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Theasaponin derivatives, which are reported to exert antitumor activity, have been widely reported to exist in edible plants, including in the seed cake of Camellia oleifera (C.), which is extensively grown in south of China. The purpose of this study was to isolate new theasaponin derivatives from C. seed cake and explore their potential antitumor activity and their underlying molecular mechanism. In the present study, we first isolated and identified four theasaponin derivatives (compounds 1, 2, 3, and 4) from the total aglycone extract of the seed cake of Camellia oleifera by utilizing a combination of pre-acid-hydrolysis treatment and activity-guided isolation. Among them, compound 1 (C1) and compound 4 (C4) are newly discovered theasaponins that have not been reported before. The structures of these two new compounds were characterized based on comprehensive 1D and 2D NMR spectroscopy and high-resolution mass spectrometry, as well as data reported in the literature. Secondly, the cytotoxicity and antitumor property of the above four purified compounds were evaluated in selected typical tumor cell lines, Huh-7, HepG2, Hela, A549, and SGC7901, and the results showed that the ED50 value of C4 ranges from 1.5 to 11.3 µM, which is comparable to that of cisplatinum (CDDP) in these five cell lines, indicating that C4 has the most powerful antitumor activity among them. Finally, a preliminary mechanistic investigation was performed to uncover the molecular mechanism underlying the antitumor property of C4, and the results suggested that C4 may trigger apoptosis through the Bcl-2/Caspase-3 and JAK2/STAT3 pathways, and stimulate cell proliferation via the NF-κB/iNOS/COX-2 pathway. Moreover, it was surprising to find that C4 can inhibit the Nrf2/HO-1 pathway, which indicates that C4 has the potency to overcome the resistance to cancer drugs. Therefore, C1 and C4 are two newly identified theasaponin derivatives with antitumor activity from the seed cake of Camellia oleifera, and C4 is a promising antitumor candidate not only for its powerful antitumor activity, but also for its ability to function as an Nrf2 inhibitor to enhance the anticancer drug sensitivity. [ABSTRACT FROM AUTHOR]

Twelve novel cordycepin derivatives were designed and synthesized with modification at positions of 2′, 5′-hydroxyl and N6 amino groups of cordycepin. The results showed that the inhibitory activities of 3, 4b, 6c and 6d on A549 were comparable to the positive control gefitinib, and the inhibitory activity of 6a on A549 was better than that of gefitinib. Also, the inhibitory activities of twelve cordycepin derivatives against E. coli 1924, S. aureus 4220 and S. mutans 3289 were studied. Among them, 4b showed certain inhibitory on S. mutans 3289, while 6b showed certain inhibition on S. aureus 4220. [ABSTRACT FROM AUTHOR]

Four new lignans named cephaliverins A-D (1-4), along with seven known analogues (5-11), were isolated from Cephalotaxus oliveri Mast. Their structures were elucidated on the basis of HR-ESI-MS and NMR analyses, and their absolute configurations were determined by ECD comparison. Cephaliverin A (1), herpetotriol (5) and hedyotol A (6) exhibited moderate antitumor activity against HepG2 and A549 cell lines., Competing Interests: Declaration of competing interest The authors declare that they have no conflicts of interest., (Copyright © 2024. Published by Elsevier B.V.)

Summary Purpose This phase 1a, first-in-human study assessed the safety, maximum tolerated dose (MTD), pharmacokinetics (PK), and antitumor activity of FCN-437c, a cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor. Methods The study enrolled female patients with HR + /HER2- advanced breast cancer (BC) who failed standard of care therapy. A 3 + 3 dose-escalation design was utilized with a starting dose of 50 mg daily for 3 weeks on and 1 week off treatment in 28-day cycles. Patients received escalating doses of FCN-437c monotherapy (50, 100, 200, 300, and 450 mg). Results Seventeen patients received FCN-437c 50 mg (n = 3), 100 mg (n = 3), 200 mg (n = 3), 300 mg (n = 6), and 450 mg (n = 2). Two patients who received the 450-mg dose experienced dose-limiting toxicities (DLTs; grade 4 thrombocytopenia and neutropenia); no DLT was observed at any other dose level. Frequently reported treatment-emergent adverse events (TEAEs) of any grade were hematological: leukopenia (94.1%), neutropenia (88.2%), anemia (64.7%), and thrombocytopenia (47.1%). Grade 3–4 TEAEs included neutropenia (64.7%) and leukopenia (47.1%). Exposure of FCN-437c increased almost proportionally to doses ranging from 50 to 200 mg. At doses from 200 to 450 mg, there appeared to be a trend of saturation. The MTD was determined to be 300 mg. Of 15 patients with measurable disease, nine (60.0%) patients experienced stable disease; no complete or partial responses were observed. Conclusions These results established an acceptable safety profile for FCN-437c in patients with advanced BC, and there were no unexpected signals relative to other CDK4/6 inhibitors. (NCT04488107; July 13, 2020) [ABSTRACT FROM AUTHOR]

