Assessment of the Significance and Clinical Implications of Stress Hormones in Acute Pressure Injuries Among Trauma Patients.

Objective: This study examines the dynamic changes of stress hormones, including insulin (INS), fasting blood glucose (FBG), glucagon (Glu), and cortisol (Cort), in trauma patients. By monitoring these changes and observing acute pressure injury (API) occurrences on the skin, the research analyzes the influence of stress hormones on API development in trauma patients. Methods: A prospective analysis involved 218 trauma patients admitted to a grade III-A general hospital in Wenzhou from April 2021 to June 2023. Among them, 44 cases developed API (API group), and 174 cases did not (control group). Levels of INS, Cort, Glu, and FBG were measured in both groups. Additionally, Abbreviated Injury Scale-Injury Severity Score (AIS-ISS) surveys and API severity assessments were conducted. Correlations between stress hormone levels and AIS-ISS were discussed. The predictive effects of AIS-ISS and stress hormones on API occurrence in trauma patients were analyzed using receiver operating characteristic (ROC) curves. The relationship between stress hormone levels and API severity was also observed. Results: Study's outcomes indicated distinct relationships between stress hormone levels and API occurrence in trauma patients. Specifically, INS demonstrated a negative correlation with AIS-ISS, highlighting its potential as a significant factor. Glu, Cort, and FBG revealed positive associations, emphasizing their roles in influencing API development (P < .05). The diagnostic efficacy of stress hormones in predicting API occurrence, as represented by the Area Under Curve (AUC) = 0.8100. Notably, within the API group, INS levels demonstrated a decline with worsening API. Conversely, Glu, Cort, and FBG exhibited increases in tandem with the aggravation of API symptoms (P < .05). Conclusions: This research suggests that assessing stress hormone levels in clinical settings can effectively predict API occurrence. Early testing could aid in the development of preventive or intervention measures, reducing the incidence and harm of API in trauma patients.

Chemodynamic/Photothermal Synergistic Cancer Immunotherapy Based on Yeast Microcapsule-Derived Au/Pt Nanoparticles.

In recent years, microbiota-based tumor immunotherapy has become a hotspot in cancer research. However, the use of microorganisms alone to activate the immune response for antitumor therapy was unsatisfactory. In this study, we biosynthesized gold nanoparticles (AuNPs) and platinum nanoparticles (PtNPs) based on yeast microcapsules to activate the immune response for antitumor treatment in synergy with chemodynamic therapy (CDT) and photothermal therapy (PTT). We generated AuNPs and PtNPs on yeast microcapsules (YAP) and fabricated nanoscale particles (Bre-YAP) by ultrasonic fragmentation and differential centrifugation. Bre-YAP retained the glucan component of yeast as an adjuvant; in the meantime, these two kinds of metal nanoparticles contained were excellent CDT and PTT mediators. By inspection, they could reach a high level of distribution in tumors and tumor-draining lymph nodes (TDLNs). Under the laser irradiation of tumors, this immunological nanomaterial significantly remodeled the microenvironments of tumors and TDLNs. The primary tumors were effectively inhibited or even eradicated, and the overall survival of mice was significantly improved as well. Therefore, yeast microcapsule-based Bre-YAP with immune properties could be used as an effective cancer treatment modality.

The processing methods, phytochemistry and pharmacology of Gastrodia elata Bl.: A comprehensive review.

ETHNOPHARMACOLOGICAL RELEVANCE: Gastrodia elata Bl. (GE) is one of the rare Chinese medicinal materials with a long history of medicine and cooking. It consists of a variety of chemical components, including aromatic compounds, organic acids and esters, steroids, saccharides and their glycosides, etc., which has medicinal and edible value, and is widely used in various diseases, such as infantile convulsions, epilepsy, tetanus, headache, dizziness, limb numbness, rheumatism and arthralgia. It is also commonly used in health care products and cosmetics. Thus, its chemical composition and pharmacological activity have attracted more and more attention from the scientific community. AIM: In this review, the processing methods, phytochemistry and pharmacological activities of GE were comprehensively and systematically summarized, which provides a valuable reference for researchers the rational of GE. MATERIALS AND METHODS: A comprehensive search of published literature and classic books from 1958 to 2023 was conducted using online bibliographic databases PubMed, Google Scholar, ACS, Science Direct Database, CNKI and others to identify original research related to GE, its processing methods, active ingredients and pharmacological activities. RESULTS: GE is traditionally used to treat infantile convulsion, epilepsy, tetanus, headache, dizziness, limb numbness, rheumatism and arthralgia. To date, more than 435 chemical constituents were identified from GE including 276 chemical constituents, 72 volatile components and 87 synthetic compounds, which are the primary bioactive compounds. In addition, there are other biological components, such as organic acids and esters, steroids and adenosines. These extracts have nervous system and cardiovascular and cerebrovascular system activities such as sedative-hypnotic, anticonvulsant, antiepileptic, neuron protection and regeneration, analgesia, antidepressant, antihypertensive, antidiabetic, antiplatelet aggregation, anti-inflammatory, etc. CONCLUSION: This review summarizes the processing methods, chemical composition, pharmacological activities, and molecular mechanism of GE over the last 66 years, which provides a valuable reference for researchers to understand its research status and applications.

