Glycosides from the leaves of Fraxinus Hubeiensis.

Fraxinus hubeiensis is a plant endemic to China and widely used as folk medicine to treat various diseases. However, its chemical constituents have never been reported sufficiently. Thus, the primary objective of this study was to investigate the phytochemical constituents and biological activities of F. hubeiensis leaves. Hence, combined column chromatographic and spectroscopic techniques were used to identify and characterize the secondary metabolites such as a pair of 3-keto-glycoside epimers (1) and (2), along with five known compounds (3 ~ 7). The results of α-glucosidase inhibitory activity exhibited that 1 and 2 had moderate activity with IC50 values of 359.50 and 468.43 µM, respectively, compared to a positive control acarbose with the IC50 value of 164.08 µM. However, Compounds 1-6 were shown to be inactive against the tested microbes.

A Review of the Phytochemistry and Pharmacology of the Fruit of Siraitia grosvenorii (Swingle): A Traditional Chinese Medicinal Food.

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

Heilaohuacid G, a new triterpenoid from Kadsura coccinea inhibits proliferation, induces apoptosis, and ameliorates inflammation in RA-FLS and RAW 264.7 cells via suppressing NF-𝜠B pathway.

Heilaohu, the roots of Kadsura coccinea, has been used in Tujia ethnomedicine to treat rheumatic arthritis (RA). Heilaohuacid G (1), a new 3,4-seco-lanostane type triterpenoid isolated from the ethanol extract of Heilaohu, whose structure was determined using HR-ESI-MS data, NMR spectroscopic analyses, and ECD calculations. In this study, our purpose is to elucidate the mechanisms of Heilaohuacid G in the treatment of RA by inhibited proliferation of rheumatoid arthritis-fibroblastoid synovial (RA-FLS) cells and inhibited the inflammatory reactions in LPS-induced RA-FLS and RAW 264.7 cell lines via inhibiting NF-κB pathway. The biological activity screening experiments indicated that Heilaohuacid G significantly inhibited proliferation of RA-FLS cells with IC50 value of 8.16 ± 0.47 µM. CCK-8 assay, ELISA, flow cytometry assay, and Western blot were used to measure the changes of cell viability, apoptosis, and the release of inflammatory cytokines. Heilaohuacid G was found not only induced RA-FLS cell apoptosis, but also inhibited the inflammatory reactions in LPS-induced RA-FLS and RAW 264.7 cell lines via inhibiting NF-κB pathway. Furthermore, Heilaohuacid G (p.o.) at doses of 3.0, 6.0, and 12.0 mg/kg and the ethanol extracts of Heilaohu (p.o.) at doses of 200, 400, and 800 mg/kg both were confirmed antiinflammatory effects on xylene-induced ear mice edema model.

Cyclocarya paliurus (Batalin) Iljinskaja: Botany, Ethnopharmacology, phytochemistry and pharmacology.

