Three New Constituents with Anti-Inflammatory and Antimicrobial Activities in Vitro from the Roots of Capsicum annuum L.

Three new compounds, including two new sesquiterpenes (1-2), named Annuumine E-F, and one new natural product, 3-hydroxy-2,6-dimethylbenzenemethanol (3), together with seventeen known compounds (4-20) were isolated from the ethanol extract of the roots of Capsicum annuum L. Among them, five compounds (4, 5, 9, 10 and 20) were isolated from this plant for the first time. The structures of new compounds (1-3) were determined via detailed analysis of the IR, HR-ESI-MS and 1D and 2D NMR spectra. The anti-inflammatory activities of the isolated compounds were evaluated by their ability to reduce NO release by LPS-induced RAW 264.7 cells. Notably, compound 11 exhibited moderate anti-inflammatory activity (IC50 =21.11 µM). Moreover, the antibacterial activities of the isolated compounds were also evaluated.

Decryption of Active Constituents and Action Mechanism of the Traditional Uighur Prescription (BXXTR) Alleviating IMQ-Induced Psoriasis-Like Skin Inflammation in BALB/c Mice.

Bai Xuan Xia Ta Re Pian (BXXTR) is a traditional Uighur medicine ancient prescription in China widely used in the treatment of psoriasis, presenting a high curative rate and few side effects. Given that the active constituents and action mechanism still remain unclear, the aim of this study is to explore the potential active constituents and mechanism of antipsoriasis of BXXTR. Psoriasis-like lesions model in BALB/c mice was induced by Imiquimod (IMQ), including five treatment groups: control group, IMQ-treated group, IMQ-ACITRETIN group (Positive control group), IMQ-BXXTR low dose group, IMQ-BXXTR medium dose group and IMQ-BXXTR high dose group. The Psoriasis Area and Severity Index (PASI) score, skin and ear thickness, and histologic section were collected. The differentially expressed genes were determined by using RNAseq technology and the relevant pathways were analyzed by KEGG database. The ELISA kit and western blot assays were used to detect the related protein expression levels. In addition, the chemical constituents of BXXTR were determined by UPLC-TOF-MS analysis and the potential active constituents were predicted by SEA DOCK and Gene Ontology (GO). The data demonstrated that BXXTR significantly alleviated IMQ-induced psoriasis. RNA-seq analysis showed that BXXTR induced the expression levels of 31 genes; the KEGG analysis suggested that BXXTR could significantly change IL-17-related inflammatory pathways. The ELISA kit confirmed that the expression level of IL-17A protein was significantly reduced. 75 compounds of BXXTR were determined by UPLC-TOF-MS analysis, 11 of 75 compounds were identified as potential active compounds by similarity ensemble approach docking (SEA DOCK) and Gene Ontology (GO). BXXTR reduced the severity of skin lesions by inhibiting IL-17-related inflammatory pathways. The results indicated that BXXTR could suppress psoriasis inflammation by multiple-constituents-regulated multiple targets synergistically. Collectively, this study could provide important guidance for the elucidation of the active constituents and action mechanism of BXXTR for the treatment of psoriasis.

[Regional characteristic analysis of alkaloids and chlorogenic acid in wild Phellodendri Amurensis Cortex].

In the present research, 674 wild medicinal material samples of Phellodendri amurensis Cortex were collected from 31 sampling sites in the whole distribution of its original plant Phellodendron amurense. The samples were collected under the premise that the stem diameter of sampling plant, sampling position and time were controlled. And the sampling sites were set at the interval of a latitude. The content of 6 kinds of active ingredients, palmatine chloride, berberine hydrochloride, phellodendrine chloride, jatrorrhizine hydrochloride, magnoflorine, chlorogenic acid, etc in the medicinal material samples were determined, and the results showed that the content of most active ingredients in the medicinal materials showed significant differences due to the difference of sampling sites. Among them, the medicinal materials from Liaoning region had the highest content of active ingredients, followed by Beijing and Jilin regions, and that from Heilongjiang region had the lowest content. The study has important directive significance to the exploration of environmental factors for the formation of active constituent and artificial planting regionalization of high quality Phellodendri amurensis Cortex.

Dillenia species: A review of the traditional uses, active constituents and pharmacological properties from pre-clinical studies.

