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Nine new nontriterpenoids were identified from Panax notoginseng rot roots, and their cytotoxicities may be related to the EGFR inhibition.

Deep neural networks have achieved breakthrough improvement in various application fields. Nevertheless, they usually suffer from a time-consuming training process because of the complicated structures of neural networks with a huge number of parameters. As an alternative, a fast and efficient discriminative broad learning system (BLS) is proposed, which takes the advantages of flat structure and incremental learning. The BLS has achieved outstanding performance in classification and regression problems. However, the previous studies ignored the reason why the BLS can generalize well. In this article, we focus on the interpretation from the viewpoint of the frequency domain. We discover the existence of the frequency principle in BLS, i.e., the BLS preferentially captures low-frequency components quickly and then fits the high frequencies during the incremental process of adding feature nodes and enhancement nodes. The frequency principle may be of great inspiration for expanding the application of BLS.

The broad learning system (BLS) is an emerging flat network, which has demonstrated its outstanding performance in classification and regression problems. The regularization plays an important role in the performance of the BLS. In real applications, since the BLS network is usually expanded dynamically, a predetermined regularization parameter may reduce the performance of the network. Using a fixed regularization in some cases, the classification accuracy of the BLS decreases dramatically when we expand the network. To alleviate this problem, we propose a method that automatically finds appropriate regularization parameters for different datasets, which is based on the weighted generalized cross-validation (WGCV). The experimental results indicate that the WGCV method improves the performance of the BLS, and alleviates the accuracy decrease of the incremental learning algorithm.

Phyllaciduloids E (1) and F (2), two new cleistanthane diterpenoids, were isolated from the leaves of Phyllanthus acidus (L.) Skeels (Phyllanthaceae). Their planar structures were established by spectroscopic analysis and comparison with literature values. The relative configurations of phyllaciduloids E and F were confirmed by DFT-NMR chemical shift calculations and subsequent CP3 probability methods. Phyllaciduloids E and F were evaluated for their cytotoxicity. However, no significant activities were detected at concentrations up to 40 μM.

Eleven flavonoids including one new flavonol glycoside, quercetin-3

Management errors during pre-hospital care, triage process and resuscitation have been widely reported as the major source of preventable and potentially preventable deaths in multiple trauma patients. Common tools for defining whether it is a preventable, potentially preventable or non-preventable death include the Advanced Trauma Life Support (ATLS®) clinical guideline, the Injury Severity Score (ISS) and the Trauma and Injury Severity Score (TRISS). Therefore, these surrogated scores were utilized in reviewing the study’s trauma services. Trauma data were prospectively collected and retrospectively reviewed from January 1, 2018, to December 31, 2018. All cases of trauma death were discussed and audited by the Hospital Trauma Committee on a regular basis. Standardized form was used to document the patient’s management flow and details in every case during the meeting, and the final verdict (whether death was preventable or not) was agreed and signed by every member of the team. The reasons for the death of the patients were further classified into severe injuries, inappropriate/delayed examination, inappropriate/delayed treatment, wrong decision, insufficient supervision/guidance or lack of appropriate guidance. A total of 1913 trauma patients were admitted during the study period, 82 of whom were identified as major trauma (either ISS > 15 or trauma team was activated). Among the 82 patients with major trauma, eight were trauma-related deaths, one of which was considered a preventable death and the other 7 were considered unpreventable. The decision from the hospital’s performance improvement and patient safety program indicates that for every trauma patient, basic life support principles must be followed in the course of primary investigations for bedside trauma series X-ray (chest and pelvis) and FAST scan in the resuscitation room by a person who meets the criteria for trauma team activation recommended by ATLS®. Mechanisms to rectify errors in the management of multiple trauma patients are essential for improving the quality of trauma care. Regular auditing in the trauma service is one of the most important parts of performance improvement and patient safety program, and it should be well established by every major trauma center in Mainland China. It can enhance the trauma management processes, decision-making skills and practical skills, thereby continuously improving quality and reducing mortality of this group of patients.

Phyllaciduloids E (

Panax notoginseng (Burk.) F.H. Chen is a perennial herb in the genus Panax in the Araliaceae family. The root of P. notoginseng, an important Chinese medicinal material, has been widely used as a tonic and hemostatic drug for promoting blood circulation, relief from bruises, and treating blood loss caused by both internal and external injuries. Research on P. notoginseng has led to the isolation of more than 200 natural compounds or as transformed products, and the saponins are the major components. Herein, this chapter introduces the history and origin, chemical and biological studies, as well as clinical applications of P. notoginseng.

