Naisheng Bai

Ent-kaurane diterpenoids from Rabdosia rubescens and their cytotoxic effects on human cancer cell lines

Two new ent-kaurane diterpenoids, 16,17-exo-epoxide-oridonin ( 1) and 11,15- O,O-diacetyl-rabdoternins D ( 2), together with thirteen known ones, were isolated from the aerial parts of Rabdosia rubescens. Their structures were established on the basis of high-field 1D and 2D NMR methods supported by HRMS. All diterpenoids were tested for cytotoxicity against human Hep G2, COLO 205, MCF-7, and HL-60 cancer cells. The compounds oridonin ( 3), 14- O-acetyl-oridonin ( 4), 1,14- O,O-diacetyl-oridonin ( 5), rosthorin ( 6), effusanin E ( 7), and ponicidin ( 8), as well as six alpha-methylene gamma-ketone bearing diterpenoids, were modestly active in these assays.

Importance of extract standardization and in vitro/ex vivo assay selection for the evaluation of antioxidant activity of botanicals: a case study on three Rosmarinus officinalis L. extracts.

The overproduction of free radicals and oxygen reactive species is suspected to be implicated in a wide range of metabolic reactions that can have pernicious consequences in the development of a variety of human diseases. Botanical extracts are sources of antioxidants that counteract both free radicals and oxygen reactive species. The processing conditions used in the botanical extraction may influence the antioxidant composition; therefore, different extracts from the same plant may have different antioxidant properties. To illustrate this fact, we conducted a study using three commercial rosemary (Rosmarinus officinalis L.) leaf extracts. The three extracts were standardized to contain, respectively, 20% carnosic acid, 40% ursolic acid, or 20% rosmarinic acid. They were evaluated for their total (hydrophilic + lipophilic) antioxidant effects on oxygen radical absorbance capacity (ORAC), their ferric reducing/antioxidant power (FRAP), and their capacity to inhibit Cu(2+)-induced low-density lipoprotein (LDL) oxidation ex vivo. The ursolic acid extract showed the lowest antioxidant capacity on all models. The rosmarinic acid extract had an antioxidant capacity 1.5 times higher on ORAC and four times higher on FRAP than the carnosic acid extract. However, the carnosic acid extract was better than the rosmarinic acid extract in inhibiting the oxidation of LDL ex vivo. These results encourage conducting further studies to evaluate the carnosic acid and rosmarinic acid extracts in vivo. Our study offers an example of the importance of the extraction procedures, on which depends the nature of the antioxidant composition, and highlights interest to proceed with in vitro/ex vivo assay selection for the evaluation of the antioxidant properties of botanical extracts.

Acute effects of Fraxinus excelsior L. seed extract on postprandial glycemia and insulin secretion on healthy volunteers

AIM OF THE STUDY Fraxinus excelsior L. (Family: Oleaceae) seeds are consumed as a food, condiment, and folk medicine. The seeds are traditionally used as a potent hypoglycemic agent, but no clinical evidence exists in as to this regard. We assessed the clinical efficacy and safety of the seed extract (FraxiPure, Naturex), containing 6.8% of nuzhenide and 5.8% of GI3 (w/w), on plasma glucose and insulin levels against glucose (50 g) induced postprandial glycemia. MATERIALS AND METHODS Preselected dose (1.0 g) was used in a double blind, randomized, crossover, placebo (wheat bran) controlled study on 16 healthy volunteers. Each treatment was given immediately after a fasting blood glucose sample (0 min). Postprandial plasma glucose levels were estimated at 0, 15, 30, 45, 60, 90 and 120 min; and postprandial plasma insulin at 0, 30, 60, 90 and 120 min. RESULTS The extract lowered the incremental postprandial plasma glucose concentration as compared to placebo at 45 min (P = 0.06) and 120 min (P = 0.07). It statistically (P = 0.02) reduced the glycemic area under the blood glucose curve. The seed, also, induced a significant (P = 0.002) secretion of insulin at 90 min after glucose administration. However, the insulinemic area under the blood insulin curve was not different than the placebo. No adverse events were reported. CONCLUSIONS Our findings confirm the hypoglycemic action of Fraxinus excelsior L. seed extract. These promising results, thus, encourage conducting long-term clinical studies to further evaluate the efficacy and safety of Fraxinus excelsior L. seed extract in healthy and diabetic volunteers and also to explore the possible mechanism(s) of action.