CONTEXT: Dillenia (Dilleniaceae) is a genus of about 100 species of flowering plants in tropical and subtropical trees of Southern Asia, Australasia, and the Indian Ocean Islands. Until now, only eight Dillenia species have been reported to be used traditionally in different countries for various medical purposes. Out of eight species, D. pentagyna (Roxb), D. indica (Linn.) and D. suffruticosa (Griffith Ex. Hook. F. & Thomsom Martelli) have been reported to be used to treat cancerous growth. OBJECTIVE: The present review explored and provided information on the therapeutic potential of Dillenia species. METHODS: Comprehensive and relevant literature on the therapeutic potential of Dillenia species was gathered through electronic databases including Google Scholar, Scopus, PubMed, and books, without limiting the dates of publication. RESULTS AND CONCLUSION: The review demonstrated that only a few Dillenia species have been proven scientifically for their therapeutic potential in pre-clinical studies, including D. pentagyna, D. indica, D. papuana (Martelli), D. meliosmifolia (Hook. F. Ex. Thomsom) and D. suffruticosa (Griffith Ex Hook. F. & Thomson). A few species of Dillenia have undergone isolation and characterization of compounds with lupeol and betulinic acids having tremendous pharmacological potential. Dillenia species warrant further studies on their therapeutic potential, which may eventually lead to the development of new drug candidates for treatment of various diseases.

Integrating Network Pharmacology and Molecular Docking Approach to Elucidate the Mechanism of Commiphora wightii for the Treatment of Rheumatoid Arthritis.

Background: Rheumatoid arthritis (RA) is considered a notable prolonged inflammatory condition with no proper cure. Synovial inflammation and synovial pannus are crucial in the onset of RA. The "tumor-like" invading proliferation of new arteries is a keynote of RA. Commiphora wightii (C wightii) is a perennial, deciduous, and trifoliate plant used in several areas of southeast Asia to cure numerous ailments, including arthritis, diabetes, obesity, and asthma. Several in vitro investigations have indicated C wightii's therapeutic efficacy in the treatment of arthritis. However, the precise molecular action is yet unknown. Material and methods: In this study, a network pharmacology approach was applied to uncover potential targets, active therapeutic ingredients and signaling pathways in C wightii for the treatment of arthritis. In the groundwork of this research, we examined the active constituent-compound-target-pathway network and evaluated that (Guggulsterol-V, Myrrhahnone B, and Campesterol) decisively donated to the development of arthritis by affecting tumor necrosis factor (TNF), PIK3CA, and MAPK3 genes. Later on, docking was employed to confirm the active components' efficiency against the potential targets. Results: According to molecular-docking research, several potential targets of RA bind tightly with the corresponding key active ingredient of C wightii. With the aid of network pharmacology techniques, we conclude that the signaling pathways and biological processes involved in C wightii had an impact on the prevention of arthritis. The outcomes of molecular docking also serve as strong recommendations for future research. In the context of this study, network pharmacology combined with molecular docking analysis showed that C wightii acted on arthritis-related signaling pathways to exhibit a promising preventive impact on arthritis. Conclusion: These results serve as the basis for grasping the mechanism of the antiarthritis activity of C wightii. However, further in vivo/in vitro study is needed to verify the reliability of these targets for the treatment of arthritis.

Comprehensive assessment of Zingiber sianginensis: Phytometabolomic analysis and its impact on oxidative stress biomarkers.

In India, ginger is highly valued for cultural and medicinal purposes. Besides traditional uses, ginger has been proven for its efficacy in cancer, chemotherapy-induced nausea, bacterial infections, neuroinflammation, and oxidative stress. This study focuses on Zingiber sianginensis, a rare ginger species in the Siang region of Arunachal Pradesh, India. This study studied pharmacognostical evaluation, phytometabolomics analysis, and its effect on oxidative stress biomarkers. Microscopic and chemical tests were employed for pharmacognostical evaluation, revealing distinctive characteristics of Zingiber sianginensis, such as non-close collateral vascular bundles and unique cork layers. Chemical tests, including the phloroglucinol and hydrochloric acid test, differentiated Zingiber sianginensis from Zingiber officinale Roscoe. Phytometabolomics analysis, using Gas Chromatography-Mass Spectrometry (GC/MS) and Liquid Chromatography-Electrospray Ionisation-Quadrupole Time of Flight-Mass Spectrometry (LC-ESI-QTOF-MS/MS) techniques, identified a diverse range of metabolites in Zingiber sianginensis, including polyphenols, monoterpenoids, diterpenoids, sesquiterpenoids, and organic compounds. The LC-ESI-QTOF-MS/MS analysis revealed 158 compounds, verified through cross-referencing with established databases. Heavy metal analysis by Inductively Coupled Plasma-Mass Spectrometry (ICP-MS) confirmed that Zingiber sianginensis complies with safety standards, showing concentrations of heavy metals within acceptable limits. The isolation and characterization of compounds from Zingiber sianginensis identified natural products such as (R)-(-)- alpha-Curcumene (1), 1-Dehydro-[10]-gingerdione (2), 6-Shogaol (3), and 6-Gingerol (4). Quantification of 6-gingerol revealed that Zingiber sianginensis contains approximately twice the amount compared to Zingiber officinale Roscoe's, suggesting its potential as a source for higher 6-gingerol content. The hydroalcoholic extract of Zingiber sianginensis exhibited antioxidant properties, reducing oxidative stress biomarkers in human dermal fibroblast cells treated with rotenone. Allantoin and 3-bromotyrosine levels significantly decreased, indicating the extract's potential in combating oxidative stress-related disorders. Overall, this comprehensive study provides valuable insights into the pharmacognostical, phytometabolomic, and safety aspects of Zingiber sianginensis, highlighting its potential as a source of bioactive compounds with health benefits.