Sugarcane leaves have been extensively consumed as a herbal tea for centuries in China, which is an economically important crop containing multiple health benefits. Here we report the structure and in vitro antitumor activity of a purified sugarcane leaf polysaccharide (SLP70–1). SLP70–1 is a homogeneous heteropolysaccharide made up of mannose, glucose, and galactose with a molar ratio of 1.00: 1.89: 2.83. Additionally, the molecular weight of SLP70–1 was 3.23 kDa. Linkage together with NMR examination demonstrated the structural foundation of SLP70–1 were consisted of →4)- α -D-Gal p -(1→, →4)- α -D-Glc p -(1→, →2)- β -D-Man p -(1→, →3)- β -D-Gal p -(1→, →4,6)- β -D-Gal p -(1→, →6)- α -D-Gal p -(1→, →3,6)- α -D-Glc p -(1→ and α -D-Glc p -(1→，and the side chain was confirmed to be →4)- α -D-Glc p -(1→ and →6)- α -D-Gal p -(1→. According to an in vitro cell experiment, SLP70–1 could markedly decrease the survival ability of cancer cells exhibiting concentration dependence, including the survival rate of cancer cells in the lungs, colon, cervix, kidney, and breast, implying potent antitumor activity. In summary, SLP70–1 exhibits features that qualify it as a promising antitumor adjuvant candidate. • A novel polysaccharide SLP70-1 was obtained from sugarcane leaves. • The glycosidic bond types and linkage patterns were successfully clarified. • SLP70-1 exhibited a certain antitumor effect in vitro. • The underlying structure-function relationship was elucidated. [ABSTRACT FROM AUTHOR]

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A new bis-γ-pyrone polypropionate compound onchidione II (1), together with three known compounds, was isolated from a marine pulmonate mollusc Onchidium struma, collected at Hainan Island of China. The structure of new compound was determined by extensive spectroscopic analyses including IR, 1D and 2D NMR techniques, and chemical methods. Compounds 1–4 were evaluated for their cytotoxicity against human tumor cell lines HepG-2, A549, and MCF-2. The results showed that compounds 1 and 2 were moderate cytotoxic against HepG-2, A549, and MCF-2 cell lines, with IC50 values from 13.2 to 22.4 μM. [ABSTRACT FROM AUTHOR]

Two new highly functionalized cembrane diterpenoids named ximaolobophytolides A (1) and B (2) as minor components, together with seven related known compounds (3-9), have been isolated and identified from the Ximao soft coral Lobophytum sp. They were characterized by the presence of an α-methylene-γ-lactone moiety. Based on the comprehensive analyses of 1D and 2D NMR spectroscopic data, the absolute configurations of these two new compounds were elucidated by the combination of quantum mechanical (QM)-NMR and time-dependent density functional theory/electronic circular dichroism (TDDFT-ECD) calculation approaches. In the anti-tumor bioassays, compounds 3-9 showed moderate to significant inhibitory effects (IC 50 values ranging from 29.66 to 0.39 μM) against the proliferations of five tumor cells HEL, A549, H1975, MDA-MB-231, and H1299. It might be worthy to point out that compounds 4, 7, and 8 exhibited better anti-tumor activities than that of the positive control Doxorubicin., (© 2023 Wiley-VHCA AG, Zurich, Switzerland.)

