antipyretic, antiparasitic, antitussive, and sudorific properties and also in the treatment of diarrhea and dysentery in many African countries. Several studies have revealed that in addition to these applications, baobab has antioxidant, anti-inflammatory, analgesic, and antimicrobial activities. The health benefits of baobab have been attributed to its bioactive compounds, namely phenols, flavonoids, proanthocyanins, tannins, catechins, and carotenoids. Baobab fruit is also an important source of vitamin C and micronutrients, including zinc, potassium, magnesium, iron, calcium, and protein, which may reduce nutritional deficiencies. Despite scientific studies revealing that this fruit has a wide diversity of bioactive compounds with beneficial effects on health, there is a gap in the review of information about their mechanisms of action and critical analysis of clinical trials exploring, in particular, their effect on glycemia regulation. This work aims to present a current overview of the bioactive compounds, biological activities, and effects of A. digitata fruit on blood glucose, highlighting their potential mechanisms of action and effects on glycemia regulation, evaluated in recent animal and human trials. Full article

Platycosides, saponins from balloon flower root (Platycodi radix), have diverse health benefits, such as antioxidant, anti-inflammatory, anti-tussive, anti-cancer, anti-obesity, anti-diabetes, and whitening activities. Deglycosylated platycosides, which show greater biological effects than glycosylated platycosides, are produced by the hydrolysis of glycoside moieties in glycosylated platycosides. In this review, platycosides are classified according to the chemical structures of the aglycone sapogenins and also divided into natural platycosides, including major, minor, and rare platycosides, depending on the content in Platycodi radix extract and biotransformed platycosides. The biological activities of platycosides are summarized and methods for deglycosylation of saponins, including physical, chemical, and biological methods, are introduced. The biotransformation of glycosylated platycosides into deglycosylated platycosides was described based on the hydrolytic pathways of glycosides, substrate specificity of glycosidases, and specific productivities of deglycosylated platycosides. Methods for producing diverse and/or new deglycosylated platycosides are also proposed. Full article

Both the bulbs and flowers of Fritillaria thunbergii Miq. (BFT and FFT) are widely applied as expectorants and antitussives in traditional Chinese medicine, but few studies have been conducted to compare the chemical compositions of these plant parts. In this study, 50% methanol extracts of BFT and FFT were analyzed via UHPLC-Q-Exactive Orbitrap MS/MS, and the feasibility of using non-targeted UHPLC-HRMS metabolomics and molecular networking to address the authentication of bulb and flower samples was evaluated. Principal component analysis (PCA), Orthogonal Partial Least Squares-Discriminant Analysis (OPLS-DA), and heat map analysis showed there were dissimilar metabolites in BFT and FFT. As a result, 252 and 107 peaks in positive ion mode and negative mode, respectively, were considered to represent significant difference variables between BFT and FFT. Then, MS/MS-based molecular networking of BFT and FFT was constructed to perform an in-depth characterization of the peaks using different variables. A total of 31 alkaloids with significant differences were annotated in this paper, including seven cis-D/E-vevanine without C20-OH and one trans-D/E-cevanine with C20-OH, thirteen trans-D/E-cevanine without C20-OH, five cevanine N-oxide, and five veratramine. Among the 31 alkaloids, eight alkaloids had higher FFT than BFT contents, while all the flavonoids identified in our work had greater FFT than BFT contents. The influence of different ingredients on the pharmacological activities of BFT and FFT should be investigated in future studies. Full article

Siraitia grosvenorii (Swingle) C. Jeffrey ex Lu et Z. Y. Zhang is a unique economic and medicinal plant of Cucurbitaceae in Southern China. For hundreds of years, Chinese people have used the fruit of S. grosvenorii as an excellent natural sweetener and traditional medicine for lung congestion, sore throat, and constipation. It is one of the first species in China to be classified as a medicinal food homology, which has received considerable attention as a natural product with high development potential. Various natural products, such as triterpenoids, flavonoids, amino acids, and lignans, have been released from this plant by previous phytochemical studies. Phar- macological research of the fruits of S. grosvenorii has attracted extensive attention, and an increasing number of extracts and compounds have been demonstrated to have antitussive, expectorant, antiasthmatic, antioxidant, hypoglycemic, immunologic, hepatoprotective, antibacte- rial, and other activities. In this review, based on a large number of previous studies, we summarized the related research progress of the chemical components and pharmacological effects of S. grosvenorii, which provides theoretical support for further investigation of its biological functions and potential clinical applications. Full article