The potential of Valeriana as a traditional Chinese medicine: traditional clinical applications, bioactivities, and phytochemistry.

Valeriana plants are members of the Caprifoliaceae family, which include more than 200 species worldwide. We summarized previous reports on traditional clinical applications, bioactivities, and phytochemistry of Valeriana by searching electronic databases of Science Direct, Web of Science, PubMed, and some books. Some Valeriana species have been used as traditional medicines, demonstrating calming fright and tranquilizing mind, promoting Qi and blood, activating blood circulation and regulating menstruation, dispelling wind and eliminating dampness, regulating Qi-flowing to relieve pain, and promoting digestion and checking diarrhea, and treating diseases of the nervous, cardiovascular, and digestive systems, inflammation, gynecology, and others. Pharmacology studies revealed the effects of Valeriana, including sedative, hypnotic, antispasmodic, analgesic, antidepressant, anxiolytic, anticonvulsant, antiepileptic, neuroprotective, antibacterial, antiviral, cytotoxic, and antitumor effects as well as cardiovascular and cerebrovascular system improvements. More than 800 compounds have been isolated or identified from Valeriana, including iridoids, lignans, flavonoids, sesquiterpenoids, alkaloids, and essential oils. Constituents with neuroprotective, anti-inflammatory, cytotoxic, and sedative activities were also identified. However, at present, the developed drugs from Valeriana are far from sufficient. We further discussed the pharmacological effects, effective constituents, and mechanisms directly related to the traditional clinical applications of Valeriana, revealing that only several species and their essential oils were well developed to treat insomnia. To effectively promote the utilization of resources, more Valeriana species as well as their different medicinal parts should be the focus of future related studies. Clinical studies should be performed based on the traditional efficacies of Valeriana to facilitate their use in treating diseases of nervous, cardiovascular, and digestive systems, inflammation, and gynecology. Future studies should also focus on developing effective fractions or active compounds of Valeriana into new drugs to treat diseases associated with neurodegeneration, cardiovascular, and cerebrovascular, inflammation and tumors. Our review will promote the development and utilization of potential drugs in Valeriana and avoid wasting their medicinal resources.

Herbal Medicine in Ischemic Stroke: Challenges and Prospective.

Herbal medicines, mainly of plant source, are invaluable source for the discovery of new therapeutic agents for all sorts of human ailments. The complex pathogenesis of stroke and multifactorial effect of herbal medicine and their active constituents may suggest the promising future of natural medicine for stroke treatment. Anti-oxidant, anti-inflammatory, anti-apoptotic, neuroprotective and vascular protective effect of herbal medicines are believed to be efficacious in stroke treatment. Herbs typically have fewer reported side effects than allopathic medicine, and may be safer to use over longer period of time. Herbal medicines are believed to be more effective for the longstanding health complaints, such as stroke. Several medicinal plants and their active constituents show the promising results in laboratory research. However failure in transformation of laboratory animal research to the clinical trials has created huge challenge for the use of herbal medicine in stroke. Until and unless scientifically comprehensive evidence of the efficacy and safety of herbal medicine in ischemic stroke patients is available, efforts should be made to continue implementing treatment strategies of proven effectiveness. More consideration should be paid to natural compounds that can have extensive therapeutic time windows, perfect pharmacological targets with few side effects. Herbal medicine has excellent prospective for the treatment of ischemic stroke, but a lot of effort should be invested to transform the success of animal research to human use.

Essential Oil from Sweet Potato Vines, a Potential New Natural Preservative, and an Antioxidant on Sweet Potato Tubers: Assessment of the Activity and the Constitution.

Pathogenic fungi and oxidation are the major factors that cause the deterioration of sweet potatoes and also cause the loss of quality that makes consumption unsafe. In the present study, the in vitro results demonstrate that the essential oil from sweet potato vines exhibits significantly enhanced activity compared to that of the control. Furthermore, the essential oil can actively inhibit the growth of some common microorganisms inducing pathogenic bacteria and fungi (inhibition rates above 50% at low concentrations). A total of 31 constituents were identified using GC-MS and confirmed that linalool and p-hydroxybenzoic acid are the major active ingredients. The experiment involving actual tubers showed that the essential oil could retains its quality and effectiveness again the fungus disease. This suggests that it could be used in the food industry to increase the shelf life of stored produce (tubers) to ensure food safety without the use of additives or preservatives.