Perilla frutescens var. frutescens is an economically important crop—a widely used herb that has been cultivated in China for over 2000 years. A novel polysaccharide (PFP) was extracted from P. frutescens var. frutescens and purified by the Sevag method and Sephadex G-200 gel chromatography. Its structural characteristics and antitumor activity were investigated. Total sugar, uronic acid, and protein contents in PFP were 89.73%, 8.93%, and 1.56%, respectively, and its molecular weight was 1.18 × 106 Da. FT-IR, ion chromatography and NMR showed that PFP was a pyranose consisting primarily of rhamnose, arabinose, galactose, glucose, xylose, and galacturonic acid, at molar ratios of 0.13: 0.55: 1.40: 1.00: 0.13: 0.22 with α- and β-type glycosidic residues, its main chain may consists by α- L -Ara f -(1→, →6)-β- D -Gal p -(1→, →4)-α- D -Glc p -(1→, →1,4)-β- D -Xyl p (1→, →4)-α-Gal p A-(1→, →2,4)-α- L -Rha p -(1→. PFP inhibited tumor proliferation and reduced mitochondrial membrane potential in vivo in H22 tumor-bearing mice by blocking the cell cycle S phase. PFP also exhibited protective effects on mouse liver and thymus tissues. These findings provide a theoretical basis for the development of safe and effective natural anti-liver cancer drugs from novel polysaccharides produced by PFP. • Perilla frutescens var. frutescens is a medicinal and edible plant with bioactivity. • A novel polysaccharide (PFP) was isolated from this herb. • PFP protects the murine immune organs and has antitumor effects in vivo. • PFP induces cell apoptosis and cell cycle arrest in mice. • P. frutescens var. frutescens may be a source of natural anticancer drugs. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance Sophora flavescens (Fabaceae), also known as Kushen (Chinese: 苦参), has been an important species in Chinese medicine since the Qin and Han dynasties. The root of Sophora flavescens has a long history in the traditional medicine of many countries, including China, Japan, Korea, India and some countries in Europe. In traditional Chinese medicine (TCM), Sophora flavescens has been used extensively, mainly in combination with other medicinal plants in prescriptions to treat fever, dysentery, hematochezia, jaundice, oliguria, vulvar swelling, asthma, eczema, inflammatory disorders, ulcers and diseases associated with skin burns. The aim of this review is to provide updated and comprehensive information regarding the botany, ethnopharmacology, phytochemistry, biological activities and toxicology of Sophora flavescens and to discuss possible trends and opportunities for further research on Sophora flavescens . Materials and methods We systematically searched major scientific databases (PubMed, Elsevier, SpringerLink, Google Scholar, Medline Plus, ACS, “ Da Yi Yi Xue Sou Suo ( http://www.dayi100.com/login.jsp )”, China Knowledge Resource Integrated (CNKI) and Web of Science) for information published between 1958 and 2015 on Sophora flavescens . Information was also acquired from local classic herbal literature, conference papers, government reports, and PhD and MSc dissertations. Results The broad spectrum of biological activities associated with Sophora flavescens has been considered a valuable resource in both traditional and modern medicine. Extracts are taken either orally or by injection. More than 200 compounds have been isolated from Sophora flavescens , and the major components have been identified as flavonoids and alkaloids. Recent in vitro and in vivo studies indicate that at least 50 pure compounds and crude extracts from Sophora flavescens possess wide-ranging antitumor, antimicrobial, antipyretic, antinociceptive, and anti-inflammatory pharmacological abilities. The anticancer and anti-infection abilities of these components are especially attractive areas for research. Conclusions Sophora flavescens is a promising traditional medicine, but there is a need for more precise studies to test the safety and clinical value of its main active crude extracts and pure compounds and to clarify their mechanisms of action. Moreover, some existing studies have lacked systematic methods and integration with the existing literature, and some of the experiments were isolated, used small sample sizes and were unreliable. More validated data are therefore required. [ABSTRACT FROM AUTHOR]

Abstract: Eclipta prostrata L., (Asteraceae), is used in China for both food and medicine purposes. This research is concerned with the isolation and purification of phytochemical constituents from the aerial parts of E. prostrata, using gradient solvent fractionation, macroporous resin, silica gel, Sephadex LH-20 and ODS columns, and TLC analyses. Four fractions (water, 30% ethanol, 60% ethanol and 90% ethanol) were obtained. Four compounds, wedelolactone (I), eclalbasaponin I (II), luteolin (III) and luteolin-7-O-glucoside (IV) were purified and their structures were identified by the interpretation of spectroscopic analyses including MS, 1H and 13C NMR. Antitumor activities of extracts (total fraction), four fractions and the isolated compounds were assessed using hepatoma cell smmc-7721 as an in vitro assay system. The 30% ethanol fraction and eclalbasaponin I dose-dependently inhibited the proliferation of hepatoma cell smmc-7721 with IC50 values of 74.2399 and 111.1703μg/ml, respectively, more strongly compared with 5-fluorouracil positive control group with the IC50 value of 195.3131μg/ml. Antitumor activities of other fractions and compounds were lower than positive control. These results suggested that some specific compounds or extracts from E. prostrata are potential sources of natural anti-tumor materials and worthy of further study. [Copyright &y& Elsevier]

