Quantification of tripdiolide in human whole blood by liquid chromatography coupled with atmospheric pressure chemical ionization tandem mass spectrometry

A liquid chromatographic-tandem mass spectrometric (LC-MS/MS) assay was developed and validated to determine tripdiolide in human whole blood using dexamethasone acetate as an internal standard (I.S.). Liquid-liquid extraction with ethyl acetate was used to isolate them from the biological matrix. Detection was performed on a mass spectrometer coupled with a negative atmospheric pressure chemical ionization (APCI) in the multiple-reaction monitoring (MRM) mode. The calibration curve was linear (r² = 0.9973) in the concentration range of 0.5-100.0 ng/mL in human whole blood with a lower limit of quantification of 0.5 ng/mL. Intra-day and inter-day relative standard deviations (R.S.D.s) were less than 7.0 and 10.1%, respectively. Extraction recoveries of tripdiolide ranged from 80.5 to 90.1%. This assay can be used to determine trace tripdiolide in human whole blood.     

Simultaneous Determination of Triptolide and Tripdiolide in Extract of Tripterygium wilfordii Hook. f. by LC–APCI-MS

A novel method using liquid chromatography coupled with atmospheric pressure chemical ionization mass spectrometry in the negative selected ion monitoring mode has been developed and validated for rapid simultaneous determination of triptolide and tripdiolide in the extract of Tripterygium wilfordii Hook. f. The molecular ions m/z [M–H]⁻ 359 and 375 were selected for the quantification in selected ion monitoring mode for triptolide and tripdiolide. Standard calibration curve was linear over the concentration range of 0.12–24 and 0.15–30 μg mL⁻¹ for triptolide and tripdiolide. The relative standard deviations of intra- and inter-day were in the range of 4.7–9.9 and 8.9–12.6%. The average recoveries were between 96.4 and 104.6%. The limits of quantitation were 2.0 × 10⁻³ and 2.5 × 10⁻³ μg mL⁻¹ for triptolide and tripdiolide.     

Gastroprotective Effects of Inulae Flos on HCl/Ethanol-Induced Gastric Ulcers in Rats

Inulae Flos, the flower of Inula britannica L., is used as a dietary supplement, beverage, and medicine in East Asia. In this study, we evaluated the gastroprotective effects of Inulae Flos extract (IFE) against gastric mucosal lesions induced by hydrochloric acid (HCl)/ethanol in rats and explored its potential mechanisms by measuring antioxidant enzyme activity, mucus secretion, and prostaglandin E₂ (PGE₂) levels. Pretreatment with IFE at doses of 100 and 300 mg/kg significantly inhibited gastric lesions in HCl/ethanol-treated rats. IFE increased the activities of superoxide dismutase and catalase and the levels of glutathione and PGE₂ in gastric tissues. The administration of IFE also significantly increased the gastric wall mucus contents in HCl/ethanol-induced gastric lesions. These findings suggest that IFE has gastroprotective effects against HCl/ethanol-induced gastric lesions and exerts these effects through increased antioxidant levels and gastric mucus secretion. Inulae Flos may be a promising agent for the prevention and treatment of gastritis and gastric ulcers.     

Active ingredients of Inula helenium L. exhibits similar anti-cancer effects as isoalantolactone in pancreatic cancer cells

Abstract

Isoalantolactone is one of the major active ingredients from Inula helenium L. However, it is low cost-effective to isolate isoalantolactone from Inula helenium L. In this study, we optimized the extraction strategy and obtained a mixture of active ingredients with exact proportion (termed as F35), which were alloalantolactone, alantolactone and isoalantolactone at the ratio of 1/5/4 respectively. The anti-tumor activity of F35 was compared with isoalantolactone on pancreatic cancer cells. As a result, F35 showed nearly the same anti-proliferation activity as isoalantolactone in two cell lines. Both F35 and isoalantolactone could induce mitochondrion-related apoptosis at the concentration of 6?μg/ml. In addition, F35 inhibited colony-formation and migration of PANC-1 and SW1990 cells. To conclude, F35 exhibited similar anti-proliferation and anti-migration effect as isoalantolactone on two pancreatic cancer cell lines, suggesting that alantolactone or alloalantolactone might have comparable anti-tumor effect as isoalantolactone.     

