Analysis of plasma migration components in Patrinia villosa (Thunb.) Juss. effective parts by UPLC-Q-TOF-MS.

Patrinia villosa (Thunb.) Juss. (PVJ) is described as pungent, bitter and slightly cold in Chinese medicine, and is associated with the large intestine, stomach and liver meridians. The preliminary experiments of our research team proved that PVJ total flavonoids have excellent inhibitory effects on liver cancer cells. The present experiment uses the UPLC-Q-TOF-MS technology and serum pharmacochemistry methods to analyze the chemical components in vitro and in vivo of PVJ antiliver tumors. A total of 14 chemical components were identified in the total flavonoids extract of PVJ, and it is mainly composed of flavonoids, flavonones, flavonols and phenolic acids. At the same time, seven prototypical components and seven metabolic components were detected in the drug-containing plasma. Hydrocaffeate and scutellarein are the phase I metabolites of caffeic acid and scutellarin, respectively. Sulfated apigenin, sulfated luteolin, sulfated kaempferol and methylated kaempferol are the II phase metabolites of apigenin, luteolin, kaempferol, respectively. The experiment provides a reference for the research and development of antitumor drug candidates, and provides a basis for revealing the bioactive components of PVJ and the antitumor mechanism.

Anti-Melanogenic Effects of Ethanol Extracts of the Leaves and Roots of Patrinia villosa (Thunb.) Juss through Their Inhibition of CREB and Induction of ERK and Autophagy.

Patrinia villosa (Thunb.) Juss is a traditional herb commonly used in East Asia including Korea, Japan, and China. It has been administered to reduce and treat inflammation in Donguibogam, Korea. The mechanism for its anti-inflammatory effects has already been reported. In this study, we confirmed the efficacy of Patrinia villosa (Thunb.) Juss ethanol extract (Pv-EE) for inducing autophagy and investigate its anti-melanogenic properties. Melanin secretion and content were investigated using cells from the melanoma cell line B16F10. Pv-EE inhibited melanin in melanogenesis induced by α-melanocyte-stimulating hormone (α-MSH). The mechanism of inhibition of Pv-EE was confirmed by suppressing the mRNA of microphthalmia-associated transcription factor (MITF), decreasing the phosphorylation level of CREB, and increasing the phosphorylation of ERK. Finally, it was confirmed that Pv-EE induces autophagy through the autophagy markers LC3B and p62, and that the anti-melanogenic effect of Pv-EE is inhibited by the autophagy inhibitor 3-methyl adenine (3-MA). These results suggest that Pv-EE may be used as a skin protectant due to its anti-melanin properties including autophagy.

A novel flavonoid with antioxidant activity from Patrinia villosa (Thunb.) Juss.

Patrinia villosa (Thunb.) Juss (P. villosa), a perennial herb, is widely used as a medicinal plant in Chinese folk. This study aims to isolate and identify the chemical constituents from P. villosa and evaluate their antioxidant activity. Normal silica column chromatography, ODS silica column chromatography, Sephadex LH-20 column chromatography and semi-preparative HPLC methods were used to obtain a new compound named 3-n-pentadecyl-4'-methoxyluteolin (1) and two known compounds including luteolin-7-O-ß-D-glucuronide methyl ester (2) and apigenin-7-O-ß-D-glucuronide methyl ester (3). The antioxidant activity of these compounds was determined by DPPH and ABTS methods and the IC50 values were calculated. The IC50 values of ABTS scavenging activity of 1, 2 and 3 were 12.99 ± 0.09 µM, 7.13 ± 0.07 µM and 5.15 ± 0.08 µM, respectively, and the IC50 values of DPPH scavenging activity of 1, 2 and 3 were 51.86 ± 0.41 µM, 23.95 ± 0.71 µM and 25.06 ± 0.65 µM, respectively. All the compounds exhibited good antioxidant activities in vitro.

Therapeutic effect and metabolomics mechanism of Patrinia Villosa (Thunb.) juss on liver injury in rats.