A new bisamide N1-acetyl-N7-phenylacetyl cadaverine (1) and a series of diketopiperazines including a new diketopiperazine cyclo(2-hydroxy-Pro-R-Leu) (2), together with a new natural product cyclo(4-hydroxy-S-Pro-S-Trp) (3) and two known leucine-based diketopiperazines cyclo(4-hydroxy-R-Pro-S-Leu) (4) and cyclo (S-Pro-R-Leu) (5), were isolated from ethyl acetate extract of a fermentation broth of a marine-derived Streptomyces sp. Their structures were elucidated by the interpretation of spectroscopic analysis. The antitumor activities of compounds 1–3 against HL-60 cell lines were tested by MTT assay. [ABSTRACT FROM AUTHOR]

Abstract: A water-soluble polysaccharide LT1 was isolated from the basidiocarps of Lentinus edodes by hot water extraction and ethanol precipitations, further purified by gel chromatography. The Mw of LT1 was estimated to be 642kDa by using HPGPC. Chemical and spectroscopic studies illustrated that LT1 has a backbone chain composed of 1→4-linked and 1→3-linked glucopyranosyl residues and has branches of single glucosyl stubs at C-6 of β-(1→4)-linked glucopyranosyl. AFM and Congo-red test revealed that LT1 existed as triple helix chain in 0.10M NaOH solution or distilled water. Our studies showed that LT1 presented significant antitumor bioactivities on Sarcoma180 solid tumor cell implanted in BALB/c mice, which implies that LT1 could be potentially applied as a natural antitumor drug. [Copyright &y& Elsevier]

Cancer is a serious threat to human health. With the increasing resistance to known drugs, it is still urgent to find new drugs or pro-drugs with anti-tumor effects. Natural products produced by microorganisms have played an important role in the history of drug discovery, particularly in the anticancer and anti-infective areas. The plant rhizosphere ecosystem is a rich resource for the discovery of actinomycetes with potential applications in pharmaceutical science, especially Streptomyces. We screened Streptomyces-like strains from the rhizosphere soil of wheat (Triticum aestivum L.) in Hebei province, China, and thirty-nine strains were obtained. Among them, the extracts of 14 isolates inhibited the growth of colon tumor cell line HCT-116. Strain NEAU-wh-3-1 exhibited better inhibitory activity, and its active ingredients were further studied. Then, 16S rRNA gene sequence similarity studies showed that strain NEAU-wh3-1 with high sequence similarities to Embleya scabrispora DSM 41855T (99.65%), Embleya hyalina MB891-A1T (99.45%), and Streptomyces lasii 5H-CA11T (98.62%). Moreover, multilocus sequence analysis based on the five other house-keeping genes (atpD, gyrB, rpoB, recA, and trpB) and polyphasic taxonomic approach comprising chemotaxonomic, phylogenetic, morphological, and physiological characterization indicated that the isolate should be assigned to the genus Embleya and was different from its closely related strains, therefore, it is proposed that strain NEAU-wh3-1 may be classified as representatives of a novel species of the genus Embleya. Furthermore, active substances in the fermentation broth of strain NEAU-wh-3-1 were isolated by bioassay-guided analysis and identified by nuclear magnetic resonance (NMR) and mass spectrometry (MS) analyses. Consequently, one new Zincophorin analogue together with seven known compounds was detected. The new compound showed highest antitumor activity against three human cell lines with the 50% inhibition (IC50) values of 8.8–11.6 μg/mL and good antibacterial activity against four pathogenic bacteria, the other known compounds also exhibit certain biological activity. [ABSTRACT FROM AUTHOR]