毛冬青总皂苷对大鼠脑缺血再灌注损伤的保护作用及血液微量元素影响

目的研究毛冬青总皂苷对脑缺血再灌注损伤的保护作用,并初步探讨其血液微量元素的影响。方法动物随机分为假手术组、模型组、毛冬青总皂苷(高、中、低)剂量组及阳性药物对照组,运用大鼠大脑中动脉栓塞,制作脑缺血再灌注损伤模型,缺血10 min后,给药组及阳性药物组于舌下静脉给予高、中、低剂量的毛冬青总皂苷及假手术组、模型组给予等体积的溶剂。缺血60 min再灌注24 h后,每组取8只大鼠断头取脑,TTC染色,测定脑梗死体积;取血,测定血液中3种微量元素Ca、Zn、Cu的含量。结果毛冬青总皂苷组与模型组相比,毛冬青总皂苷治疗组脑梗死体积减小,病理变化较轻;模型组与假手术组比较血液中Ca、Cu含量增加明显有统计学意义,Zn含量明显降低与假手术组比较有统计学意义(P0.05),毛冬青高、中、低剂量组与模型组比较Ca、Cu含量明显降低,Zn含量明显升高,而且呈明显的量效关系,与模型组比较有统计学意义(P0.05)。结论毛冬青总皂苷对脑缺血再灌注损伤具有一定的保护作用,其保护机制与毛冬青总皂苷抗氧化作用及增强氧自由基的清除有关。     

A Novel Diterpenoid,11—O—β—D—glucopyranosylneo—triptophenolide, from Tripterygium wilfordii Hook.f

A new diterpenoid was isolated from the ethanolic extract of the dried root bark of Tripterygium wilfordii Hook.f. It is the first example of abietane diterpenoid glycoside isolated from Tripterygium wilfordii Hook.f.Its structure was identified to be 11-0-β-D-glucopyranosyl-neotriptophenolide based on spectral methods.     

Antioxidant and antifungal activity of different extracts obtained from aerial parts of Inula crithmoides L.

The total phenolic content, antioxidant and antifungal activities of three Inula crithmoides extracts (n-hexane, methylene chloride and MeOH) were investigated. The methanolic extract showed the highest total phenolic content. In the DPPH assay, the methanolic and hexane extracts exhibited the highest DPPH-radical scavenging activity; in the 5-lipoxygenase assay, the hexane extract showed greater inhibitory effect with an IC₅₀ similar to that of Trolox and ascorbic acid. The antifungal activity of the methanolic extract revealed a higher activity against Phytophtora cryptogea and Alternaria solani.     

Antibacterial alkaloids from Artabotrys crassifolius Hook.f. & Thomson

Chloroform extract of bark of Artabotrys crassifolius Hook.f. & Thomson exhibited antibacterial activities against both American Type Culture Collection and clinical bacterial strains in vitro with zones of inhibition ranging from 7 to 14 mm. Further analysis of this extract yielded artabotrine, liridine, lysicamine and atherospermidine. Artabotrine displayed a broad array of antibacterial activity mostly against Gram-positive bacteria with minimum inhibitory concentration (MIC) values ranging from 1.25 μg/mL to 5 μg/mL. Of note, artabotrine, liridine and lysicamine are bactericidal against Gram-negative extended-spectrum beta-lactamase-producing Klebsiella with MIC values equal 2.5, 2.5 and 10 μg/mL, respectively, and minimum bactericidal concentrations values equal to 2.5, 5 and 20 μg/mL.     

Sesquiterpenoids from the Aerial Parts of Inula japonica

Fourteen sesquiterpenoids with an eudesmane C‐atom skeleton, including four new ones, (1β,5α,7β,8β,11β)‐5‐hydroperoxy‐1‐hydroxyeudesm‐4(15)‐eno‐12,8‐lactone ( 1 ), (1β,5α,7β,8β)‐8‐(acetyloxy)‐5‐hydroperoxy‐1‐hydroxycostic acid methyl ester ( 12 ), and a mixture of (1β,3β,4β,7β,8β)‐1,3‐dihydroxyeudesma‐5,11(13)‐dieno‐12,8‐lactone ( 7 ) and (1β,3β,4β,7β,8β,11β)‐1,3‐dihydroxyeudesm‐5‐eno‐12,8‐lactone ( 8 ), were isolated from the aerial parts of Inula japonica (Asteraceae). Their structures were determined by extensive spectroscopic methods, and those of 7 and 12 confirmed by means of single‐crystal X‐ray diffraction analysis.     

Acidic isomerization of alantolactone derivatives

A series of derivatives of the natural sesquiterpene lactones alantolactone (1) and isoalantolactone (2) was prepared. The α-methylene-γ-lactone moiety was retained in the structures of these for further modifications using reactions that affected exclusively the nonconjugated double bonds of the decalin ring. __________ Translated from Khimiya Prirodnykh Soedinenii, No. 4, pp. 325–330, July–August, 2006.