Isolation, structural properties, and bioactivities of polysaccharides from Althaea officinalis Linn.: A review.

Althaea officinalis Linn. (AO) is a widely distributed herbaceous plant with a long history of medicinal and food functions in Europe and Western Asia. Althaea officinalis polysaccharide (AOP), as one of the main components and a crucial bioactive substance of AO, has a variety of pharmacological activities, including antitussive, antioxidant, antibacterial, anticancer, wound healing, immunomodulatory, and infertility therapy effects. Many polysaccharides have been successfully obtained in the last five decades from AO. However, there is currently no review available concerning AOP. Considering the importance of AOP for biological study and drug discovery, the present review aims to systematically summarize the recent major studies on extraction and purification methods of polysaccharides from different AO parts (seeds, roots, leaves and flowers), as well as the characterization of their chemical structure, biological activity, structure-activity relationship, and the application of AOP in different fields. Meanwhile, the shortcomings of AOP research are further discussed in detail, and new valuable insights for future AOP research as therapeutic agents and functional foods are proposed.

Development of an online UPLC-PDA-ESI-Q-TOF-MS-LOX-FLD system for rapid screening of anti-inflammatory compounds in Polygala tenuifolia Willd.

In this study, the first ultra-high performance liquid chromatography-photo-diode array-electrospray ionization-quadrupole-time-of-flight-mass spectrometry-lipoxygenase-fluorescence detector (UPLC-PDA-ESI-Q-TOF-MS-LOX-FLD) online system was developed for the identification and evaluation of anti-inflammatory active ingredients in Polygala tenuifolia Willd. Using this system, the UPLC fingerprints, mass fragments and LOX-binding peak profiles in the samples were rapidly and simultaneously obtained. A total of 101 compounds were isolated and identified and 38 compounds (11 oligosaccharide esters, nine xanthones, 17 saponins, and one glycosyloxyflavone) showed strong LOX-binding activity. Six compounds were selected to study their LOX-binding ability, and the results indicated that the content of the six compounds had a good linear relationship with the LOX-binding ability, and it was found that the substitution position, the type of substituent and the number of glycosyl groups all had a certain influence on the LOX-binding ability of the compounds. The LOX-binding activities of 10 compounds were verified by the surface plasmon resonance (SPR) technique and the activity results were consistent with the online system. After validation, we identified 7 active compounds that combined with LOX to exert anti-inflammatory effects for the first time. All the results fully demonstrate the efficiency, stability and reliability of the online system and this work provides an exemplary and useful method for the rapid screening of potential anti-inflammatory active compounds in P. tenuifolia and other traditional Chinese medicines. At the same time, it provides a new direction for screening small molecule inhibitors of enzymes like LOX.

Evaluation of antioxidant, enzyme inhibition, nitric oxide production inhibitory activities and chemical profiles of the active extracts from the medicinal and edible plant: Althaea officinalis.