ETHNOPHARMACOLOGICAL RELEVANCE: Cyclocarya paliurus (Batalin) Iljinskaja (C. paliurus) also known as Sweet tea tree, Money tree, Money willow, green money plum, mountain willow and shanhua tree, is a native rare monocotyledonous plant in Southern China. It possesses numerous traditional benefits, including clearing heat, detoxification, producing saliva, slake thirst, anti-inflammatory, insecticidal, dispelling wind and relieving itching. It is also effective in preventing and treating diabetes, hypertension, hyperlipidemia, dizziness and swelling and pain, as well as reducing cholesterol, and modulating the functions of the immune system. The stem, leaves and bark of this plant are all medicinal parts, but the leaves have the highest research value. AIM OF THE STUDY: This article summarized the plant's botanical description, distribution, ethnopharmacology, phytochemical profiles and pharmacological for the first time, to provide possible directions for future development and research in brief. MATERIAL AND METHODS: The literature for this current manuscript was obtained from reports published from 1992 to May 2021 in diverse databases such as the China Knowledge Resource Integrated databases (CNKI), SciFinder, Google Scholar, Baidu Scholar, Elsevier and Pub-Med. The domestic and foreign references published about C. paliurus over recent years were collected, analyzed and summarized. RESULTS: The botanical characteristics of the fruits of C. paliurus are unique in having a central nutlet surrounded by a circular wing to distinguish the living genera of Juglandaceae. In traditional medicine, C. paliurus leaves are used by the local people of Southern China to make tea to prevent diabetes. More than 210 compounds have been isolated from C. paliurus. Among them, the characteristic 3,4-seco-dammaranes accounted for the most. Other compounds include dammarane tetracyclic triterpenoids, various pentacyclic triterpenoids, flavonoids, isosclerones, phenolic derivatives and polysaccharides. The plant extracts and compounds have been reported to exert various pharmacological activities, such as anti-hyperglycemic, anti-hyperlipidemic, anti-cancer, cytotoxic, anti-oxidative, anti-inflammatory, hepatoprotective, and anti-microbial activities. CONCLUSIONS: Comprehensive literature analysis shows that C. paliurus extract and its compounds have a variety of biological activities for the treatment of various diseases. The current modern pharmacology research is mostly related to the records of ethnic pharmacology, mainly in vitro research, relatively few in vivo research. Therefore, future studies should focus on this aspect. In addition, we also would like to recommend further research should concentrate on toxicity studies and quality control of C. paliurus to fill the study gap, as well as to provide theoretical support for the further development of the potential functions and clinical applications of the plant.

Anti-inflammatory and antioxidant activities of chemical constituents from the flower buds of Buddleja officinalis.

Five new glycosides including mimenghuasu A and B (1-2), isolinarin (3), cyclocitralosides A and B (4-5), along with forty-seven known compounds were isolated from the flower buds of Buddleja officinalis. These structures were elucidated by extensive spectroscopic analysis (UV, IR, 1 D, 2 D NMR, and MS spectra). The anti-inflammatory activities of the isolated compounds were determined by enzyme-linked immunosorbent assay (ELISA) on the expression of TNF-α (LPS-activated RAW264.7 cells) and MTT experiment on LPS-induced HUVECs proliferation effects. Good suppressive effects on the expression of TNF-α were shown by 4 and 5 with IC50 values of 19.35 and 22.10 µM, respectively, compared to positive control indomethacin (IC50 16.40 µM). In addition to this, some isolated compounds exhibited excellent antioxidant activities including compounds 16, 18, 29, 39, and 47 (IC50 µM: 82.59, 72.94, 33.65, 46.67, and 20.81, respectively) with almost the same or stronger potency with reference to vitamin C as positive control (IC50 81.83 µM).

The medicinal uses of the genus Bletilla in traditional Chinese medicine: A phytochemical and pharmacological review.

ETHNOPHARMACOLOGICAL RELEVANCE: Different orchids are important in traditional medicine, and species belonging to the genus Bletilla are important. Bletilla species have been used for thousands of years in Traditional Chinese Medicine (TCM) for the treatment of several health disorders, such as gastrointestinal disorders, peptic ulcer, lung disorders, and traumatic bleeding etc. AIM OF THIS REVIEW: This review aims to provide a systematic overview and objective analysis of Bletilla species and to find the probable relationship between their traditional use, chemical constituents, and pharmacological activities, while assessing their therapeutic potential in treatment of different human diseases. MATERIALS AND METHODS: Relevant literatures on Bletilla species have been collected using the keywords "Bletilla", "phytochemistry", and "pharmacology" in scientific databases, such as "PubMed", "Scifinder", "The Plant List", "Elsevier", "China Knowledge Resource Integrated databases (CNKI)", "Google Scholar", "Baidu Scholar", and other literature sources, etc. RESULTS: This review indicates the isolation and identification of over 261 compounds from this genus, till December 2020. These chemical isolates belong to the stilbenes (bibenzyls and phenanthrenes), flavonoids, triterpenoids, steroids, simple phenolics, and glucosyloxybenzyl 2-isobutylmalates classes of compounds. These compounds have been reported to be characteristically distributed in Bletilla striata (Thunb.) Rchb. f. (BS), Bletilla ochracea Schltr. (BO), and Bletilla formosana (Hayata) Schltr. (BF). The crude extracts and pure compounds derived from the three Bletilla species have reportedly exhibited a wide spectrum of in vitro and in vivo pharmacological effects, such as hemostatic, anti-inflammatory, anti-tumor, and anti-microbial activities. As a Traditional Chinese Medicine (TCM), Bletilla species or preparations containing Bletilla species have been used for the treatment of epistaxis, gastrointestinal bleeding, cough and hemoptysis, gastric and duodenal ulcer, and traumatic injuries. Thus, Bletilla species have proven potential both in traditional uses and scientific studies. CONCLUSIONS: Pharmacological studies have validated the use of Bletilla species in the traditional medicine, especially hemorrhagic diseases. Polysaccharides and stilbenes are the major bioactive chemical constituents of Bletilla genus according to the literatures. However, the mechanism of action of these molecules is yet to be studied. In addition, a detailed comparative analysis of the phytochemistry and biological activities of the three Bletilla species (BS, BO and BF) is highly recommended for understanding their ethnopharmacological uses and applications in clinics. Clinical toxicity tests on BS have been found to be negative, but it can't be used with Aconitum carmichaeli in traditional uses. Furthermore, not many reports are present in the literature regarding the conservation of Bletilla species.

