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C26H21Cl2F3N4O, monoclinic, Pc (no. 7), a = 21.218(6) Å, b = 5.9599(16) Å, c = 9.439(3) Å, β = 99.295(3)°, V = 1177.9(5) Å3, Z = 2, Rgt(F) = 0.0471, wRref(F2) = 0.1282, T = 296(2) K.

C20H24O10, orthorhombic, P212121 (no. 19), a = 6.3728(6) Å, b = 14.3835(14) Å, c = 20.453(2) Å, V = 1874.8(3) Å3, Z = 4, Rgt(F) = 0.0272, wRref(F2) = 0.0558, T = 296(2) K.

Two new C13-norsesquiterpenes claulanterpene A (1) and B (2), together with two known sesquiterpenes (3–4), were isolated from methanol extract of the stem and leaf of Clausena lansium collected from Qingyuan county, Guangdong Province, China. Their structures were elucidated on the base of extensive spectroscopic analysis and comparison with data reported in the literature. Among them, compound 4 showed antibacterial activity against Bacillus cereus. [ABSTRACT FROM AUTHOR]

C26H21Cl2F3N4O, monoclinic, Pc (no. 7), a = 21.218(6) Å, b = 5.9599(16) Å, c = 9.439(3) Å, β = 99.295(3)°, V = 1177.9(5) Å3, Z = 2, Rgt(F) = 0.0471, wRref(F2) = 0.1282, T = 296(2) K. [ABSTRACT FROM AUTHOR]

C20H24O10, orthorhombic, P212121 (no. 19), a = 6.3728(6) Å, b = 14.3835(14) Å, c = 20.453(2) Å, V = 1874.8(3) Å3, Z = 4, Rgt(F) = 0.0272, wRref(F2) = 0.0558, T = 296(2) K. [ABSTRACT FROM AUTHOR]

Two new amides, claulansamides A and B ( 1 and 2, resp.), together with five known amides, 3- 7 and six known quinolones, 8- 13, were isolated from the stems and roots of Clausena lansium. Their structures were elucidated on the basis of extensive spectroscopic methods. Their absolute configurations were determined by single-crystal X-ray diffraction technique, CD, and optical rotation. HPLC Chiral separation of 1 afforded two enantiomers, (+)- and (−)-claulansamide A, respectively. Compounds 9, 12, and 13 were isolated from the genus Clausena for the first time. All compounds were evaluated for their cytotoxic activities against A549, BGC-823, and HeLa cancer cell lines. However, only 9 showed cytotoxic activity against A549 cell line with an IC50 value of 46.3 μ M, and 11 against BGC-823 and HeLa cell lines with the IC50 values of 55.0 and 14.7 μ M, respectively. [ABSTRACT FROM AUTHOR]

Two new coumarins, clauexcavatins A (1) and B (2), along with seven known ones (3–9), were isolated from the roots of Clausena excavata Burm. f. (Rutaceae). Their structures were elucidated on the basis of spectral data. [ABSTRACT FROM AUTHOR]

C20H24O10, orthorhombic, P212121 (no. 19), a = 6.3728(6) Å, b = 14.3835(14) Å, c = 20.453(2) Å, V = 1874.8(3) Å3, Z = 4, Rgt(F) = 0.0272, wRref(F2) = 0.0558, T = 296(2) K. [ABSTRACT FROM AUTHOR]

A new phenethanol, (2'R)-4-(2', 3'-dihydroxy-3'-methyl-butanoxy)-phenethanol (1), along with other eleven known benzene derivatives (2-12) were isolated from the roots, stems and leaves of Clausena excavata (Rutaceae). Compounds 3 and 4 are new natural products, and compounds 5-8, 10-12 were isolated from C. excavata for the first time. Their structures were elucidated on the basis of MS, 1D and 2D NMR spectroscopic analyses including HSQC, COSY and HMBC experiments. 1 was tested for its cytotoxicities against A549, HeLa and BGC-823 cancer cell lines, and antimicrobial activities against Candida albicans and Staphylococcus aureus. The results showed that 1 did not exhibit cytotoxic and antimicrobial activities.