Characterization and flocculability of a novel proteoglycan produced by Talaromyces trachyspermus OU5.

A filamentous fungus strain OU5 was isolated from a soil sample for its ability to produce rich exopolymers (EPS), with high flocculation capability towards kaolin suspension and swine wastewater, at low-carbon source conditions. EPS from strain OU5 was extracted and characterized to determine its flocculating behavior and active constituents involved in the flocculation. Strain OU5 was identified as Talaromyces trachyspermus by 18S rDNA-ITS gene sequencing and morphological observation. The extracted EPS was a novel proteoglycan (designated as BF-OU5) composed of 84.6% (w/w) polysaccharides and 15.2% (w/w) proteins. The enzymatic digestion tests revealed that the polysaccharides in BF-OU5, composed of 67% glucose, 16.4% mannose, 8.6% xylose and 8% galactose, contributed to 99.7% of flocculating capacity and were the major active ingredients in the flocculation. By contrast, the proteins in BF-OU5 only had minor roles in the flocculation. The presence of hydroxyl, amide, carboxyl and methoxyl functional groups in BF-OU5, and the high molecular weight (1.053 × 10(5)-2.970 × 10(5) Da) as well as the structure of a spherical conformation with inner pores and channels made of cross-linked netted textures contributed to the flocculation. A dosage of 20 mg/l BF-OU5 initiated more than 92.5% of flocculating efficiency towards kaolin suspension without any added coagulants; its flocculability was stable over a wide range of pH (4.0-8.0) and temperature (20°C-100°C). Treatment of swine wastewater using BF-OU5 achieved 52.1% flocculating removal for chemical oxygen demand, 39.7% for Kjeldahl nitrogen, 18.6% for NH4(+)-N, 21.5% for total phosphorus, and 75% for turbidity.

Recent developments in the field of the determination of constituents of TCMs in body fluids of animals and human.

Although traditional Chinese medicines (TCMs) play important role in drug discovery and human health, the actual value of TCMs has not been fully recognized worldwide due to its complex components and uncontrollable quality. For the modernization and globalization of TCMs, it is important to establish selective, sensitive and feasible analytical methods for determination and quantification of bioactive components of TCMs in body fluids primarily due to the low concentration, the complex nature of the biological matrices, and multi-components and their metabolites present in biological fluids. The present review summarizes the current extraction techniques, chromatographic separation and spectroscopic (especially mass spectrometric) analysis methods and new trends on the analysis of bioactive components and metabolites of TCMs in biological fluids. In addition, the importance of establishment of pharmacokinetics and bioavailability profiles and simultaneous determination of multi-active components in TCMs is discussed to provide proper examples of analytical methods for pharmacological and clinical studies of TCMs.

In vitro anti-angiogenesis effects and active constituents of the saponin fraction from Gleditsia sinensis.

BACKGROUND: The anomalous fruits of Gleditsia sinensis Lam. (Leguminosae), a crude drug in China, have long been used in traditional Chinese medicine for the treatment of various diseases. The saponin fraction isolated from the fruits (SFGS) is considered as the active component for the antitumor activity of this crude drug. OBJECTIVES: The present study was performed to investigate the anti-angiogenesis activities and active constituents of SFGS. METHODS: Human umbilical vein endothelial cells (HUVECs) were treated with SFGS in the presence or absence of basic fibroblast growth factor (bFGF) in vitro. The proliferation, migration, and tube formation were studied by MTT, Transwell, and 2D Matrigel assays, respectively. The cell cycle and apoptosis were analyzed by flow cytometry. Enzyme-linked immunosorbent assay for protein expression of vascular endothelial growth factor (VEGF) and western blot analysis for caspase-3, caspase-8, and caspase-9 as well as Fas were performed. In addition, the effects of 13 saponin compounds isolated from SFGS on the tube formation of HUVECs were screened, and the structure-activity relationships were discussed. RESULTS: SFGS, at concentrations (1, 3, and 10 µg/mL) without significant cytotoxicity on endothelial cells, significantly inhibited the proliferation, migration, and tube formation of HUVECs induced by bFGF (10 ng/mL). It moderately arrested the cell cycle to G1 phase but greatly induced cell apoptosis and increased the expressions of caspases-3, caspase-8, and Fas but not caspase-9 in HUVECs. Moreover, SFGS did not affect the bFGF-induced autosecretion of VEGF from endothelial cells. Among the 13 saponin compounds tested, gleditsiosides B, I, J, O, and Q showed inhibition of the tube formation at a concentration of 3 µM, and only gleditsioside B exerted significant inhibition at 1 µM. CONCLUSION: SFGS is substantially able to prevent angiogenesis by interfering with multiple steps. The findings provide a new explanation for the antitumor effects of G sinensis fruits. Gleditsiosides B, I, J, O, and Q are probably the main active constituents of SFGS.