[Study on changes of Styrax varieties].

Styrax is a commonly used imported traditional Chinese medicinal material in China. It was introduced to China in the Han Dynasty and was first described as a traditional Chinese medicine in Miscellaneous Records of Famous Physicians(Ming Yi Bie Lu). In this paper, by combing ancient and modern Chinese and foreign herbal medicine books and modern literature, combined with the results of field investigations on the origin of Styrax, the changes of Styrax involving the name, quality evaluation, origin, place of origin, and harvesting and processing were systematically verified. The results show that since ancient times, the origin and place of origin of Styrax have been unclear. The medical scientists of all dynasties in China have evaluated the quality of Styrax from four aspects: texture, viscosity, odor concentration, and color. The varieties of Styrax changed twice. The first change may have occurred during the Sui and Tang Dynasties, and the base changed from Styrax officinalis to Liquidambar orientalis. The second change was in modern times, and the base changed from L. orientalis to L. styraciflua. At the same time, the place of origin changed for the first time, from Turkey, Syria, and other countries in southern Asia Minor to Honduras, Guatemala, and other countries in Central America and southern North America. This paper studied the historical evolution of Styrax in terms of quality evaluation, origin, place of origin, character, and harvesting and processing. At the same time, it summarized the application of Styrax in the western countries, which can provide a historical basis for the further development and utilization of Styrax.

Behavioral Prevention, Treatment, and Rehabilitation of Using Western and Chinese Medicines or Herbal Products among the Public in Response to COVID-19 in Hong Kong: A Cross-Sectional Study.

The coronavirus disease 2019 (COVID-19) pandemic occurred in Hong Kong for more than two years. This article conducted a cross-sectional study for participants to investigate the behavioral prevention, treatment, and rehabilitation of using Western medicines or herbal products for COVID-19 in Hong Kong. A questionnaire was designed and performed over 2 weeks from 1 May to 15 May 2022. It consisted of five parts with around 20 questions conducted including sociodemographic information, prevention, treatment, rehabilitation of COVID-19, and also the sources of information. The pattern usage of Chinese or Western medicines for COVID-19 was studied after data collection. 318 people participated in this survey, and only 311 were qualified. The sociodemographic information, e.g., personal educational level, and behavior for the prevention of COVID-19, which included wearing masks (98.7%), using alcohol hand sanitizer (83.0%), washing hands frequently (82.4%), avoiding crowds (53.1%), and staying home more often (50.6%). Western medicines, such as antipyretic drugs, antitussive drugs, and pain reliever drugs, whilst Chinese medicines, such as Lianhua Qingwen Jiaonang, Huoxiang Zhengqi San or Wan, and Nin Jiom Pei Pa Koa, were most commonly used in the treatment and rehabilitation periods of COVID-19. Herbal products, including lemon, honey, ginger, and herbal tea, were used as a daily diet to fight against COVID-19. Based on the result findings, Chinese medicines or herbal products were used during the COVID-19 pandemic, but most of the participants used an unknown Chinese medicine practitioner's prescription and self-administered Chinese medicine. The pattern of Chinese medicines and Western medicines' usage in the prevention, treatment, and rehabilitation of COVID-19 was also investigated; this showed a statistically significant association between the variables according to gender, age, and Chinese or Western medicines for further investigation.

Impacts of sulfur fumigation on the chemistry and immunomodulatory activity of polysaccharides in ginseng.

Ginseng is widely regarded as a panacea in Oriental medicine mainly due to its immunomodulatory activity. We previously found that sulfur fumigation, a commonly used pesticidal and anti-bacterial processing practice, weakened the immunomodulatory activity of ginseng. However, if and how sulfur fumigation affects the polysaccharides in ginseng, the crucial components contributing to the immunomodulatory function, remain unknown. Here we report that polysaccharides extracted from sulfur-fumigated ginseng (SGP) presented different chemical properties with polysaccharides extracted with non-fumigated ginseng (NGP), particularly increased water extraction yield and decreased branching degree. SGP had weaker immunomodulatory activity than NGP in immunocompromised mice, as evidenced by less improved immunophenotypes involving body weight, immune organ indexes, white blood cells, lymphocyte cell populations and inflammation. The different immunomodulatory activities were accompanied by changes in the interaction between the polysaccharides and gut microbiota, in which SGP stimulated the growth of different bacteria but produced less SCFAs as compared to NGP. Fecal microbiota transplantation experiment suggested that gut microbiota played a central role in causing the weakened immunomodulatory activity in vivo. This study provides definite evidence that sulfur fumigation affects the chemistry and bioactivity of ginseng polysaccharides, thereby contributing to understanding how sulfur fumigation weakens the immunomodulatory activity of ginseng.