To investigate monoterpenes and sesquiterpenes of the stems and leaves of Clausena excavata, an AcOEt fraction of the methanol extract was subjected on column chromatographies including silica gel and RP-18, as well as preparative HPLC. The structures of compounds isolated were identified on the basis of spectroscopic data as excamonoterpene (1), (6R, 9S)-9, 10-dihydroxy-4-megastigmen-3-one (2), (3R, 6R, 7E) -3-hydroxy-4, 7-megastigmadien-9-one (3), (3S) -3-hydroxy-7, 8-dihydro-beta-ionone (4), (3S, 5R, 6S) -3-hydroxy-5,6-epoxy-beta-ionone (5), (6R, 9R) -9-hydroxy-4-megastigmen-3-one (6), (3S, SR) -dihydroxy-6, 7-megstigmadien-9-one(7), (-)-loliolide(8), caryolane-1, 9alpha-diol(9) and 2, 6-dihydroxyhumula-3 (12), 7 (13), 9(E)-triene (10), were isolated from the stems and leaves of C. excavata. Compound 1 is a new monoterpene, named as excamonoterpene. Compounds 2-10 were isolated from this plant for the first time.

Ethnopharmacological Relevance: Radix Aconiti Lateralis (Fuzi in Chinese, derived from the lateral roots of Aconitum Carmichaeli Debx.) is widely used for the treatment of heart failure, internal cold, arthralgia, diarrhea and edema for thousands of years. It was usually prescribed in combination with Rhizoma Zingiberis (Ganjiang in Chinese, derived from the dry rhizome of Zingiber officinale Rosc.) to decrease toxicity and increase efficacy., Aim of the Study: In order to investigate the influence of Rhizoma Zingiberis on pharmacokinetics of six Aconitum alkaloids, i.e. aconitine (AC), hypaconitine (HA), mesaconitine (MA), benzoylaconine (BAC), benzoylhypaconine (BHA) and benzoylmesaconine (BMA), in Fuzi-Ganjiang herb couple, the comparative pharmacokinetics of six Aconitum alkaloids after oral administration of Fuzi and Fuzi-Ganjiang aqueous extract was carried out., Materials and Methods: A sensitive, specific and rapid LC-MS/MS method was developed to determine the six analytes in plasma. Then the rats were randomly divided into two groups and orally administered with Fuzi and Fuzi-Ganjiang aqueous extract. At designated time points after oral administration, the concentrations of the six Aconitum alkaloids in rat plasma were determined, and main pharmacokinetic parameters were investigated using 3P97 (Practical Pharmacokinetics Program Version 1.0)., Results: Comparing with Fuzi group, both T1/2 and AUC0-t of AC and HA decreased (P<0.05), while T1/2, AUC0-t and Cmax of BAC, BHA increased (P<0.05) in Fuzi-Ganjiang group, which indicated that Ganjiang could promote the elimination of AC and HA and enhance the absorption of BAC, BHA and BMA., Conclusion: The differences of pharmacokinetics of Aconitum alkaloids in rat plasma could support those of pharmacologics and toxicity in previous reports between Fuzi and Fuzi-Ganjiang herb couple. The results might be helpful in explaining the mechanism of combination of Fuzi-Ganjiang to decrease toxicity and increase efficacy., (Copyright © 2013 Elsevier Ireland Ltd. All rights reserved.)

This study aimed to clarify the rationality of herbaceous compatibility of a rhubarb peony decoction (DaHuang-Mu-Dan-Tang, RPD) by comparing the pharmacokinetics of aloe-emodin, rhein and emodin in rats' plasma after oral administration of RPD and rhubarb extract. A rapid, sensitive LC-MS method was developed and validated for the determination of the plasma concentrations of the three analytes after oral administration RPD and rhubarb extract. The developed method was successfully applied to a pharmacokinetic study of aloe-emodin, rhein and emodin in rats' plasma after oral administration. Compared with administration of single rhubarb, the C(max) of rhein in RPD was decreased significantly (p < 0.05). Meanwhile, the T1/2 of aloe-emodin and emodin were increased significantly (p < 0.05) after administration of RPD. In addition, the T(max) of rhein and emodin were also increased significantly (p < 0.05) in RPD. These results indicated that the absorption of rhein in rats was suppressed after oral administration RPD. Moreover, The time for rhein and emodin to reach the peak concentration was delayed and the elimination of aloe-emodin and emodin was also postponed in RPD. This study could provide a meaningful basis for evaluating the clinical application of traditional Chinese medicine in terms of pharmacokinetics.

Objective: To study the chemical constituents of the unmatured fruits of Citrus aurantium., Method: The AcOEt fraction of the methanol extracts of the unmatured fruits of C. aurantium were subjected on column chromatographies including silica gel, RP-18 and HPLC. Compound structures isolated were determined on the basis of spectroscopic data., Result: Three compounds were isolated from the unmatured fruits of C. aurantium, which were identified as citrauranoside (1), limonexin (2) and limonin (3)., Conclusion: Compound 1 is a new chroman glycoside derivative, named as citrauranoside.