The extensive chemical investigation on the branches and leaves of Terminalia chebula var. tomentella (Combretaceae) led to the isolation of two new lignan glucosides with a furofuran skeleton, termitomenins F (1) and G (2). In addition, 19 known compounds including five lignan glucosides (3–7), six hydrolyzable tannins (8–13) and eight simple phenolics (14–21) were also identified. Their structures were determined by comprehensive spectroscopic analyses. It is noted that 8 and 9 were C-glycosidic hydrolyzable tannins with one hexahydroxydiphenoyl and one gallagyl group linked to an open-chain glucosyl C-1/O-2/O-3 and O-4/O-6, respectively, which were rarely found in plants. Nine known compounds, 6–9, 13, and 18–21, were procured from the titled plant for the first time, while 3–5, 10–12 and 14–17 were also found in the fruits. Notably, the known hydrolyzable tannins 8–13 exhibited stronger α-glucosidase inhibitory activities with IC50 values ranging from 0.10 to 3.12 μM, than the positive control, quercetin (IC50 = 9.38 ± 0.33 μM). Graphic abstract

Three previously undescribed pyridyl-steroidal glycoalkaloids, solanindiosides A‒C, one rare 23S,26R-hydroxylated spirostanoid saponin, and two steroidal alkaloid aglycones, solanindins A and B, derived from the acid hydrolysis of solanindiosides A‒C, were isolated from the fruits of Solanum violaceum, together with five known analogues, including two rare steroidal glycosides, two lignans and a diterpene. Structurally, they comprise a 16β-methoxy-23-deoxy-22,26-epimino-cholest-type skeleton moiety, and a 16β-methoxy-3,23-dideoxy-22,26-epimino-cholest-3,5-dien derivative. The hitherto undescribed structures were established on the basis of extensive spectroscopic analyses. Configurations of sugar moieties were resolved by chemical derivations. Solanindiosides A‒C, (22R,23S,25R,26R)-spirost-5-ene-3β,23,26-triol3-O-β- d -xylopyranosyl-(1→3)-β- d -glucopyranoside, solanindins A and B, and (1S,2S)-1-(4-hydroxy-3-methoxyphenyl)-2-[2-methoxy-4-[(2S,3R,4R)-tetrahydro-4-[(4-hydroxy-3-methoxyphenyl)methyl]-3-(hydroxymethyl)-2-furanyl]phenoxy]-1,3-propanediol were evaluated for their cytotoxic and antibacterial activities. (1S,2S)-1-(4-hydroxy-3-methoxyphenyl)-2-[2-methoxy-4-[(2S,3R,4R)-tetrahydro-4-[(4-hydroxy-3-methoxyphenyl)methyl]-3-(hydroxymethyl)-2-furanyl]phenoxy]-1,3-propanediol showed the most potent cytotoxic activity against MCF-7 cells (IC50 = 4.386 ± 0.098 μM), while solanindin B displayed some inhibitory effects against Staphylococcus aureus Rosenbach with MIC50 value of 37.32 ± 0.793 μM. In addition, (1S,2S)-1-(4-hydroxy-3-methoxyphenyl)-2-[2-methoxy-4-[(2S,3R,4R)-tetrahydro-4-[(4-hydroxy-3-methoxyphenyl)methyl]-3-(hydroxymethyl)-2-furanyl]phenoxy]-1,3-propanediol induced dose dependent apoptosis effect in MCF-7 cells.

Phytochemical investigation on the nonpolar extracts of P. acidus leaves afforded three new cleistanthane diterpenoids, named phyllanacidins A–C (1–3), in addition to three known ones (4–6). Among them, compounds 2 and 3 represent the first examples of 17-nor cleistanthane diterpenoids. Their structures including absolute configurations were elucidated on the basis of extensive spectroscopic data and single crystal X-ray diffraction analysis. All the isolated cleistanthane diterpenoids were evaluated for their cytotoxic activities against five human cancer cell lines. Compounds 4–6 exhibited moderate cytotoxicity with IC50 values ranging from 16.11 to 30.82 μM.