Impact of Sulfur Fumigation on the Chemistry of Dioscoreae Rhizoma (Chinese Yam).

Dioscoreae Rhizoma (Chinese yam; derived from the rhizome of Dioscorea opposita Thunb.) (DR), commonly consumed as a food or supplement, is often sulfur-fumigated during post-harvest handling, but it remains largely unknown if and how sulfur fumigation impacts the chemistry of DR. In this study, we report the impact of sulfur fumigation on the chemical profile of DR and then the molecular and cellular mechanisms potentially involved in the chemical variations induced by sulfur fumigation. The results show that sulfur fumigation significantly and specifically changed the small metabolites (molecular weight lower than 1000 Da) and polysaccharides of DR at both qualitative and quantitative levels. Multifaceted molecular and cellular mechanisms involving chemical transformations (e.g., acidic hydrolysis, sulfonation, and esterification) and histological damage were found to be responsible for the chemical variations in sulfur-fumigated DR (S-DR). The research outcomes provide a chemical basis for further comprehensive and in-depth safety and functional evaluations of sulfur-fumigated DR.

[Specific DNA barcodes, germplasm resources, and genetic diversity of Eleutherococcus senticosus].

Eleutherococcus senticosus is one of the Dao-di herbs in northeast China. In this study, the chloroplast genomes of three E. senticosus samples from different genuine producing areas were sequenced and then used for the screening of specific DNA barcodes. The germplasm resources and genetic diversity of E. senticosus were analyzed basing on the specific DNA barcodes. The chloroplast genomes of E. senticosus from different genuine producing areas showed the total length of 156 779-156 781 bp and a typical tetrad structure. Each of the chloroplast genomes carried 132 genes, including 87 protein-coding genes, 37 tRNAs, and 8 rRNAs. The chloroplast genomes were relatively conserved. Sequence analysis of the three chloroplast genomes indicated that atpI, ndhA, ycf1, atpB-rbcL, ndhF-rpl32, petA-psbJ, psbM-psbD, and rps16-psbK can be used as specific DNA barcodes of E. senticosus. In this study, we selected atpI and atpB-rbcL which were 700-800 bp and easy to be amplified for the identification of 184 E. senticosus samples from 13 genuine producing areas. The results demonstrated that 9 and 10 genotypes were identified based on atpI and atpB-rbcL sequences, respectively. Furthermore, the two barcodes identified 23 genotypes which were named H1-H23. The haplotype with the highest proportion and widest distribution was H10, followed by H2. The haplotype diversity and nucleotide diversity were 0.94 and 1.82×10~(-3), respectively, suggesting the high genetic diversity of E. senticosus. The results of the median-joining network analysis showed that the 23 genotypes could be classified into 4 categories. H2 was the oldest haplotype, and it served as the center of the network characterized by starlike radiation, which suggested that population expansion of E. senticosus occurred in the genuine producing areas. This study lays a foundation for the research on the genetic quality and chloroplast genetic engineering of E. senticosus and further research on the genetic mechanism of its population, providing new ideas for studying the genetic evolution of E. senticosus.

Application of the pedicle axis view in percutaneous screw placement for type III fracture dislocation of the sacroiliac joint.

AIM: To investigate the clinical application of axial view projection of the pedicle in percutaneous screw placement for type III fracture dislocation of the sacroiliac joint. METHODS: Percutaneous sacroiliac screw fixation was performed in 29 patients with type III sacroiliac joint fractures under X-ray fluoroscopy (C-arm) using axial view projection of the pedicle after preoperative traction reduction and preoperative preparation. The study included 19 males and 10 females, aged 20 to 75 years old, with a mean age of 42.1 ± 3.4 years. RESULTS: The total operative time ranged between 44 and 135 min, with a mean of 95.5 ± 9.4 min. The intraoperative fluoroscopy time ranged between 15 and 42 s, with a mean of 25 ± 4.7 s. The intraoperative blood loss ranged between 5 and 10 ml, with a mean of 7.1 ± 1.3 ml. According to the Matta scoring system, excellent outcomes were achieved in 25 cases, whereas good outcomes were achieved in 4 cases. Based on the definition by Neo et al., pedicle screw positions were categorized into four grades: grade 0 (33 screws), grade I (2 screws), grade II (2 screws), and grade III (0 screws). Excellent outcomes were achieved in 94.6% of Grade 0 and I screws. According to Majeed's functional score, 21 cases achieved excellent outcomes, whereas 8 cases achieved good outcomes. The 29 patients were followed between 3 and 18 months, with a mean of 7.1 ± 1.2 months. All patients achieved anatomical reduction with accurate screw placement and successful healing of their fractures, with no cases of bone penetration or neurovascular injury. CONCLUSION: Axial view imaging of the pedicle using fluoroscopy is a convenient and rapid fluoroscopy method for percutaneous screw placement for type III fracture dislocation of the sacroiliac joint, with a high rate of success, good safety, and short fluoroscopy time.