Transcriptomic and metabonomic profiling reveal the anti-obesity effects of Chikusetsusaponin V, a compound extracted from Panax japonicus.

OBJECTIVES: To explore the in vivo anti-obesity effect of chikusetsusaponin V and explore the underlying mechanism by transcriptomic and metabonomic methods. METHODS: The physiological parameters of high-fat-diet induced obese mice administered with or without 25 mg/kg and 100 mg/kg of chikusetsusaponin V by gavage for 16 weeks were recorded. In addition, the RNA-sequencing and UHPLC-Q-TOF techniques were applied to obtain the transcriptomic and metabolomic profiling, respectively. KEY FINDINGS: Chikusetsusaponin V could significantly alleviate the high-fat-diet induced increase in the weight of the whole body and obesity-related organs or tissues, and ameliorate the lipid content in the blood, the lipid accumulation in the livers, as well as the hypertrophy of the fat tissues. Importantly, transcriptomic results revealed that more than 30 genes involved in the pathway which closely associates with obesity, were significantly altered. Moreover, metabolomic data indicated the key differential metabolites enriched in the pathways such as the activated protein kinase signaling pathway which is a vital mediator of obesity and other processes. CONCLUSIONS: The integrative analysis highlighted that chikusetsusaponin V significantly influenced the activated protein kinase signaling pathway at both transcriptomic and metabolomic levels, thereby exerting anti-obesity effects.

A review of the phytochemistry and pharmacology of Kadsura heteroclita, an important plant in Tujia ethnomedicine.

ETHNOPHARMACOLOGICAL RELEVANCE: Kadsura heteroclita (Roxb.) Craib (traditionally known as "Xue Tong") is an important member of the economically and medicinally important plant family Schisandraceae. "Xue Tong" is an imperative ingredient of the Tujia ethnomedicine, traditionally used for the treatment of rheumatoid arthritis (RA), hepatitis, and muscles and joint spasm. The plant is known to be a rich source of lignans and triterpenoids. These classes of natural products have been known to possess various pharmacological activities. AIM OF REVIEW: This review was motivated by the importance of K. heteroclita in traditional Chinese medicine (TCM). It aims to compile the available information on its botanical distribution and description, traditional uses, phytochemistry, pharmacological activities, toxicity, and quality control to provide a solid base for further research and development. MATERIALS AND METHODS: Relevant literature was collected by several scientific databases including PubMed, CNKI, Scifinder, The Plant List, Google Scholar, Baidu Scholar, Books (Tujia pharmaceutical records, Guangxi Chinese herbal medicine, Hunan pharmaceutical records and Field identification manual of Chinese herbal medicine) and other literature sources (Flora of China, Pharmacopoeia of the People's Republic of China) which helped in collecting maximum data about the studied species. RESULTS: Traditional uses of K. heteroclita have proven its medicinal importance, providing a rationale for scientific research. Phytochemical studies on the stem of K. heteroclita resulted in the identification of 187 chemical constituents, among which lignans and triterpenoids are the predominant groups. The isolates and crude extracts have been found to exhibit a wide spectrum of in vivo and in vitro pharmacological activities such as anti-RA, anti-inflammatory and analgesic, hepatoprotection, anti-HIV, anti-cancer and anti-HBV. Schisanlactone E (xuetongsu), a triterpenoid, is one of the major components of K. heteroclita exhibiting anti-cancer, neuroprotective and anti-neuroinflammation activities. Interestingly and luckily, this plant has been found to be safe and non-toxic within the therapeutic dose range. CONCLUSION: Pharmacological investigations have validated the use of K. heteroclita in traditional Chinese medicine (TCM). Literature review has demonstrated that lignans and triterpenoids are possibly responsible for most of the biological activities exhibited by this plant. To conclude, this plant shows immense potential for the discovery of more potent bioactive secondary metabolites and therefore further phytochemical and biological studies on other parts of K. heteroclita need to be conducted and more compounds need to be tested regarding their biological activities to completely explore its value as a tremendously important medicinal plant species.