To develop the medicinal and edible plant resources of Althaea officinalis Linn in Europe and other places, this study concentrated on the bioactive ingredients of its different extracts. The phytochemical compositions of MeOH extracts were evaluated by UPLC-DAD-ESI-Q-TOF-MSn analysis. The in vitro antioxidant properties, enzymes inhibitory effects and nitric oxide (NO) production inhibitory activities of fractions obtained from the aerial parts of Althaea officinalis (APAO) were evaluated. The results identified 76 compounds, including 8 phenolic acids, 17 flavonoids, 6 coumarins, 9 triterpenes and 11 alkaloids. Fr. C-2 of APAO was found to have the highest TPC (175.8 ± 1.5 mg GAE/g) and TFC (466.9 ± 5.0 mg RE/g) with the highest antioxidant capacity in DPPH, ABTS, CUPRAC, FRAP and ß-carotene bleaching assays. Fr. A showed noticeable inhibition of α-glucosidase with an IC50 value of 3.8 ± 0.1 µg/mL. However, Fr. B displayed stronger inhibitory activity on 5-lipoxygenase than quercetin, with the IC50 value of 8.4 ± 1.6 µg/mL. In addition, Fr. B also possessed potent inhibitory activities on NO production toward LPS-activated RAW 264.7 Cells with an IC50 value of 15.7 ± 1.6 µg/mL. Our findings suggest that different Althaea officinalis extracts may be considered sources of phenolic and flavonoid compounds with high potential as natural antioxidants, anti-inflammatory agents and blood sugar regulators. In addition, they can also be used in food and nutraceutical products with enhanced bioactivities.

Screening 5-lipoxygenase inhibitors from selected traditional Chinese medicines and isolation of the active compounds from Polygoni Cuspidati Rhizoma by an on-line bioactivity evaluation system.

To identify natural products as new prototypes for 5-lipoxygenase (5-LOX), 12 traditional Chinese medicines (TCMs) were selected for screening their 5-LOX inhibition activities. The results showed that the methanol extracts of all selected TCMs (n = 12) possessed inhibitory activities against 5-LOX at 200 µg/mL, of which six extracts of the TCMs showed significant inhibitory effects with IC50 values in the range from 33.2 ± 1.4 µg/mL to 153.5 ± 1.7 µg/mL, and the extract of Polygoni Cuspidati Rhizoma (RPC) was the most active sample. An on-line ultra-performance liquid chromatography-photodiode array-MSn -5-LOX-fluorescence detector (UPLC-PDA-MSn -5-LOX-FLD) method was applied to further identify the potential 5-LOX inhibitory constituents in RPC extracts, which resulted in the identification of seven components with 5-LOX-binding activities. Finally, four compounds (polydatin, resveratrol, emodin-8-O-glucoside, and emodin) were successfully purified from RPC extracts. The 5-LOX inhibition action was assayed in vitro, and the results showed that these compounds possessed potent inhibitory effects against 5-LOX with IC50 values of 15.3 ± 2.1, 4.5 ± 1.2, 23.8 ± 0.4, and 11.8 ± 1.5 µg/mL, respectively. This was the first study to reveal the 5-LOX inhibitory constituents of RPC, and the present investigation might provide a valuable approach for the rapid discovery of natural inhibitors from TCMs.

Yeast Microcapsule Mediated Natural Products Delivery for Treating Ulcerative Colitis through Anti-Inflammatory and Regulation of Macrophage Polarization.

The common and frequent disease, ulcerative colitis (UC), causes serious physical and mental distress to patients. M2 macrophages have proven to play a role in anti-inflammation, which is a new potential target for UC therapy. In this study, we designed a safe and macrophages-targeting oral drug delivery system. Natural products, berberine (BBR), and Epigallocatechin Gallate (EGCG) with anti-inflammatory activity were assembled and encapsulated into yeast microcapsule (YM), generating therapeutic system BBR/MPN@YM. BBR and EGCG exhibited synergistic effects against UC through the effect of antioxidation. Through the interaction between ß-1,3-d-glucan on the surface of YM and dectin-1 receptors on macrophages, BBR/MPN@YM could be effectively transported to inflammation parts and internalized into macrophages, avoiding gastric degradation. In the in vivo UC mouse model, BBR/MPN@YM could transform M1 macrophages into anti-inflammatory M2 macrophages, thus exerting specific anti-inflammatory effects. Therefore, this BBR/MPN@YM targeted oral drug delivery system provided a new macrophages-targeting strategy for the clinical treatment of UC.

A novel green synthesis of silver nanoparticles by the residues of Chinese herbal medicine and their biological activities.