A review on the plant resources of important medicinal licorice.

ETHNOPHARMACOLOGICAL RELEVANCE: Glycyrrizae Radix et Rhizoma has various effects, including tonifying the spleen and qi, clearing heat and toxic substances, eliminating phlegm, relieving cough and pain, and harmonizing the effects of other medicines. It is widely used in the pharmaceutical and food industries. AIMS OF THE STUDY: This review systematically collates the identification of Glycyrrhiza Linn. species with medicinal value and their distributions. The morphological and genetic characteristics, distribution, quantity of reserves in China, suitable environment, and area of suitable habitat of important medicinal species were reviewed. The effects of the natural environment and cultivation management (water and nutrients) on the growth and quality of licorice were reviewed. The aim is to make people have a systematic understanding of the status of medicinal plant resources of the G. Linn., and understand the natural and human factors that affect its quality, so as to provide help for the collection of resources of the important medicinal licorice and the human control of its quality in the future. MATERIALS AND METHODS: We conducted extensive searches of the primary literature, master's and doctoral theses, and pharmacopeias of many countries using PubMed, Geenmedical, CNKI, Web of Science, SCI-hub and other databases. The keywords used in searches included "classification of Glycyrrhiza," "medicinal Glycyrrhiza," "distribution of Glycyrrhiza," and "suitable environment for Glycyrrhiza" The results of research conducted by our research group on the morphological and genetic characteristics, natural distribution, and effects of artificial regulation on the growth and quality of licorice were summarized. RESULTS: There are approximately 29 species of G. Linn. worldwide, including 15 species with medicinal value. These species occur on all continents except Antarctica across 41 countries. Only one licorice is recorded in Indian pharmacopoia,two species are recorded in US and Japanese pharmacopoeias,and three species are recorded in most national pharmacopoeias: G. glabra Linn., G. uralensis Fisch. and G. inflata Batalin. These three medicinal licorice species are mainly distributed in Eurasia, especially Central Asia. The main morphological differences between these three medicinal licorice species are in the leaves, inflorescences, pods, and seeds, and they can be distinguished by ITS and psbA-trnH sequences. The reserves of wild licorice in China have decreased annually to 1.04 million(t) in 2010. The cultivation area of G. uralensis Fisch in China is currently approximately 26,900 hm2. Soil conditions have a substantial effect on the yield and quality of G. uralensis Fisch, especially water and nutrients. Appropriate irrigation and fertilization measures can enhance the quality of G. uralensis Fisch. CONCLUSIONS: G. Linn. species and their natural distributions were summarized. The morphology, genetic characteristics, suitable environment, and area of suitable habitat of three medicinal licorice species collected in major countries were described. The main environmental conditions and cultivation measures affecting their growth and medicinal quality were determined. This article provides a comprehensive review on G. Linn. medicinal plant resources to enhance the future use of these resources.

M cells of mouse and human Peyer's patches mediate the lymphatic absorption of an Astragalus hyperbranched heteroglycan.

The gut cell wall is considered an impenetrable barrier to orally administrated polysaccharides. We recently reported a selective lymphatic route for Radix Astragali polysaccharide RAP to enter Peyer's patches (PPs) to trigger immune responses. However, how RAP enters PPs is unclear. Herein, we screened the intestinal epithelial cells of mice and found that the follicle-associated epithelium cells were specifically bound with FITC-RAP. Further studies in vitro and in vivo revealed that RAP was efficiently transported by microfold (M) cells. We also confirmed that M cell-transported RAP directly contacted dendritic cells. More importantly, for the first time, we verified this interesting M cell-mediated transcytosis of RAP in the human distal ileum. Mechanistically, we identified M cells to be the transporter cells that independently deliver RAP into the lymphatic system to trigger immune responses. This interesting transcytosis mechanism might apply to many other immunomodulatory polysaccharides orally dosed to human body.