Bufo gargarizans (Cantor, 1842) (BGC), a traditional medicinal animal distributed in many provinces of China, is well known for the pharmaceutical value of Chansu and Chanpi. As traditional Chinese medicines (TCMs), Chansu and Chanpi, with their broad-spectrum of therapeutic applications, have long been applied to detoxification, anti-inflammation, analgesia, etc. We critically analyzed the current evidence for the traditional uses, chemical profiles, pharmacological activity, toxicity and quality control of BGC (Bufonidae family) to provide a scientific basis for future in-depth studies and perspectives for the discovery of potential drug candidates. All of the available information on active constituents and TCMs derived from BGC was obtained using the keywords " Bufo gargarizans ", "Chansu", "Chanpi", "Huachansu", or "Cinobufacini" through different electronic databases, including PubMed, Web of Science, Chinese National Knowledge Infrastructure (CNKI), the Wanfang Database, and Pharmacopoeia of China. In addition, Chinese medicine books from different times were used to elucidate the traditional uses of BGC. Electronic databases, including the "IUCN Red List of Threatened Species", "American Museum of Natural History" and "AmphibiaWeb Species Lists", were used to validate the scientific name of BGC. To date, about 118 bufadienolide monomers and 11 indole alkaloids have been identified from BGC in total. The extracts and isolated compounds exhibit a wide range of in vitro and in vivo pharmacological effects. The literature search demonstrated that the ethnomedicinal uses of BGC, such as detoxification, anti-inflammation and the ability to reduce swelling and pain associated with infections, are correlated with its modern pharmacological activities, including antitumor, immunomodulation and attenuation of cancer-derived pain. Bufadienolides and indole alkaloids have been regarded as the main active substances in BGC, among which bufadienolides have significant antitumor activity. Furthermore, the cardiotoxicity of bufadienolides was discussed, and the main molecular mechanism involves in the inhibition of Na+/K+-ATPase. Besides, with the development of modern analytical techniques, the quality control methods of BGC-derived TCMs are being improved constantly. An increasing number of reports suggest that BGC can be regarded as an excellent source for exploring the potential antitumor constituents. However, the future antitumor research of BGC needs to follow the standard pharmacology guidelines, so as to provide comprehensive pharmacological information and aid the reproducibility of the data. Besides, to ensure the efficacy and safety of BGC-derived TCMs, it is vital to construct a comprehensive quality evaluation model on the basis of clarifying pharmacodynamic-related and toxicity-related compositions. Image 1 [ABSTRACT FROM AUTHOR]

In this research, a novel polysaccharide (PCP) was extracted from Pleurotus citrinopileatus and purified by Sephadex G-150 gel column, and its antitumor activity was investigated using the model H22 tumor-bearing mice. PCP was found to be composed of arabinose, galactose, glucose, xylose, mannose and glucuronic acid in a proportion of 0.66: 14.59: 10.77: 1: 0.69: 0.23 with average molecular weight of 7.30 × 10 5  Da. Further analysis suggested that PCP was a pyranose with α-type and β-type glycosidic residues. The antitumor assays in vivo indicated that PCP could effectively suppress H22 solid tumor growth, protect immune organs and improve inflammation and anemia. Besides, Annexin V-FITC/PI double staining and JC-1 staining demonstrated that PCP could induce apoptosis of H22 hepatoma cells. The PI staining assay revealed that PCP induced H22 hepatoma cells apoptosis by arresting cell cycle in S phase. These results suggest that the polysaccharide from Pleurotus citrinopileatus possesses potential value in the treatment of liver cancer., Competing Interests: Declaration of competing interest The authors confirm that this article content has no conflict of interest, (Copyright © 2020 Elsevier B.V. All rights reserved.)

Previous studies have shown that crude polysaccharides from the Lycium barbarum fruit could inhibit cancer cell growth, but the major effective constituents are yet to be identified. In this study, we compared the effects of L. barbarum fruit polysaccharide fractions on the growth of hepatoma cells (SMMC-7721 and HepG2), cervical cancer cells (HeLa), gastric carcinoma cells (SGC-7901), and human breast cancer cells (MCF-7). LBGP-I-3 showed stronger inhibitory effects on MCF-7 cells (cell viability of 48.96%) than SMMC-7721 (cell viability of 78.91%) and HeLa cells (cell viability of 55.94%), and had no effect on HepG2 and SGC-7901 cells. In addition, LBGP-I-3 had no inhibitory effect on normal liver cells (L02, cell viability of 115.58%). Investigation of the underlying mechanism suggested that LBGP-I-3 inhibited the growth of cancer cells by cell cycle arrest and apoptosis. LBGP-I-3 arrested the cell cycle at the G0/G1 phase, altered mitochondrial function, activated oxidative stress, and regulated the MAPK signaling pathway to induce apoptosis. Thus, LBGP-I-3 may be a potential functional food ingredient for the prevention of cancer without toxicity to normal cells in vitro. These results could help further elucidate the structure-activity relationship of L. barbarum fruit polysaccharides and functional food development., Competing Interests: Declaration of competing interest There are no conflicts to declare., (Copyright © 2020 Elsevier B.V. All rights reserved.)