Green synthesis of silver nanoparticles (AgNPs) by using the extracts of Chinese herbal medicines (CHMs) has attracted tremendous attention due to the potential synergistic effect between metal nanoparticles and capping agents. However, since CHMs are precious and expensive, finding other cheap and eco-friendly resources for biosynthesizing AgNPs with superior medicinal activites is necessary. Herbal medicine residues (HMRs) are the by-products of traditional Chinese herbal medicine after decoction and were identified to contain approximately 30-50% of medicinally active ingredients, which may be advantageous for green synthesis of medicinal AgNPs. Inspired by this, we present herein the preparation of AgNPs by reusing Bazheng Mixture residues and evaluate both biosynthesis parameters and bioactivities, where Bazheng Mixture is a famous Chinese patent medicine for relieving inflammation and pain, and allaying fever. The UV-visible spectrum and DLS analysis showed that the as-prepared AgNPs were sensitive to pH, material proportion and incubation time, but the yield was impervious to material proportion. TEM, HRTEM, SAED and DLS characterization found that AgNPs (pH 10.0; material proportion 1 : 1; 6 h) had a face-centered cubic (fcc) structure and spherical shape with an average size of 22.2 ± 0.5 nm covered by anions, and existed in monodispersed form with long term stability. The AgNPs displayed potent toxic effects against both cancer cell lines and pathogens, and superior antioxidant activity. The IC50 for HCT116, HepG2 and HeLa cell lines were 13.07, 19.67, and 26.18 µg mL-1, respectively. The MICs of AgNPs for E. coli and S. aureus were both 50.0 µg mL-1. The uptake analysis of AgNPs for both pathogens and cancer cell lines was performed to preliminarily illustrate the mechanism of toxic effects. These results confirm that HMRs could be a low-cost, nontoxic and eco-friendly resource for green synthesis of medicinal AgNPs, and also provide an alternative method for general recycling strategies of HMRs.

Design, synthesis of Cinnamyl-paeonol derivatives with 1, 3-Dioxypropyl as link arm and screening of tyrosinase inhibition activity in vitro.

This study aimed to obtain tyrosinase inhibitors for treating hyperpigmentation. A series of cinnamyl ester analogues were designed and synthesized with cinnamic acid (CA) and peaonol compounds. The safety, melanin content and inhibitory effects of all target compounds were evaluated. In the enzymatic activity test, the inhibitory rate of compounds 8, 13 and 14 had stronger inhibitory activity with the IC50 values of 20.7 µM, 13.98 µM and 15.16 µM, respectively than the positive drug kojic acid (IC50 with 30.83 µM). The cytotoxicity evaluation showed that compounds 13 and 14 have higher safety than the other compounds to the proliferation of B16F10 cells. The result of the melanocyte test supported that compound13 has stronger cellular tyrosinase inhibitory activity than kojic acid and arbutin at 100 µM and 200 µM. The enzyme kinetics mechanism revealed that compound 13 was a non-competitive inhibitor while compounds 8 and 14 were mixed inhibitors. For the experiments of melanin content and tyrosinase activity in the B16F10 melanona cells, the inhibition rates of compounds 8, 14 and 13 were with 19.62%, 20.59% and 23.83%, respectively. In addition, compound 13 revealed the highest inhibitory activity to tyrosinase in the melanocyte with inhibition rates of 23.83%, which was better than kojic acid and arbutin (19.21% and 20.45%) at the same concentration. In the anti-melanogenesis experiment, compounds 8 and 13 had better anti-melanin effects than kojic acid from 25 µM to 100 µM. In summary, the results indicated that compounds 8, 13 and 14 had better tyrosinase inhibitory activity and anti-melanogenesis activity. Especially, the compound 13 has potentiality to develop novel tyrosinase inhibitors and whitening agents. The docking studies results revealed that the functional group of compound 13 mostly depends on the phenolic hydroxyl moiety, and its hydroxyl group did not insert into the active site of tyrosinase, which was in agreement with the results of the kinetics study.

[Preparation and quality standard of standard decoction of Scrophulariae Radix pieces].