As a subgroup of flavoalkaloids, N-ethyl-2-pyrrolidinone substituted flavan-3-ols are reported to possess various biological activities that may play important roles in the beneficial healthcare functions of tea. The HPLC and LC-MS analyses showed the existence of N-ethyl-2-pyrrolidinone substituted flavan-3-ols in 'Jin-Ya', which is a Yunnan black tea produced only from the buds of the tea plant Camellia sinensis var. assamica. Further phytochemical study on this precious black tea led to the identification of 8 flavoalkaloids, 1-8, along with 11 known flavan-3-ols (9-14) and flavonol glycosides (15-19). The new compounds, (-)-6-(5″S)-N-ethyl-2-pyrrolidinone-epiafzelechin (1), (-)-8-(5″R)-N-ethyl-2-pyrrolidinone-epiafzelechin-3-O-gallate (2a), and (-)-8-(5″S)-N-ethyl-2-pyrrolidinone-epiafzelechin-3-O-gallate (2b), were identified based on extensive spectroscopic analysis. Flavoalkaloids 2-6 showed inhibitory activity on α-glucosidase with IC50 values ranging from 2.09 to 8.47 μM, compared to those of quercetin and acarbose (IC50 = 6.87 and 228.9 μM, respectively). Moreover, compounds 2, 3, and 6 displayed an inhibitory effect on acetyl-cholinesterase with IC50 values of 14.23, 33.79, and 34.82 μM, respectively, compared to tacrine (IC50 = 0.223 μM).

Background: Root rot is a serious destructive disease of Panax notoginseng, a famous cultivated araliaceous herb called Sanqi or Tianqi in Southwest China. Methods: The chemical substances of Sanqi rot roots were explored by chromatographic techniques. MS, 1D/2D-NMR, and single crystal X-ray diffraction were applied to determine the structures. Murine macrophage RAW264.7 and five human cancer cell lines were used separately for evaluating the antiinflammatory and cytotoxic activities. Results and Conclusion: Thirty dammarane-type triterpenes and saponins were isolated from the rot roots of P. notoginseng. Among them, seven triterpenes, namely, 20(S)-dammar-25-ene-24(S)-hydroperoxyl-3β,6α,12β,20-tetrol (1), 20(S)-dammar-3-oxo-23-ene-25-hydroperoxyl-6α,12β,20-triol (2), 20(S)-dammar-12-oxo-23-ene-25-hydroperoxyl-3β,6α,20-triol (3), 20(S)-dammar-3-oxo-23-ene-25-hydroperoxyl-12β,20-diol (4), 20(S),24(R)-epoxy-3,4-seco-dammar-25-hydroxy-12-one-3-oic acid (5), 20(S),24(R)-epoxy-3,4-seco-dammar-25-hydroxy-12-one-3-oic acid methyl ester (6), and 6α-hydroxy-22,23,24,25,26,27-hexanordammar-3,12,20-trione (7), are new compounds. In addition, 12 known ones (12–16 and 19–25) were reported in Sanqi for the first time. The new Compound 1 showed comparable antiinflammatory activity on inhibition of NO production to the positive control, whereas the known compounds 9, 12, 13, and 16 displayed moderate cytotoxicities against five human cancer cell lines. The results will provide scientific basis for understanding the chemical constituents of Sanqi rot roots and new candidates for searching antiinflammatory and antitumor agents. Keywords: 20,24-epoxylated, Dammarane-type triterpenes, Hydroperoxylated, Panax notoginseng, Inhibition of NO production

Dasiphora fruticosa L. (Rosaceae), also known as Potentilla fruticosa L. (syn.), is a hardy deciduous shrub widely distributed in the north temperate regions of the world. Three methylene bisflavan...

Continuous cropping obstacle, mainly caused by microorganisms and organic components in soil, has become a serious problem for the plantation of Panax notoginseng (Araliaceae) due to the rapidly increased demands of this famous herbal medicine in recent decades. The rhizosphere soils cultivated with 3-year-old healthy and ill notoginseng were chemically investigated by gas chromatography-mass spectrometry (GC-MS) and compared with the corresponding soils without the plantation of notoginseng. Totally 47 liposoluble components were identified. Furthermore, the multiple statistical analysis showed that these constituents were qualitatively and quantitatively associated with the differences between the cultivated soil with P. notoginseng and the uncultivated soil. Among them, neophytadiene (4), D-α-tocopherol (38), (3β,22E,24S)-ergosta-5,22-dien-3-ol (39), (3β,24R)-ergost-5-en-3-ol (40), stigmasta-5,22-dien-3-ol (41), stigmast-4-en-3-one (44) and (5α)-stigmastane-3,6-dione (47) contributed most to the significant differences between the cultivated and uncultivated soils, whereas cyclopentadecane (3), octadecanoic acid methyl ester (16), docosanoic acid ethyl ester (31), nonacosane (34), 38 and 39 were found in much higher amount in the soils with ill P. notoginseng as compared to the case of those with the healthy P. notoginseng. On the other hand, liposoluble components in different cultivation areas were of great diversity; however, they were able to remain relatively consistent across the overall trend of differential substances.