Fraxinus excelsior seed extract FraxiPure™ limits weight gains and hyperglycemia in high-fat diet-induced obese mice

PURPOSE The aim of this study was to determine whether a Fraxinus excelsior L. seed extract, FraxiPure™ (0.5% in the diet), limits weight gain and hyperglycemia in mice. In a previous report, we identified several secoiridoids in FraxiPure™, some of which activated peroxisome proliferator-activated receptor alpha (PPARα) in vitro and inhibited the differentiation of 3T3-L1 preadipocyte cells. In a separate study, FraxiPure™ reduced glycemia in healthy volunteers, following an oral glucose tolerance test. These findings suggest that FraxiPure™ has antiobesity and antihyperglycemia effects. MATERIALS AND METHODS FraxiPure™ was tested in mice that were fed a high-fat diet over 16 weeks and compared with low-fat and high-fat diet controls. Weight gain, omental and retroperitoneal fat, fasting blood glucose, and fasting blood insulin were measured. RESULTS FraxiPure™ reduced gains in body weight by 32.30% (p < 0.05), omental fat by 17.92%, and retroperitoneal fat by 17.78%. FraxiPure™ also lowered fasting blood glucose levels by 76.52% (p < 0.001) and plasma insulin levels by 53.43% (p < 0.05) after 16 weeks. Moreover, FraxiPure™ lowered liver weight gains by 63.62% (p < 0.05) and the incidence of fatty livers by 66.67%. CONCLUSIONS Our novel results demonstrate the antiobesity effects of chronic administration of an F. excelsior seed extract and confirm its ability to regulate glycemia and insulinemia. In addition, this extract, which is rich in secoiridoid glucosides, protects against obesity-related liver steatosis.

Characterization of nine polyphenols in fruits of Malus pumila Mill by high-performance liquid chromatography

Polyphenols are important bioactive substances in apple. To explore the profiles of the nine representative polyphenols in this fruit, a high-performance liquid chromatography method has been established and validated. The validated method was successfully applied for the simultaneous characterization and quantification of these nine apple polyphenols in 11 apple extracts, which were obtained from six cultivars from Shaanxi Province, China. The results showed that only abscission of the Fuji apple sample was rich in the nine apple polyphenols, and the polyphenol contents of other samples varied. Although all the samples were collected in the same region, the contents of nine polyphenols were different. The proposed method could serve as a prerequisite for quality control of Malus products.

Synthesis and Evaluation of a Series of Oleanolic Acid Saponins as α‐Glucosidase and α‐Amylase Inhibitors

Sixteen naturally occurring oleanolic acid saponins and their derivatives were synthesized in an efficient and practical strategy, and their inhibitory activities against α‐glucosidase and α‐amylase were evaluated in vitro. Among all the compounds, 28‐O‐monoglucoside 8 exhibited remarkably potent inhibitory activity against α‐glucosidase with an IC50 value of 87.3 µM, which was fivefold stronger than that of the antidiabetic acarbose. Based on the preliminary structure–activity relationships, for 28‐O‐monoglucosides, the presence of a terminal α‐l‐rhamnopyranosyl residue enhanced the α‐glucosidase and α‐amylase inhibitory activities. Furthermore, for 3,28‐O‐bidesmosides, sugar‐substituted moieties attached to the C‐3 and C‐28 positions of the oleanolic acid scaffold are helpful to increase the inhibitory activities against α‐amylase and α‐glucosidase.

Hepatoprotective standardized EtOH–water extract from the seeds of Fraxinus rhynchophylla Hance

Fraxinus rhynchophylla Hance (Oleaceae), its stem barks are known as Cortex fraxini (秦皮 qín pí) listed in Chinese Pharmacopoeia. Phytochemical study has indicated that methanol extracts from Qinpi has protective effect on acute liver injury. The present study investigates the hepatoprotective activity of EtOH–water extract from the seeds of F. rhynchophylla Hance against carbon tetrachloride-induced liver injury in mice. The EtOH–water extract significantly alleviated liver damage as indicated by the decreased levels of serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST), the malondialdehyde (MDA) content, and increased the levels of superoxide dismutase (SOD), glutathione (GSH) and glutathione peroxidase (GSH-Px), and reduced the pathological tissue injury induced by CCl4. Quantitative analysis of seven major constituents (1–7) in EtOH–water extract (EWE) was developed by high performance liquid chromatography-diode-array detector (HPLC-DAD). The current research indicates that the EWE from the seeds of F. rhynchophylla Hance decreased liver index, inhibited the increase of serum aminotransferase induced by CCl4, and decreased hepatic MDA content, SOD and GSH-Px activities. These results suggested that the pretreatment with EWE protected mice against CCl4-induced liver injuries. Based on the results, the EtOH–water extract from the seeds of F. rhynchophylla Hance is efficacious for prevention and treatment of CCl4-induced hepatic injury in mice. Secoiridoid and tyrosol glucosides might be the active ingredients responsible for the biological and pharmacological activities of hepatoprotection.