The standard decoction of Chinese herbal decoction pieces is a standard reference substance to measure whether different dosage forms of Chinese medicine are basically consistent with those of clinical decoction,and provides new ideas and methods for effectively solving the problems of uneven quality in Chinese medicine dispensing granules. In this study,a systematic method for evaluating the quality of Scrophulariae Radix decoction was established from the perspective of " standard decoction",providing reference for the quality control of the Scrophulariae Radix dispensing granules. 15 batches of Scrophulariae Radix decoction pieces from different origins were collected,and 15 batches of standard decoctions were prepared according to the standardized process with water as solvent.Harpagide and harpagoside were used as quantitative detection indicators to determine the content,calculate the transfer rates and determine the extraction rate. The high performance liquid chromatography( HPLC) was used to establish a standard decoction fingerprint analysis method. The results showed that the transfer rates of harpagide and harpagoside in 15 batches of Scrophulariae Radix pieces standard decoction were( 70. 84±13. 39) % and( 48. 56±6. 40) % respectively; the extraction rate was( 57. 47±5. 89) %. Nine peaks were identified in the HPLC fingerprint,and the similarity was higher than 0. 97 between the fingerprints of 15 batches of standard decoction and the control fingerprint. In this study,the preparation process of standard decoction of Scrophulariae Radix pieces conformed to the traditional decoction preparation method. The sources of the samples were representative,and the established fingerprint method was stable and feasible,which can provide reference for the preparation and quality control of Scrophulariae Radix dispensing granules.

LC-MS guided isolation of gracilistones A and B, a pair of diastereomeric sesquiterpenoids with an unusual tetrahydrofuran-fused tricyclic skeleton from Acanthopanax gracilistylus and their potential anti-inflammatory activities.

Gracilistones A (1) and B (2), two new eudesmane-type sesquiterpenoids with an unusual tetrahydrofuran-fused 6/6/5 tricyclic ring system, were obtained from Acanthopanax gracilistylus under the guidance of LC-MS investigation. Their structures and absolute configurations were assigned by extensive spectroscopic analyses and quantum calculation methods. Compounds 1 and 2 showed potent inhibitory activity against LPS-induced nitric oxide production in RAW 264.7 macrophages, compared with the positive control L-NMMA. In addition, compounds 1 and 2 were also evaluated for their antioxidant (DPPH• and ABTS•+) and xanthine oxidase (XO) inhibitory activities, and they exhibited weak inhibitory effects at 100 µM.

The chemistry and pharmacology of Ligularia przewalskii: A review.

ETHNOPHARMACOLOGICAL RELEVANCE: Ligularia przewalskii (Maxim.) Diels (LP) (called zhangyetuowu in Chinese), is generally found in moist forest areas in the western regions of China. The root, leaves and flower of LP are utilized as a common traditional medicine in China. It has been utilized conventionally in herbal remedies for the remedy of haemoptysis, asthma, pulmonary phthisis, jaundice hepatitis, food poisoning, bronchitis, cough, fever, wound healing, measles, carbuncle, swelling and phlegm diseases. AIM OF THE STUDY: The review aims to provide a systematic summary of LP and to reveal the correlation between the traditional uses and pharmacological activities in order to provide updated, comprehensive and categorized information and identify the therapeutic potential for its use as a new medicine. MATERIALS AND METHODS: The relevant data were searched by using the keywords "Ligularia przewalskii" "phytochemistry", "pharmacology", "Traditional uses", and "Toxicity" in "Scopus", "Scifinder", "Springer", "Pubmed", "Wiley", "Web of Science", "China Knowledge Resource Integrated databases (CNKI)", "Ph.D." and "M.Sc. dissertations", and a hand-search was done to acquire peer-reviewed articles and reports about LP. The plant taxonomy was validated by the databases "The Plant List", "Flora Reipublicae Popularis Sinicae", "A Collection of Qinghai Economic Plants", "Inner Mongolia plant medicine Chi", Zhonghua-bencao and the Standard of Chinese herbal medicine in Gansu. RESULTS: Based on the traditional uses, the chemical nature and biological effects of LP have been the focus of research. In modern research, approximately seventy-six secondary metabolites, including thirty-eight terpenoids, nine benzofuran derivatives, seven flavonoids, ten sterols and others, were isolated from this plant. They exhibit anti-inflammatory, antioxidative, anti-bacterial and anti-tumour effects, and so on. Currently, there is no report on the toxicity of LP, but hepatotoxic pyrrolizidine alkaloids (HPA) were first detected with LC/MSn in LP, and they have potential hepatotoxicity. CONCLUSIONS: The lung-moistening, cough-relieving and phlegm-resolving actions of the root of LP are attributed to the anti-inflammatory properties of flavonoids and terpenoids. The heat-clearing, dampness-removing and gallbladder-normalizing (to cure jaundice) actions of the flowers of LP are based on the anti-inflammatory, antioxidant and hepatoprotective activity properties of terpenoids, flavonoids and sterols. The Traditional Chinese Medicine (TCM) characteristics of LP (bitter flavour) corroborate its potent anti-inflammatory effects. In addition, the remarkable anti-inflammatory and antioxidant capacities of LP contribute to its anti-tumour and antitussive activities. Many conventional uses of LP have now been validated by modernized pharmacological research. For future research, further phytochemical and biological studies need to be conducted on LP, In particular, the safety, mechanism of action and efficacy of LP could be of future research interest before beginning clinical trials. More in vivo experiments and clinical studies are encouraged to further clarify the relation between traditional uses and modern applications. Regarding the roots, leaves and flowers of LP, their chemical compositions and clinical effects should be compared. The information on LP will be helpful in providing and identifying its therapeutic potential and economic value for its use as a new medicine in the future.