Six diterpenoids including three ent-kauranes (1-2, 4) and three cleistanthanes (3, 5-6) were isolated from the roots and stems of Phyllanthus acidus (L.) Skeels. Of them, (16S)-ent-16,17,18-tri-hydroxy-19-nor-kaur-4-en-3-one (1), phyllanthone A (2), and 6-hydroxycleistanthol (3) are new compounds, while the ent-kaurane diterpenoids were reported from the titled plant for the first time. Their structures were elucidated on the basis of the extensive spectroscopic analyses. Compounds 2 and 4-6 displayed cytotoxic potential with IC

Tea, as one of the most popular beverages with various bioactivities, is commonly produced from the fresh leaves of two widely cultivated tea plants, Camellia sinensis and C. sinensis var. assamica. Both plants belong to the genus Camellia section Thea, which was considered to have 12 species and 6 varieties according to Min's taxonomic system. Most species, except the cultivated species, are known as wild tea plants and have been exploited and utilized to produce tea by the local people of its growing areas. Thus far, six species and varieties have been phytochemically studied, leading to the identification of 398 compounds, including hydrolyzable tannins, flavan-3-ols, flavonoids, terpenoids, alkaloids, and other phenolic and related compounds. Various beneficial health effects were reported for tea and its components, involving antioxidant, antitumor, antimutagenic, antidiabetic, hypolipidemic, anti-inflammatory, antimicrobial, antiviral, antifungal, neuroprotective, hepatoprotective, etc. In this review, the geographical distribution of tea plants and the chemical constituents (1-398) reported from the genus Camellia section Thea and some tea products (green, black, oolong, and pu-erh tea) that have ever been studied between 1970 and 2018 have been summarized, taking species as the main hint, and the main biological activities are also discussed.

Panax, a genus of the Araliaceae family, is an important herbal group in traditional Chinese medicine (TCM). Nine species and three varieties are included in the genus of Panax, in which nearly all species have been used for medicinal purposes. Among them, Panax notoginseng (Burk) F. H. Chen, Panax ginseng C. A. Meyer and Panax quinquefolius L. are the most representative and valuable herbs world-wide, with a long history of cultivation. As the main bioactive chemical constituents, saponins with different aglycones are the major components in various Panax spp., and their pharmacological activities are mainly reflected in the effects on blood system, cardio- and cerebro-vascular systems, nervous system, metabolism, and immune regulation. Researchers of Kunming Institute of Botany (KIB), Chinese Academy of Sciences (CAS), have put many efforts into conducting the investigations on Panax species. Herein, we reviewed the research progress on Panax spp. in KIB, CAS, over the past few decades, from the aspects of history and origin, phytochemistry and pharmacological activities. Graphical Abstract

Two new sphingofungins G (1) and H (2) with a five-membered lactone ring were identified from the solid-state fermentation of Aspergillus penicilliodes Speg., a dominant microorganism isolated previously from the post-fermentation of ripe Pu-er tea, together with six known metabolites. Their structures were elucidated by extensive spectroscopic methods. All of them were isolated from the mycelia culture of A. penicilliodes for the first time. The known compound, trypacidin, exhibited potent cytotoxities against five human cancer cell lines, e.g. myeloid leukemia HL-60, lung cancer A-549, hepatocellular carcinoma SMMC7721, breast cancer MCF-7, and colon cancer SW480, with IC

Twelve indolyl diketopiperazines 1–12 were isolated from the mycelia culture of Aspergillus penicilliodes Speg., a dominant microorganism from the post fermentation process of ripe Pu-er tea. Their structures were elucidated by extensive spectroscopic methods. Among them, trypostatins C (1) and D (2) featuring with a rare methyl vinyl ketone side chain at C-2 are new compounds, while 3 and 4 were obtained for the first time from nature source. The isolates 3–12 did not show obvious cytotoxicities against five human cancer cell lines at a concentration of 40 μM. Electronic supplementary material The online version of this article (10.1007/s13659-018-0156-z) contains supplementary material, which is available to authorized users.

