三台花中的一新奇化合物--Serratumin A

从云南西双版纳产的三台花（Ｃｌｅｒｏｄｅｎｄｒｕｍ ｓｅｒｒａｔｕｍ ｖａｒ．ａｍｐｌｅｘｉｆｏｌｉｕｍ Ｍｏｌｄｅｎｋｅ）的地上部分分离到６个化合物,它们的结构通过波谱解析（包括２Ｄ ＮＭＲ技术）得到鉴定。其中化合物１是一新奇的单萜烯酸和单糖衍生物的缩合物,命名为ｓｅｒｒａｔｕｍｉｎ Ａ（１）;化合物２～６为首次从该植物中分离得到。     

Evaluation of hepatoprotective activity of legumes.

Mung bean, adzuki bean, black bean and rice bean are foods and folk medicines of Taiwan. We evaluated the effects of various water extract concentrations (100, 500 and 1000 mg/kg body wt.) and silymarin (25 mg/kg body wt. on acetaminophen-induced liver injury by measuring serum glutamate-oxalate-transaminase (sGOT) and serum glutamate-pyruvate-transaminase (sGPT) activities in rats. The results showed that the sGOT and the sGPT activities, increased by APAP, were decreased significantly (P < 0.05) through treatment with inceasing amounts up to 1000 mg/kg body wt. of the exracts. In particular, the mung bean aqueous extract showed the best hepatoprotective effect on APAP-induced hepatotoxicity. The pathological changes of liver injury caused by APAP improved by the treatment with all of the legume extracts, which were compared to silymarin as a standardized drug. In addition to these results, the extract of mung bean acted as a potential hepatoprotective agent in dietary supply.     

Phytochemical constituents and hepatoprotective activity of Viburnum tinus

From the leaves of Viburnum tinus L. (Adoxaceae) two acylated iridoid glucosides (viburtinoside A and B), a coumarin diglucoside scopoletin 7-O-beta-D-sophoroside and a natural occurred dinicotinic acid ester 2,6-di-C-methyl-nicotinic acid 3,5-diethyl ester were isolated. In addition to these, 10 known compounds were isolated, namely two bidesmosidic saponins, a hexamethoxy-flavone and five flavonol glycosides, as well as suspensolide A and oleanolic acid were isolated for the first time in this genus and species, respectively. The structures were determined mainly by spectroscopic methods (UV, IR, ESI-MS, 1H-, 13C NMR and DEPT). Toxicity of the investigated extract was determined (LD50=500 mg/kg). CCl4-induced hepatotoxicity has been evaluated in terms of the determination of alanine aminotransferase (ALT), aspartate aminotransferase (AST), lipid peroxide and nitric oxide levels in serum and compared using adult male rats weighing 150-180 g. Their highly elevated levels were significantly reduced by treatment with the investigated aqueous methanol extract in dose-dependent manner.     

Ontogeny of Axillary and Accessory Buds in Clerodendrum phlomidis L.

Plastochronic changes in the vegetative shoot apex and originand development of axillary and accessory buds are studied. The flat shoot apex shows structural and dimensional changesin a plastochron. They are described in three phases, the pre-leafinitiation, the leaf initiation, and the post-leaf initiation.The youngest axillary bud meristem is identified near the axilat the second node when the subtending leaf primordium is 200–12µ long. The corpus of the bud meristem has a more activerole in bud development than has the tunica layers. The shellzone associated with a young bud meristem persists until thebud has attained the structural and functional attributes ofthe main shoot apex. It loses its histological identity by producingderivatives which merge with the ground tissue and procambialcells of bud traces. In a developing bud the provascular systemof the bud appears as an arc, a loop, or as a ring in transversesections at different levels. These configurations are composedof anastomosing procambial strands of bud trace and residualmeristem, both being differentiated from developing bud meristem.     

Synthesis and the hepatoprotective activity of dibenzocyclooctadiene lignan derivatives

The halogenated and oxidized derivatives (1a–1e, 1a′–1c′, 2a–2d, 2a′–2b′, 3a–3e, 3′ and 3a′–3b′) of schizandrin (1), schizandrin B (2) and schisanhenol (3) were synthesized. The hepatoprotective effects of these dibenzocyclooctadiene lignan analogues against CCl₄-induced injury were preliminarily evaluated. Most of the analogues exhibited higher protective effects than the positive control biphenyldicarboxylate (DDB). Among these active analogues, dichloroschisanhenol (3a) exhibited the strongest protective activity (cell survival rate exceeding 98.0%).     