Pheophytin analogues from the medicinal lichen Usnea diffracta.

A new pheophytin, (132S, 17S, 18S)-132-hydroxy-20-chloro-ethylpheophorbide a (3), along with two known analogues (1-2) were isolated from the lichen Usnea diffracta Vainio (Parmeliaceae). Among them, compound 3 was a rare C-20-chloro type pheophytin obtained from lichens. Their structures were elucidated by extensive spectroscopic analysis, and all the compounds were obtained for the first time from U. diffracta. Compounds (1-3) were evaluated for their xanthine oxidase (XO) inhibitory activities in vitro, and the results showed that 1-3 possessed significant enzyme inhibitory actions with IC50 values of 46.9 ± 3.8, 75.9 ± 7.4 and 42.1 ± 1.7 µg/mL, respectively.

[Chemical structure of cyperotundic acid from rhizomes of Cyperus rotundus].

Thirteen compounds were isolated from the ethyl acetate extract of the rhizomes of Cyperus rotundus(Xiangfu) by means of various chromatographic techniques(silica gel, Al2O3, Sephadex LH-20, MCI GEL CHP-20P and HPLC), and their structures were identified as cyperotundic acid(1),(4S, 5E, 10R)-7-oxo-trinoreudesm-5-en-4ß-ol(2), 4-hydroxy-4, 7-dimethyl-1-tetralone(3), taraxerone(4), dammaradienyl acetate(5), zeorin(6), sarmentine(7), guineensine(8), pellitorine(9), caprolactam(10), liriodendrin(11), 3-hydroxy-1-(4-hydroxy-3,5-dimethoxyphenyl)-2-[4-(3-hydroxy-1-(E)-propenyl)-2,6-dimethoxyphenoxy]propyl-ß-D-glucopyranoside(12)and 1-(3, 4-methylenedioxyphenyl)-1E-tetradecene(13) by extensive spectroscopic analyses(IR, MS, 1D-and 2D-NMR). Compound 1 was a new rearranged sesquiterpene and named as cyperotundic acid, which did not obey the isoprene rule.Compounds 2-13 were obtained from the genus Cyperus for the first time.

Promotion of regulatory T cell induction by immunomodulatory herbal medicine licorice and its two constituents.

Regulatory T cells (Treg) play a critical role to control immune responses and to prevent autoimmunity, thus selective increase of Treg cells in vivo has broad therapeutic implications for autoimmune and inflammatory diseases. Licorice is a well-known herbal medicine used worldwide for over thousands of years, and accumulating evidence has shown its immunomodulatory potential. However, it is not clear whether licorice could regulate the induction and function of Treg cells. Here we found licorice extract could promote Treg cell induction, and then we used a rational approach to isolate its functional fractions and constituents. The results showed that two constituents, isoliquiritigenin and naringenin, promoted Treg cell induction both in vitro and in vivo. The effective fractions and two constituents of licorice also enhanced immune suppression of Treg cells, and they further reduced severity of DSS-induced colitis in mice. This study suggested that promotion of regulatory T cell induction could be an underlying mechanism of the historically and widely used herbal medicine licorice, providing its two effective molecules against autoimmune and inflammatory diseases.

Paeoveitols A-E from Paeonia veitchii.