Chamaedorea tepejilote Liebm is a palm native to the south of Mexico and Central America. In Mexico, the male inflorescences are roasted, fried, boiled, or accompanied by other ingredients to decrease their bitter aftertaste, and they can be consumed by the inhabitants. However, it has been observed that raw inflorescences have hypoglycemic, antitussive, and antimicrobial potentials, but the thermal treatment effect in these activities has not been studied; for this reason, this study evaluated the impact of three thermal treatments (hydrothermal (HP), steaming at elevated pressure (SEP), and microwave (MW)) on the nutritional and nutraceutical characteristics of Pacaya inflorescences; inflorescences without thermal treatment (WTT) were considered as the control. In the nutritional characterization, only the protein content was the fraction that increased significantly (p < 0.05) when thermal treatment was applied. On the other hand, all thermal treatments significantly modified (p < 0.05) the chlorophyll “a” content (HP reduced 0.59-fold; SEP and MW increased 0.07-0.25-fold), and chlorophyll “b” decreased. A significant (p < 0.05) carotenoids content increase in all thermally treated samples (between 0.80-fold and 8.73-fold) and total phenolic compounds (between 7.75-fold and 8.16-fold) compared to the WTT samples was observed. Microwave cooking was the only thermal treatment that significantly (p < 0.05) increased (0.97-fold) the antioxidant activity in the DPPH radical. HP (14.11%) and SEP (18.20%) significantly (p < 0.05) reduced the dipeptidyl peptidase-IV enzyme inhibition when compared to WTT (24.42%). These changes have been associated with the partial loss, destruction, or denaturalization of cell walls’ proteins, lipids, or cellulose, causing the liberating or creation of compounds with nutritional and nutraceutical activity. Full article

Background: Himalayan Viola species (Banksha) are traditionally important herbs with versatile therapeutic benefits such as antitussive, analgesic, antipyretic, antimalarial, anti-inflammatory, and anticancerous ones. The current investigation was focused on exploring polyphenolic profiles, antioxidant, and antimicrobial potentials of wild viola species at 15 gradient locations (375–1829 m). Methods: Morphological, physiochemical, and proximate analyses were carried out as per WHO guidelines for plant drug standardization. Total polyphenolic and flavonoid content were carried out using gallic acid and rutin equivalent. UPLC-DAD was used to profile the targeted polyphenols (gallic acid, vanillic acid, syringic acid, p-coumaric acid, ferulic acid, rutin, quercetin, luteolin, caffeic acid, and epicatechin). Similarly, all samples were screened for antioxidant and antimicrobial activity. Statistical analysis was used to correlate polyphenolic and targeted activities to assess Viola species adaptation behavior patterns. Results: Viola canescens (V. canescens) and Viola pilosa (V. pilosa) were found abundantly at their respective sites. Among flowers and leaves, flowers of V. canescens and V. pilosa showed higher total polyphenolic and flavonoid content (51.4 ± 1.13 mg GAE/g and 65.05 ± 0.85 mg RE/g, and 33.26 ± 0.62 mg GAE/g and 36.10 ± 1.41 mg RE/g, respectively). Furthermore, UPLC-DAD showed the uppermost content of p-coumaric acid in flowers and ferulic acid in leaves, while rutin was significant in both the tissues. Conclusions: The adaptive behavior of Viola species showed variability in morphological characters with the altitudes, while targeted polyphenols and activities were significant at mid-altitudes. This research helps in the selection of right chemotype for agrotechnological interventions and the development of nutraceutical products. Full article