Theanaphthoquinone (TNQ) is the initial and main oxidation product of theaflavin, a representative black tea pigment. Nevertheless, TNQ is virtually undetected in the high-performance liquid chromatography analysis of black tea leaves using photodiode array detection. To elucidate the degradation mechanism of theaflavin in the black tea production process, this study investigated the reaction of TNQ with epigallocatechin-3-O-gallate (EGCg), which is the most abundant polyphenol in tea leaves. In citrate–phosphate buffer solution at pH 6 and room temperature, TNQ reacted nonenzymatically with EGCg to afford three products, whose structures were determined on the basis of spectroscopic data. The results indicated that the double bond of the ortho-naphthoquinone moiety in TNQ reacted with the autoxidation product of EGCg. This study demonstrates novel reactions occurring in the process of theaflavin degradation, which might be involved in the formation of thearubigins, the major black tea pigments composing oligomeric catechin oxidation products.

The young leaves of Phyllanthus acidus (Euphorbiaceae) are commonly used as edible vegetables in Indonesia, Thailand, and India, and their water infusions as dieting aids for people trying to remain slim. However, it is regarded as a poisonous plant in Malaya, and current researches are insufficient to provide a conclusion on its toxicity and safety under large doses. In this study, we firstly found that the refined nonpolar extracts of P. acidus leaves showed significant cytotoxic effect against BEAS-2B and L02 normal cell lines with IC50 values of 2.15 and 1.64 mg/mL, respectively. Further bioactivity-guided isolation produced four new rare dichapetalins (pacidusins A–D) from the most active fraction. Their structures including absolute configurations were elucidated by extensive spectroscopic data and X-ray diffraction analysis. All the isolated dichapetalins exhibited moderate cytotoxicity against, BEAS-2B and L02 normal cell lines with IC50 values ranging from 12.44 to 22.55 μM, as well as five human cancer cell lines with IC50 values ranging from 3.38 to 22.38 μM. Furthermore, the content of the main dichapetalins in the leaves were determined by analytical HPLC, which showed that the leaves contained a very high amount of the four isolated dichapetalins with a total yield of 0.488 mg/g of dry plant material. These toxic dichapetalins may lead to adverse health effects in higher doses. Our findings indicate that the dichapetalin containing leaves may not be suitable for consumption in large quantities as food, but demonstrate their potency as anti-cancer agents for new drug discovery.

Camellia fangchengensis Liang et Zhong, belonging to the genus Camellia sect. Thea (Theaceae), is an endemic tea species to the south and southwest areas of Guangxi province, People's Republic of China. Known as a wild tea plant, the leaves have been used for producing green tea or black tea by the local people of its growing area. HPLC and LC-MS analysis showed the leaves contain oligomeric catechins as major phenolic components. Further detailed phytochemical study led to the identification of five flavan-3-ol dimers (1-5) including two new ones, fangchengbisflavans A (1) and B (2) from the leaves of C. fangchengensis, together with six known monomers (6-11) and one glucoside (12), in addition to gallic acid (13). Their structures were determined by extensive spectroscopic analysis. Most of the isolates displayed significant antioxidant activities in 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+) radical scavenging assays. The results suggested that the leaves of C. fangchengensis, rich in flavan-3-ol oligomers and monomers as potent antioxidants, could be a valuable plant resource for the production of tea and natural beverages.

A novel highly oxygenated norbisabolane sesquiterpene, namely phyllanthacidoid U (1), along with nine known sesquiterpenes (2-10) was isolated from the roots and stems of

A novel highly oxygenated norbisabolane sesquiterpene, namely phyllanthacidoid U (1), along with nine known sesquiterpenes (2–10) was isolated from the roots and stems of Phyllanthus acidus (L.) Skeels (Phyllanthaceae), collected from Xishuangbanna, Yunnan province, China. Their structures were elucidated by means of extensive spectroscopic analysis and by comparison of their data with reported values in literatures. Instead of the C-13 ester O-glycosyl found mostly in the titled plant growing in Thailand, compound 1 possessed a rare N-β-glucosamine-2-N-acetate moiety linked directly to the carbonyl at C-13 through an amido bond. Moreover, the acyl group at C-10 in 1 was (Z)-2-(2-hydroxyethyl)-pent-2-enedioyl group, instead of benzoic or p-hydroxybenzoic moieties found commonly in the reported norbisabolane sesquiterpenes. The known sesquiterpene 5 displayed stronger anti hepatitis B virus (HBV) activity with IC50 values of 1.69 ± 0.22 and 2.79 ± 0.69 μM towards HBV surface antigen (HBsAg) and HBV excreted antigen (HBeAg) secretion, respectively.