Impact of Sulfur Fumigation on Ginger: Chemical and Biological Evidence.

We previously found that sulfur fumigation, a commonly used controversial method for the post-harvest handling of ginger, induces the generation of a compound in ginger, which was speculated to be a sulfur-containing derivative of 6-shogaol based on its mass data. However, the chemical and biological properties of the compound remain unknown. As a follow-up study, here we report the chemical structure, systemic exposure, and anticancer activity of the compound. Chromatographic separation, nuclear magnetic resonance analysis, and chemical synthesis structurally elucidated the compound as 6-gingesulfonic acid. Pharmacokinetics in rats found that 6-gingesulfonic acid was more slowly absorbed and eliminated, with more prototypes existing in the blood than 6-shogaol. Metabolism profiling indicated that the two compounds produced qualitatively and quantitatively different metabolites. It was further found that 6-gingesulfonic acid exerted significantly weaker antiproliferative activity on tumor cells than 6-shogaol. The data provide chemical and biological evidence that sulfur fumigation may impair the healthcare functions of ginger.

Licorice: Resources, applications in ancient and modern times.

ETHNOPHARMACOLOGICAL RELEVANCE: Licorice has been widely used as a medicinal herb since ancient times. Licorice is also spelled as "liquorice" and it is known as "Glycyrrhizae Radix et Rhizoma" (Chinese: gan cao) in the Chinese Pharmacopoeia. Licorice root has a wide range of pharmacological effects, including adrenocortical hormone-like effects, as well as multiple pharmacological effects on the digestive system, immune system, and cardiovascular system. AIM OF THE REVIEW: This review aims to comprehensively investigate the history of licorice and its medicinal and industrial applications in China and other nations, including research and application prospects related to the aerial parts of licorice. METHOD: An extensive review of the literature was carried out, including ancient and modern texts, doctoral and masters' theses, monographs on medicinal plants, pharmacopoeias and electronic databases, including Web of Science, Springer, CNKI, and Google Scholar. RESULTS: The ancient and modern applications of licorice were systematically investigated. In ancient times, practitioners in China discovered the medicinal potential of licorice and used it widely. In modern times, licorice is widely used in food, medicines and supplements, tobacco, chemical applications, environmental applications, animal husbandry and other industries. The potential of the aerial portion of the plant is also gradually being researched, developed, and utilized. CONCLUSION: Licorice is one of the oldest and most widely used herbal medicines in the world. This article reviews its medicinal potential and application in various fields, and briefly introduces current research into its aerial parts. This review aims to highlight the importance of licorice and provide direction for its future development.

A lymphatic route for a hyperbranched heteroglycan from Radix Astragali to trigger immune responses after oral dosing.

Gut barrier makes a huge research gap between in vivo and in vitro studies of orally bioactive polysaccharides: whether/how they contact the related cells in vivo. A hyperbranched heteroglycan RAP from Radix Astragali, exerting antitumor and immunomodulatory effects in vitro and in vivo, is right an example. Here, we determined first that RAP's antitumor activity is immune-dependent. Being undegraded and non-absorbing, RAP quickly entered Peyer's patches (PPs) in 1 h where it directly targeted follicle dendritic cells and initiated antitumor immune responses. RAP was further delivered to mesenteric lymph node, bone marrow, and tumor. By contrast, the control Dendrobium officinale polysaccharide did not enter PPs. These findings revealed a blood/microbiota-independent and selective lymphatic route for orally administrated RAP to directly contact immune cells and trigger antitumor immune responses. This route bridges the research gap between the in vitro and in vivo studies and might apply to many other bioactive polysaccharides.

Correlation between quality and geographical origins of Leonuri Herba revealed by the qualitative fingerprint profiling and quantitative determination of chemical components.