Patrinia villosa (Thunb.) Juss (P.V) is widely used in the treatment of chronic diseases, such as appendicitis, enteritis and gynecological inflammation. Modern research indicated that the herb has pharmacological effect on liver injury caused by inflammation, but the metabolomics mechanism is not clear. For the purpose of discovering the therapeutic effect and metabolomic mechanism of P.V on liver injury, 40 Sprague-Dawley (SD) rats were divided into normal group, model group, and P.V groups (0.98, 1.97, and 2.96 g/kg). The model group and P.V groups were injected intraperitoneally with 40% CCl4 (v/v, olive oil) to establish liver injury model. After administration of P.V for seven consecutive days. Therapeutic effect of P.V on liver injury rats were analyzed. P.V could decrease serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels of liver injury rats as a dose-dependent manner. Compared with the model group, the pathological analysis of liver tissue of P.V groups exhibit significant decrease tendency of hepatic tissue structure destruction, cytoplasmic vacuolation, cellular swelling, and inflammatory cell infiltration as a dose-dependent manner. 82 endogenous metabolites in rat serum and liver were analyzed by Ultra-high performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS). 14 metabolites in serum and 26 metabolites in liver were significantly different between the P.V group (2.96 g/kg) and the model group. Metabolic pathway analysis revealed that the main pathway including alanine, aspartate and glutamate metabolism, and TCA cycle were significantly altered. It is suggested that P.V can alleviate CCl4 induced liver injury, and its effect on metabolites may be an important mechanism of action.

A New Biphenyl Neolignan from Leaves of Patrinia villosa (Thunb.) Juss.

RESULTS: One new stereoisomer of biphenylneolignan with four known compounds was isolated from the leaves of Patrinia villosa Juss. METHODS: The structure of the new compound was elucidated as 2,6,2',6'-tetramethoxy-4,4'-bis (1,2-trans-2,3-epoxy-1-hydroxypropyl) biphenyl (1) on the basis of spectroscopic analysis and comparison with literature data. The four known compounds were identified as 2,6,2',6'-tetramethoxy-4,4'-bis(1,2-cis-2,3-epoxy-1-hydroxypropyl)biphenyl (2), 1H-indole-3-carbaldehyde (3), luteolin (4) and quercetin(5) by comparison of their spectral data with the reported data, respectively. CONCLUSIONS: Compound 1 is a new biphenylneolignan, compound 2 and 3 were isolated for the first time from the plant. SUMMARY: One new stereoisomer of biphenylneolignan named 2,6,2',6'-tetramethoxy-4,4'-bis (1,2-trans-2,3-epoxy-1-hydroxypropyl) biphenyl with four known compounds was isolated from the leaves of Patrinia villosa Juss.

Species classification and bioactive ingredients accumulation of BaiJiangCao based on characteristic inorganic elements analysis by inductively coupled plasma-mass spectrometry and multivariate analysis.

BACKGROUND: Patrinia scabiosaefolia Fisch and Patrinia villosa (Thunb.) Juss., two species herbs with the same Chinese name "BaiJiangCao", are important ancient herbal medicines widely used for more than 2000 years. The clinical application of two species herb is confused due to the difficult identification. OBJECTIVE: The objective was to authenticate the species of BaiJiangCao and analyze the accumulation of bioactive ingredients based on characteristic inorganic elements analysis. MATERIALS AND METHODS: Content of 32 inorganic elements in BaiJiangCao from different habitats were determined by inductively coupled plasma-mass spectrometry (ICP-MS), and the characteristic inorganic elements were picked to distinguish the species of the herb by principal component analysis and cluster analysis. Contents of two bioactive ingredients, luteoloside, and oleanolic acid, in the samples, were also analyzed by high-performance liquid chromatography method. Relationship between accumulation of bioactive ingredients and content of macroelements in BaiJiangCao was established by statistics. RESULTS: A 4 macroelements (Na, Mg, K, Fe) in 32 determined inorganic elements were picked for characteristic inorganic elements. Content of Na, Mg, K and Fe showed positive correlations with that of luteoloside, content of Na, Mg showed positive correlations with that of oleanolic acid, but content of K and Fe showed negative correlations with that of oleanolic acid. CONCLUSION: It is for the first time to utilize the characteristic inorganic elements as an index to classify the herb species by the method of ICP-MS and multivariate analysis. And it is also the first report to investigate the influence of inorganic elements in herb on the accumulation of bioactive components which could affect the pharmacological efficacy of the herb medicine. And this method could also be utilized in research of corresponding aspects.