Qualitative and quantitative analysis of chemical constituents of Ptychopetalum olacoides Benth

Abstract Ptychopetalum olacoides is a folk medicinal plant for health care in market, especially in Brazil. Fourteen known compounds were isolated from P. olacoides and their chemical structures were elucidated by extensive spectroscopic data, including 1D NMR, 2D NMR, UV, IR and HR-ESI-MS. The 14 known compounds were identified as N-trans-feruloyl-3,5-dihydroxyindolin-2-one (1), magnoflorine (2), menisperine (3), 4-coumaroylserotonin (4), moschamine (5), luteolin (6), 4′-methoxyluteolin (7), 3-methoxyluteolin (8), 3, 7-dimethoxyluteolin (9), caffeic acid (10), ferulic acid (11), vanillic acid (12), syringic acid (13) and ginsenoside Re (14). To our knowledge, compounds (1–6, 13–14) were isolated from the plant for the first time. Additionally, quantitative analysis results indicated that calibration equations of compounds (1–3, 6, 9, 11–13) exhibited good linear regressions within the test ranges (R2 ≥ 0.9990) and magnoflorine and menisperine were the major constituents in the barks of P. olacoides. The contents of magnoflorine and menisperine accounted for 75.96% of all analytes. However, the content of phenolic components was smaller and the highest content was no more than 1.04 mg/g. Collectively, these results suggested that alkaloids are the dominant substances in P. olacoides, which can make a difference for the quality control and further use of P. olacoides.

A new sesquiterpene lactone glucoside and other constituents from Inula salsoloides with insecticidal activities on striped flea beetle (Phyllotreta striolata Fabricius)

Abstract A new sesquiterpene, eupatolide 13-O-β-d-glucopyranoside (eupatolide-II, 1), lactone glucoside, along with 15 known compounds, were isolated from the whole plant of Inula salsoloides (Asteraceae). Dichloromethane extract and compounds 1–11 were used to investigate insecticidal activities against vegetable important pest, striped flea beetle (Phyllotreta striolata Fabricius). None of the samples show any toxicity under concentration of 500 times, while compound 1 and the extract had toxic effect when the concentration increased to 250 times. But the corrected mortality of compound 1 and the extract were only 44.83 and 13.80%, respectively. Compound 11 (inulasalene) showed repellency effect in the no-choice test, and the repellency rate was 70%. Compounds 1 and 3 (inulasalsolide) showed the antifeeding rates of 65.22 and 47.06%, respectively. Compound 10 (11β,13-dihydrogeneupatolide) showed strong attractive effects on the adults, while the difference of injured area between the treatment and control was also not significant.

Characteristic Components, Biological Activities and Future Prospective of Fructus Mori: a Review

Purpose of ReviewChina has a long history in planting mulberry with the most varieties and the largest production in the world. This article provides a brief overview of an important edible fruit and traditional medicine in China—Fructus Mori (FM, mulberry fruit or Morus alba L. fruit), including the main chemical constituents, major bioactivities and the future prospective.Recent FindingsPhytochemical studies have revealed that Fructus Mori contains a great diversity of nutritive compounds such as organic acids, amino acids, vitamins, minerals, and bioactive components, including polysaccharides, polyphenolics, anthocyanins, flavonoids, alkaloids, stilbenes, and diels-alder type adducts. Besides, the extracts and active components of FM were reported to have numerous biological activities, including antioxidant, antihyperglycemic, antitumor, hepatoprotective, and neuroprotective activities in in vitro and in vivo studies.SummaryThis review provides recent findings systematically regarding the structural characteristics and biological activities of FM, which may be useful for stimulating deep research of therapeutic potentials and for predicting their uses as important and safe functional foods to benefit human health.