BACKGROUND: Leonuri Herba (Yimucao) is a very common Chinese herbs for treating menstrual and maternal diseases for thousands of years in China. However, the herb collected in different origins was easily found in the markets which induce the unstable quality for clinic use. In this study, a comprehensive strategy of using multiple chromatographic analysis and chemometric analysis was firstly investigated for chemical discrimination of Leonuri Herba from different geographical origins. METHODS: UHPLC-QTOF-MS/MS was applied to identify the peaks of Leonuri Herba and chemical fingerprints were established in 30 batches from different geographical origins. Meanwhile, dissimilarities of chemical compositions among different origins were further investigated by principal component analysis and cluster analysis. And a quantitative UHPLC-QTOF-MS/MS approach were established to investigate the potential marker for quality control of Leonuri Herba. RESULTS: A total of 49 chromatographic peaks of Leonuri Herba were identified by UHPLC-QTOF-MS/MS. Leonuri Herba were classified into four categories, and eight major compounds detected could be used as chemical markers for discrimination. Also, the eight components, including leonurine, 4',5-dihydroxy-7-methoxyflavone, rutin, hyperoside, apigenin, quercetin, kaempferol and salicylic acid, were simultaneously quantified using the extracting ion mode of UHPLC-QTOF-MS/MS. CONCLUSION: The current strategy not only clearly expounded the correlation between quality and geographical origins of Leonuri Herba, but also provided a fast, accurate and comprehensive qualitative and quantitative method for assessing the quality of Leonuri Herba.

Antifibrotic activities of Scutellariae Radix extracts and flavonoids: Comparative proteomics reveals distinct and shared mechanisms.

BACKGROUND: Scutellariae Radix (SR), the root of Scutellaria baicalensis Georgi, and SR flavonoids have antifibrotic activities. It remains obscure, however, amongst SR aqueous extract (SRA), SR methanolic extract (SRM) and five major SR flavonoids (baicalein, baicalin, wogonoside, wogonin and oroxyloside), which ones are the most promising antifibrotics and what their mechanisms are. PURPOSE: To compare the antifibrotic activities of SR extracts and flavonoids, and the proteomic signatures of selected SR extract and flavonoid, versus IN1130 phosphate, an antifibrotic positive control (abbreviated as IN1130), in TGF-ß1-induced in vitro model of fibrosis in NRK-49F renal fibroblasts. METHODS: Isobaric labelling-based mass spectrometry was used for proteomic studies. Differentially expressed proteins were further analyzed using Gene Ontology annotation enrichment, protein-protein interaction network analysis and pathway analysis. Selected proteins of interest were validated by enzyme-linked immunosorbent assay (ELISA). RESULTS: Baicalein was the SR flavonoid with the best efficacy-toxicity ratio. SRM contained 8-fold more flavonoids and was more potently antifibrotic than SRA. Proteomic analysis of cells treated by TGF-ß1, with or without baicalein (40 and 80 µM), SRM (40 and 80 µg/ml) and IN1130 (1 µM) suggested that baicalein, SRM and IN1130 all repressed TGF-ß1-induced ribosomal proteins in cell lysates, while baicalein and SRM, but not IN1130, regulated the intracellular lysosome pathway; secretomic analysis suggested that 40 and 80 µg/ml SRM and 80 µM baicalein, but not IN1130 and 40 µM baicalein increased ribosomal proteins in conditioned media, whereas only baicalein regulated the lysosome pathway. ELISA verified secretomic findings that baicalein, SRM and IN1130 repressed TGF-ß1-induced PAI-1 (Serpine1), Plod2, Ctgf (Ccn2), Ccl2 and Ccl7; baicalein and IN1130, but not SRM, reversed TGF-ß1-induced Cyr61 (Ccn1) and Tsku; only baicalein reversed TGF-ß1 repression of Mmp3; only IN1130 reversed TGF-ß1-repressed Nov (Ccn3). ELISA validated cell-lysate proteomic findings that baicalein, SRM and IN1130 all reversed TGF-ß1-induced Enpp1; only IN1130 reversed TGF-ß1-induced Impdh2 and Sqstm1 and TGF-ß1-repressed Aldh3a1. Baicalein and SRM induced Ccdc80, while only baicalein induced Tfrc. CONCLUSION: Baicalein, SRM and IN1130 repress TGF-ß1-induced fibrogenesis in renal fibroblasts by regulating overlapping protein targets and biological pathways. Our findings offer a comprehensive view of shared, drug- and dose-specific pharmacological and toxicological mechanisms and provide a valuable resource for further research and development of more efficacious and safer antifibrotics.

Cordyceps polysaccharide marker CCP modulates immune responses via highly selective TLR4/MyD88/p38 axis.