A Rapid and Accurate 1HNMR Method for the Identification and Quantification of Major Constituents in Qishen Yiqi Dripping Pills.

BACKGROUND: Qishen Yiqi dripping pills (QSYQ), composed of four herbal medicines-Salvia miltiorrhiza, Astragalus membranaceus, Panax notoginseng, and Dalbergiaodorifera-are widely used to treat ischemic cerebrovascular and hemorrhagic cerebrovascular conditions. OBJECTIVE: In this study, a rapid and accurate proton NMR (1HNMR) spectroscopy method was established to control the quality of QSYQ and ensure their clinical efficacy. METHOD: Firstly, different types of metabolites were identified based on the proton signal peaks of chemical shifts, coupling constants, and related information provided through two-dimensional NMR spectroscopy. Secondly, a quantitative 1HNMR method was established for the simultaneous determination of major constituents in QSYQ samples. In addition, an HPLC method was performed to verify the results obtained by the quantitative proton NMR (qHNMR)  method. RESULTS: In the present study, 26 metabolites were identified in the 1HNMR spectra of QSYQ. In addition, a rapid and accruate qHNMR method was established for the simultaneous determination of protocatechualdehyde, rosmarinic acid, danshensu, calycosin-7-O-ß-D-glucoside, and ononin in ten batches of QSYQ samples for the first time. Moreover, the proposed qHNMR method and HPLC method were compared using Bland-Altman and plots Passing-Bablok regression, indicating no significant differences and a strong correlation between the two analytical methods. CONCLUSIONS: This method is an important tool for the identification and quantification of major constituents in QSYQ. HIGHLIGHTS: Compared with traditional HPLC, the established qHNMR method has the advantages of simple sample preparation, short analysis time, and non-destructive analysis.

Flavonoid glycosides from the rhizomes of Pronephrium penangianum.

Six flavonoid glycosides jixueqisus A-F, together with nine known flavonoids, were isolated from the rhizomes of the fern Pronephrium penangianum. Among them, two red pigments jixueqisus A and B possess the same rare 6,8-dimethyl-2-phenyl-7H-1-benzopyran-7-one skeleton (a long conjugated system). Jixueqisu Cwas a dihydrochalcone glycoside, jixueqisu D was a chalcone glycoside, jixueqisu E was an aurone glycoside, and jixueqisu F was a flavonone glycoside. Interestingly, jixueqisus D-F, (2S)-5,2',5'-trihydroxy-7-methoxyflavanone and 5,2',5'-trihydroxy-7-methoxyflavone possessed a 2,5-dihydroxy substituted benzene ring (B-ring). Their structures were elucidated by various spectroscopic and chemical methods. Furthermore, the plausible biosynthetic pathways of jixueqisus A-F were discussed, respectively. All isolated compounds were evaluated for their activities against the proliferation of MCF-7, HepG-2, HCT-116 and BGC-823 tumor cell lines, four known flavane-4-ol glycosides, abacopterins A and C, eruberin B and triphyllin A, exhibited moderate activities to various cell lines.