Paeoveitols A-E (1-5), involving three monoterpenes and two benzofuran constituents, were isolated from Paeonia veitchii. Their structures were determined based on extensive spectral analyses (IR, UV, MS, 1D and 2D NMR), and the absolute configuration of compound 1 was confirmed by single-crystal X-ray diffraction. By the agitating human melatonin receptor 1 (MT1) assay on HEK293 cell line in vitro, compound 4 showed weak activity with the agitation rate of 22.52% at the concentration of 1.79 mM.

Lignans from the Fruits of Melia toosendan and Their Agonistic Activities on Melatonin Receptor MT1.

Investigation on the fruits of Melia toosendan afforded seven new lignans (1-7), along with seventeen known compounds (8-24). The structures of the new compounds, involving four neo-lignans (1-4), two sesquilignans (5-6), and a nor-lignan (7), were elucidated based on extensive spectroscopic analyses (high-resolution electrospray ionization mass spectra, ultraviolet, infrared, one-dimensional and two-dimensional nuclear magnetic resonance). Compound 24 exhibited activity on melatonin receptor type 1 with an agonistic rate of 57.77% at 1.02 mM according to the assay on HEK293 cell lines in vitro.

Bioactivity-guided isolation of anti-hepatitis B virus active sesquiterpenoids from the traditional Chinese medicine: Rhizomes of Cyperus rotundus.

ETHNOPHARMACOLOGICAL RELEVANCE: The rhizome of Cyperus rotundus (C. rotundus) is a well-known traditional Chinese medicine to cure hepatitis in many formulae, but the active components responsible for hepatitis have not been elucidated. According to our bioassay on HepG2.2.15 cell line in vitro, the ethanol extract of C. rotundus demonstrated potent anti-HBV activity. This current study was designed to isolate and identify the anti-HBV active constituents from the rhizomes of C. rotundus. MATERIAL AND METHODS: Bioactivity and LC-MS guided fractionation on the extract of C. rotundus using various chromatographic techniques including open-column, Sephadex LH-20 and semi-preparative high performance liquid chromatography led to the isolation and identification of thirty-seven sesquiterpenoids. Structural elucidation of the isolates was carried out by extensive spectroscopic analyses (UV, IR, HRMS, 1D- and 2D -NMR). The anti-HBV activity and cytotoxicity were evaluated on the HBV-transfected HepG2.2.15 cell line in vitro. The cytotoxicity effects of the isolates were assessed by a MTT assay. The secretions of HBsAg and HBeAg in the culture medium were detected by ELISA method, and the load of HBV DNA was quantified by real-time fluorescent PCR technique. RESULTS: Five new patchoulane-type sesquiterpenoids, namely cyperene-3, 8-dione (1), 14-hydroxy cyperotundone (2), 14-acetoxy cyperotundone (3), 3ß-hydroxycyperenoic acid (4) and sugetriol-3, 9-diacetate (5), along with 32 known sesquiterpenoids were isolated from the active fractions of C. rotundus. Compounds 2 and 3 were the first cyperotundone-type sesquiterpenoids with a hydroxyl group at C-14 position. Nine eudesmane-type sesquiterpenoids (15-21 and 23-24) significantly inhibited the HBV DNA replication with IC50 values of 42.7±5.9, 22.5±1.9, 13.2±1.2, 10.1±0.7, 14.1±1.1, 15.3±2.7, 13.8±0.9, 19.7±2.1 and 11.9±0.6 µM, respectively, of which, compounds 17, 21, 23 and 24 possessed high SI values of 250.4, 125.5,>259.6 and 127.5, respectively. Two patchoulane-type sesquiterpenoids (4 and 7) effectively suppressed the secretion of HBsAg in a dose-dependent manner with IC50 values of 46.6±14.3 (SI=31.0) and 77.2±13.0 (SI=1.7) µM, respectively. Compounds 2, 8, 12, 15, 17 and 25 possessed moderate activities against HBeAg secretion with IC50 values of 162.5±18.9 (SI=13.3), 399.2±90.0 (SI=10.6), 274.7±70.8 (SI=5.2), 313.9±87.5 (SI=7.2), 334.0±70.4 (SI=9.9) and 285.3±20.9 (SI=15.5) µM, respectively. CONCLUSIONS: This is the first study to reveal the anti-HBV constituents of C. rotundus, demonstrating that the eudesmane-type sesquiterpenoids might contribute to the anti-HBV activity of the rhizomes of C. rotundus.