Cordyceps, one of the most expensive natural health supplements, is popularly used to modulate immune function. However, little is known regarding the underlying mechanism of its immunomodulatory activity. We newly reported a Cordyceps quality marker CCP (Mw 433.778 kDa) which was characterized as a 1,4-α glucan by chemical and spectral analysis and is able to induce significant immune responses of macrophages. Herein, we further investigated the molecular mechanism of CCP's immunomodulatory effects. The results indicate that CCP modulates the TLR4/MyD88/p38 signaling pathway of macrophages, where TLR4 plays a crucial role as verified on TLR4-deficient (TLR4-/-) bone marrow-derived macrophages (BMDMs) and TLR4-/- mice. These findings provide a precise understanding of the molecular mechanism of Cordyceps' immunomodulatory benefits.

A specific and bioactive polysaccharide marker for Cordyceps.

Cordyceps is one of the most expensive and widely used functional foods. But the authenticity is still a concern due to the lack of appropriate markers. By targeting polysaccharides, this study aimed to develop a specific, and bioactive marker for Cordyceps. Firstly, the results of screening tests of 250 samples by examining both genetic markers and polysaccharide profile showed that a unique polysaccharide fraction (named CCP) was particular to the caterpillar parts. Its potential as a marker was further demonstrated by its ability to induce NO and cytokine production in RAW 264.7 cells. CCP was characterized to be an α-1,4-glucan with a branch at C-6 by the conventional structure analyzing and de novo oligosaccharides sequencing. The content of CCP was closely correlated to the traditional classification criteria. Generally, CCP was a marker that simultaneously enables qualitative and quantitative analysis of Cordyceps.

Ginseng ameliorates exercise-induced fatigue potentially by regulating the gut microbiota.

The therapeutic effects of water extract of ginseng (WEG) on exercise-induced fatigue (EF) have been reported in several previous studies, but the molecular mechanisms involved remain unexplored. In this study, the anti-EF effects of WEG were studied, and the potential mechanisms were discussed. We characterized the chemical components of WEG by ultra-high performance liquid chromatography-tandem triple quadrupole mass spectrometry (UHPLC-QqQ-MS/MS) and high performance liquid chromatography coupled with evaporative light scattering detection (HPLC-ELSD), and then examined the anti-EF effects of WEG on a rat model of weight-loaded swimming with a focus on endogenous metabolism and gut microbiota. WEG contains abundant (90.15%, w/w) saccharides and ginsenosides with structurally diverse glycosyls. WEG taken orally showed strong anti-EF effects by ameliorating energy metabolism abnormality, oxidative stress, lipid peroxidation, inflammatory response, disorders in the metabolism of bile acid, amino acid, fatty acid and lipid, as well as the gut microbiota dysbiosis. Given that gut microbiota is significantly associated with energy expenditure, systemic inflammation and host metabolism, these findings suggest a potential central role of the gut microbiota in mediating the anti-EF effect of WEG. That is, the saccharides and ginsenosides in WEG serve as energy substrates for specific intestinal bacteria, thereby beneficially regulating the gut microbiota, and the reshaped gut microbial ecosystem then triggers several molecular and cellular signaling pathways (e.g. butyrate or TGR5 signals) to achieve the therapeutic effects on EF. The outcomes highlighted here enable deeper insight into how WEG overcomes EF.

A hybrid platform featuring nanomagnetic ligand fishing for discovering COX-2 selective inhibitors from aerial part of Saussurea laniceps Hand.-Mazz.