The flower head of Chrysanthemum morifolium Ramat. (Juhua): A paradigm of flowers serving as Chinese dietary herbal medicine.

ETHNOPHARMACOLOGICAL RELEVANCE: Dietary herbal medicines are widely used for the prevention and treatment of a variety of diseases due to their pharmacological activities in China. Juhua (the flower head of Chrysanthemum morifolium Ramat.), the most representative flower-derived one, which is mainly used for the treatment of respiratory and cardiovascular diseases, shows significant activities, such as antimicrobial, anti-inflammatory, and anticancer, and, neuroprotective, as well as effects on the cardiovascular system. AIMS OF THIS REVIEW: This review aims to provide an overview of the crucial roles of flowers in Chinese dietary herbal medicine, and the pharmaceutical research progress of Juhua (the paradigm of dietary herbal medicine derived from the flower) including its applications in Traditional Chinese medicine and diet, cultivars, phytochemistry, quality control, pharmacology, and toxicity, along with chrysanthemum breeding and biotechnology. METHOD: The information associated with Chinese dietary herbal medicine, flower-derived medicine, dietary flower, and pharmaceutical research of Juhua, was collected from government reports, classic books of Traditional Chinese medicine, the thesis of doctors of philosophy and maters, and database including Pubmed, Scifinder, Web of Science, Google Scholar, China National Knowledge Internet; and others. RESULT: All flower-originated crude medicines recorded in Chinese pharmacopeia and their applications were summarized for the first time in this paper. The edible history and development of flowers in China, the theory of Chinese dietary herbal medicines, as well as flowers serving as dietary herbal medicines, were discussed. Moreover, applications in Traditional Chinese medicine and diet, cultivars, phytochemistry, quality control, pharmacology, and safety evaluation of Juhua, together with chrysanthemum breeding and biotechnology, were summarized in this paper. CONCLUSION: The theory of dietary herbal medicines, which are an important part of the Traditional Chinese medicine system, has a history of thousands of years. Many herbal flowers, serving as dietary herbal medicines, contribute significantly to the prevention and treatment of a variety of diseases for Chinese people. To better benefit human health, more effective supervision practice for dietary herbal medicines is needed. Although various investigations on Juhua have been done, there is a lack of analytical methods for discrimination of cultivar flowers and identification of authenticity. Research on the major compounds with bioactivities, especially those related to its clinical application or healthcare function, as well as their possible mechanize, need be strengthened. More safety evaluation of Juhua should be carried out. The research limitations Juhua is facing exist in all dietary herbal medicine.

Development of a nanodrug-delivery system camouflaged by erythrocyte membranes for the chemo/phototherapy of cancer.

Aim: Development of a new drug-delivery system using a compound derived from Pronephrium penangianum (J5) for the treatment of cervical cancer. Materials & methods: The delivery system was developed using Prussian blue nanoparticles, camouflaged by red blood cell membrane and with folic acid surface modifications. Results: Our results showed the successful development of a nanodrug-delivery system, which increases the half-life and immune evasion ability of the drug. The mechanism of this system was through suppressing B-cell lymphoma 2 and increasing B-cell lymphoma 2-associated X protein and the cleaved caspase level. An in vivo study also confirmed good antitumor activity without any side effects to normal tissue. Conclusion: This drug-delivery system provides a good alternative for the treatment of cervical cancer using J5.

Triterpenoids from stems of Kadsura heteroclita.

In the present work, we reported the triterpenoids isolated from n-butanol fraction of Kadsura heteroclita which is a Tujia ethnomedicine with trivial name "Xuetong". This effort resulted in the isolation of six unpresented triterpenoids xuetongsu A-F (1-6), along with five known triterpenoids (7-11). The structures of the reported compounds were established on the 1D, and 2D NMR and HRESIMS spectra, along with CD spectroscopic analysis. Moreover, the absolute stereochemistry of compound 7 was determined by X-ray diffraction analysis. Antioxidant and cytotoxic activities were evaluated for all isolated compounds, compound 7 shown weak cytotoxic activity against HL-60 with IC50 value of 50.0 µM.

Kadsura coccinea: A rich source of structurally diverse and biologically important compounds.

Kadsura coccinea belongs to medicinally important genus Kadsura from the Schisandraceae family. It has been used in traditional Chinese medicine (TCM) for the treatment of rheumatoid arthritis and gastroenteric disorders. The initial phytochemical work focused on the identification of some structurally novel and diverse natural products, which turned the attention of many researchers towards this plant. Thus far, 202 compounds have been reported in this plant. Lignans and terpenoids were found as the main chemical constituents of this plant. Some of the triterpenoids and sesquiterpenoids with novel structures are of particular interest for natural product researchers. The isolated compounds of this plant have shown different bioactivities including anti-tumor, anti-HIV, anti-inflammatory, nitric oxide (NO) production inhibitory and other pharmacological effects. This review systematically summarizes all the phytochemical and pharmacological work done so far on K. coccinea, and can be used as a reference for future research on this plant.

New Lignans from roots of Kadsura coccinea.

Four new dibenzocyclooctadiene lignans, named heilaohusus A-D (1-4), one new arylnaphthalene lignan named heilaohusu E (5), and seven known analogues (6-12) were isolated from the roots of Kadsura coccinea. Their structures and configurations were elucidated by a combination of HR-ESI-MS, 1H NMR, 13C NMR, HSQC, HMBC, NOESY and CD spectra. Among the known compounds, compounds 6 and 8-12 were isolated from this plant for the first time. All of compounds were evaluated for their cytotoxicity activities, compounds 3, 6 and 7 showed weak cytotoxicity against four human cancer cell lines (HepG-2, HCT-116, BGC-823 and Hela) with IC50 values range from 13.04 to 21.93 µM. Compounds 1 and 7 demonstrated potential anti-RA (rheumatoid arthritis) activity against RA-FLS cell line with IC50 values of 14.57 and 11.70 µM, respectively.

RBC membrane camouflaged prussian blue nanoparticles for gamabutolin loading and combined chemo/photothermal therapy of breast cancer.

Due to the non-targeted release of anti-cancer agent gamabufotalin (CS-6), conventional chemotherapy using this drug can cause serious side effects, which accordingly result in poor therapeutic efficiency. Recently, the development of smart nanodrug systems has attracted more and more attention due to their significant advantages of high loading efficiency, controllable release behavior and targeted accumulation at tumor sites. In this study, a nanodrug system named as HA@RBC@PB@CS-6 NPs (HRPC) was constructed. In this system, Prussian blue nanoparticles (PB NPs) with hollow porous structure were used as the carrier for CS-6 and photothermal sensitizer simultaneously. The result indicated that the encapsulation of erythrocyte membrane on the PB NPs prolonged the blood circulation life to 10 h and improved the immune evasion ability for more than 60%, as well, which is beneficial for the targeting molecule (HA) to achieve high concentration accumulation of HRPCs at tumor sites. Moreover, we also disclosed that loading drug of CS-6 performed its ultra-strong anti-tumor function partly through markedly suppressing the expression of HSP70, which conversely amplified the efficiency of photothermal therapy. The in vivo study demonstrated the outstanding performance of HRPC in synergistic photothermal/chemotherapy of cancer without side effect to normal tissues.

Two new alkaloids isolated from traditional Chinese medicine Binglang the fruit of Areca catechu.

Binglang, the fruit of Areca catechu L, has a long history as an important Chinese herbal medicine. Two new alkaloids (1 and 2), along with forty-one known compounds (3-43) were isolated from the dried fruit of Areca catechu L. The structures were elucidated on basis of the IR, UV, MS and 1D, 2D NMR spectroscopic data. Compounds 26 and 33 showed weak cytotoxicity against human gastric cancer cell line (BGC-823) with IC50 of 15.91 µM and 20.13 µM, respectively.

New Cadinane Sesquiterpenes from the Stems of Kadsura heteroclita.