ETHNOPHARMACOLOGICAL RELEVANCE: Saussurea laniceps Hand.-Mazz. (Compositae) is a representative "snow lotus" herb well known in Chinese folk medicine to treat inflammation-related diseases such as arthritis. S. laniceps (SL) shows anti-inflammatory and analgesic potencies and contains various constituents potentially with cyclooxygenase-2 (COX-2) selective inhibition. The herb is a valuable source of natural alternatives to synthetic COX-2 selective nonsteroidal anti-inflammatory drugs, a common medication for rheumatoid arthritis (RA) and osteoarthritis (OA) reported with serious cardiovascular side effects. AIM OF THE STUDY: Based on an innovative drug screening platform, this study aimed to discover safe, effective COX-2 selective inhibitors from SL. MATERIALS AND METHODS: An enzyme-anchored nanomagnetic fishing assay was developed to separate COX-2 ligands from SL. Cell and animal models of cardiomyocytes, lipopolysaccharide-stimulated macrophages, rat adjuvant-induced arthritis, and anterior cruciate ligament transection-induced OA rats, were adopted to screen the single/combined ligands regarding toxicity and bioactivity levels. Molecular docking was employed to unravel binding mechanisms of the ligands towards COX-1 and COX-2. RESULTS: Four COX-2 selective compounds were separated from SL using optimized COX-2-functionalized magnetic nanoparticles. All the four ligands were proved with evidently lower cardiotoxicity both in vitro and in vivo than celecoxib, a known COX-2 selective inhibitor. Two ligands, scopoletin and syringin, exhibited potent anti-arthritic activities in rat models of RA and OA by alleviating clinical statuses, immune responses, and joint pathological features; their optimum combination ratio was discovered with stronger remedial effects on rat OA than single administrations. The COX-1/2 binding modes of the two phytochemicals contributed to explain their cardiac safety and therapeutic performances. CONCLUSIONS: The screened chemicals are promising to be developed as COX-2 selective inhibitors as part of treating RA and OA. The hybrid strategy for discovering therapeutic agents from SL is shown here to be efficient; it should be equally valuable for finding other active chemicals in other natural sources.

Structure of a laminarin-type ß-(1→3)-glucan from brown algae Sargassum henslowianum and its potential on regulating gut microbiota.

A homogeneous polysaccharide named SHNP with apparent molecular weight of 8.4 kDa was purified from brown algae Sargassum henslowianum using ethanol precipitation, ion-exchange chromatography, and gel-filtration column chromatography. Structural analyses reveal that SHNP is completely composed of glucose, and its backbone consists of ß-D-(1→3)-Glcp with side chains comprising t-ß-D-Glcp attached at the O-6 position. Thus, SHNP is a laminarin-type polysaccharide. In vitro fermentation test results showed that SHNP was digested by gut microbiota; the pH value in the fecal culture of SHNP was significantly decreased; and total short-chain fatty acids, acetic, propionic and n-butyric acids were significantly increased. Furthermore, SHNP regulated the intestinal microbiota composition by stimulating the growth of species belonging to Enterobacteriaceae while depleting Haemophilus parainfluenzae and Gemmiger formicilis. Taken together, these results indicate that SHNP has the potential for regulating gut microbiota, but its specific role in the regulation requires to be further investigated.

Analysis of historical changes in traditional Chinese medicine based on an Indonesian collection of Chinese materia medica from c. 1870.

ETHNOPHARMACOLOGICAL RELEVANCE: Traditional Chinese Medicine is subject to changes over time: product names, botanical ingredients, processing methods and uses have varied throughout the course of history. Historic collections of Chinese materia medica (CMM) are of great value for research on the evolvement, development and variability of Chinese herbal medicine over time. These changes may have a significant influence on the safety and efficiency of nowadays' clinical practice. Here we investigate a historic collection of Chinese medicinal products purchased in Indonesia in c. 1870, containing about 395 specimens. AIM OF THE STUDY: This study compares the specimens contained in late 19th century collection of CMM with contemporary marketed materials by investigating changes in vernacular names, botanical identity and processing methods which are important aspects for safety and clinical practice today. MATERIALS AND METHODS: The contents and associated documentation of the CMM collection of Dr. C.H.A. Westhoff (University Museum Utrecht) were revised by means of morphological identification and study of the associated historic documentation. We compared this Westhoff collection with contemporary CMM, information from literature and various quality standards, including the official Chinese pharmacopoeia. RESULTS: The Westhoff collection represents a unique, well preserved collection of Chinese materia medica, with original uniform bottles, Chinese labels and a partly intact handwritten catalogue. Among the 395 specimens (bottles) of CMM surveyed, there are 387 contain a single component drug, while eight contain multiple components drugs. A total of 293 of the 395 specimens are mentioned in the modern Chinese pharmacopoeia. Ca. 25% of the specimens had been processed, such as stir-fried with or without adjuvants. Our analysis of local Chinese names, botanical content and processing methods indicate that this collection originates from southern part of China, possibly including in the region of Taiwan and was meant as a showcase for pharmaceutical education and/or as curiosity object. CONCLUSION: Differences in vernacular names, plant parts and processing methods between the Westhoff collection and the current Chinese pharmacopoeia illustrate the regional variety of CMM and changes in CMM in the course of time. This work contributes to the understanding of the evolvement of CMM from a historic perspective.