As part of our continual efforts to exploit 'Tujia Ethnomedicine' for their pharmacophoric functionalities, we herein investigated Kadsura heteroclita collected from a deep Wulin mountain area in northern Hunan province. The current study resulted in the isolation of three new sesquiterpenes: 6α,9α,15-trihydroxycadinan-4-en-3-one (1), (+)-3,11,12-trihydroxycalamenene (2), (-)-3,10,11,12-tetrahydroxy-calamenene (3), along with four known sesquiterpenes (4-7), and a cytochalasin H (8). Their chemical structures were elucidated by 1D-, and 2D-NMR spectroscopy, and HRESI-MS, CD spectrometry. The antioxidant, and cytotoxic activities of the compounds were evaluated. Compound 8 exhibited a strong antioxidant effect with an IC50 value of 3.67 µM on isolated human polymorphonuclear cells or neutrophils.

Simultaneous Determination of 19 Bioactive Constituents in QishenYiqi Dropping Pills by Ultra-Performance Liquid Chromatography Coupled with Triple Quadrupole Mass Spectrometry.

Background: QishenYiqi dripping pills (QSYQ), consisting of Salvia miltiorrhiza, Astragalus membranaceus, Panax notoginseng, and Dalbergia odorifera, is a widely used to treat ischemic cerebrovascular and hemorrhagic cerebrovascular in China. Objective: In this study, a rapid and sensitive ultra-HPLC coupled with a triple quadrupole MS (UHPLC-QQQ-MS) method was established for the simultaneous quantification of 19 bioactive components. Methods: Chromatographic separation was performed on an Agilent Eclipse Plus C18 Rapid Resolution High Definition (RRHD) column (2.1 × 50 mm, 1.8 µm) with a mobile phase composed of a 0.1% (v/v) formic acid aqueous solution and acetonitrile in a gradient elution manner. A QQQ-MS was used in positive and negative ionization mode with multiple reactions monitoring for quantitative analysis. Results: The established methods were validated with linearity, precision, repeatability, stability, recovery, and matrix effect. All calibration curves exhibited excellent linear relationship with the correlation coefficient (r) >0.9985 for each analyte within the test range. This method was successfully applied to quantify target compounds of different structural types in 12 batches of QSYQ. Conclusions: The results suggest that the established method is rapid, sensitive, and reliable. The developed UHPLC-QQQ-MS method can provide scientific basis and reference to quality control and consistency evaluation of QSYQ sample and other formulations. Highlights: A rapid, sensitive, and reliable UHPLC-QQQ-MS method has been developed and validated for simultaneous determination of 19 compounds including phenolic acids, saponins, isoflavonoids, and tanshinones in QSYQ for the first time.

Lignans from Tujia Ethnomedicine Heilaohu: Chemical Characterization and Evaluation of Their Cytotoxicity and Antioxidant Activities.

Heilaohu, the roots of Kadsura coccinea, has a long history of use in Tujia ethnomedicine for the treatment of rheumatoid arthritis and gastroenteric disorders, and a lot of work has been done in order to know the material basis of its pharmacological activities. The chemical investigation led to the isolation and characterization of three new (1⁻3) and twenty known (4⁻23) lignans. Three new heilaohulignans A-C (1⁻3) and seventeen known (4⁻20) lignans possessed dibenzocyclooctadiene skeletons. Similarly, one was a diarylbutane (21) and two were spirobenzofuranoid dibenzocyclooctadiene (22⁻23) lignans. Among the known compounds, 4⁻5, 7, 13⁻15 and 17⁻22 were isolated from this species for the first time. The structures were established, using IR, UV, MS and NMR data. The absolute configurations of the new compounds were determined by circular dichroism (CD) spectra. The isolated lignans were further evaluated for their cytotoxicity and antioxidant activities. Compound 3 demonstrated strong cytotoxic activity with an IC50 value of 9.92 µM, compounds 9 and 13 revealed weak cytotoxicity with IC50 values of 21.72 µM and 18.72 µM, respectively in the HepG-2 human liver cancer cell line. Compound 3 also showed weak cytotoxicity against the BGC-823 human gastric cancer cell line and the HCT-116 human colon cancer cell line with IC50 values of 16.75 µM and 16.59 µM, respectively. A chemiluminescence assay for antioxidant status of isolated compounds implied compounds 11 and 20, which showed weak activity with IC50 values of 25.56 µM and 21.20 µM, respectively.