Antitumor and hepatoprotective activity of natural and synthetic neo steroids

In this review, steroids with a tertiary butyl group, which are usually called neo steroids, are a small group of natural lipids isolated from higher plants, fungi, marine sponges, and yeast. In addition, steroids with a tertiary butyl group have been synthesized in some laboratories in Canada, USA, Europe, and Japan and their biological activity was studied. Some natural neo steroids demonstrate antitumor or hepatoprotective activities. In addition, synthetic neo steroids exhibit anticancer and neuroprotective properties. However, to confirm the above data, both practical and clinical experimental studies are necessary. Nevertheless, the results may be useful for pharmacologists, chemists, biochemists, and the pharmaceutical industry.     

Synthesis of the lupane group triterpenoids and there hepatoprotective activity

Hemisuccinates, hemiphthalates, acetylsalicylates, cinnamates, and p-methoxycinnamates of lupeol, betulin, and 3-O-acetylbetulin were synthesized via interaction with corresponding acid anhydrides or acid chlorides. A number of betulin esters in position 3 and 28 were shown to exhibit a pronounced hepatoprotective effect similar to that of betulin and silibor. These experimental data were in a good agreement with the computer prediction of their biological activity. Betulin 3,28-bis-hemiphthalate was more effective than carsil in models of experimental hepatitis caused by carbon tetrachloride, tetracycline, and ethanol.     

Cytotoxicity and hepatoprotective attributes of methanolic extract of Rumex vesicarius L.

Background

To evaluate the hepatoprotective potential and invitro cytotoxicity studies of whole plant methanol extract of Rumex vesicarius L. Methanol extract at a dose of 100 mg/kg bw and 200 mg/kg bw were assessed for its hepatoprotective potential against CCl₄-induced hepatotoxicity by monitoring activity levels of SGOT (Serum glutamic oxaloacetic transaminase), SGPT (Serum glutamic pyruvic transaminase), ALP (Alkaline phosphatase), TP (Total protein), TB (Total bilirubin) and SOD (Superoxide dismutase), CAT (Catalase), MDA (Malondialdehyde). The cytotoxicity of the same extract on HepG2 cell lines were also assessed using MTT assay method at the concentration of 62.5, 125, 250, 500 μg/ml.

Results

Pretreatment of animals with whole plant methanol extracts of Rumex vesicarius L. significantly reduced the liver damage and the symptoms of liver injury by restoration of architecture of liver. The biochemical parameters in serum also improved in treated groups compared to the control and standard (silymarin) groups. Histopathological investigation further corroborated these biochemical observations. The cytotoxicity results indicated that the plant extract which were inhibitory to the proliferation of HepG2 cell line with IC50 value of 563.33 ± 0.8 μg/ml were not cytotoxic and appears to be safe.

Conclusions

Rumex vesicarius L. whole plant methanol extract exhibit hepatoprotective activity. However the cytotoxicity in HepG2 is inexplicable and warrants further study.     

Hypoglycemic and hepatoprotective activity of Rosmarinus officinalis extract in diabetic rats

The present study examined the effect of water extract (200 mg/kg body weight) of Rosmarinus officinalis L. in streptozotocin (STZ)-induced diabetic rats for 21 days. The hepatoprotective effects were investigated in the liver tissues sections. There was a significant increase in serum liver biochemical parameters (aspartate aminotransferase, alanine transaminase, and alkaline phosphatase), accompanied by a significant decrease in the level of total protein and albumin in the STZ-induced rats when compared with that of the normal group. The high-dose treatment group (200 mg/kg body wt) significantly restored the elevated liver function enzymes near to normal. This study revealed that rosemary extracts exerted a hepatoprotective effect. The results indicate that the extract exhibits the protective effect on tissues and prove its potentials as an antidiabetic agent.     

The synthesis and hepatoprotective activity of esters of the lupane group triterpenoids

Hemisuccinates, hemiphthalates, acetylsalicylates, cinnamates, andp-methoxycinnamates of lupeol, betulin, and 3-O-acetylbetulin were synthesized via interaction with corresponding acid anhydrides or acid chlorides. A number of betulin esters in position 3 and 28 were shown to exhibit a pronounced hepatoprotective effect similar to that of betulin and silibor. These experimental data were in a good agreement with the computer prediction of their biological activity. Betulin 3,28-bishemiphthalate was more effective than carsil in models of experimental hepatitis caused by carbon tetrachloride, tetracycline, and ethanol.     

Isolation of quinic acid derivatives and flavonoids from the aerial parts of Lactuca indica L. and their hepatoprotective activity in vitro

In our continuing study of biologically active compounds from Korean medicinal plants, we investigated the hepatoprotective constituents of the aerial parts of Lactuca indica L. (Compositae), since the methanolic extract of L. indica has hepatoprotective activity against hepatitis B virus (HBV) production. The bioactivity-guided separation of the methanolic extract of the aerial parts of L. indica resulted in the isolation of seven quinic acid derivatives (1, 3–4, 6, and 10–12), along with five flavonoids (2, 5, and 7–9). All the isolated compounds were evaluated for hepatoprotective activity by the HBV assay in vitro. In the human HBV-transfected liver cell line HepG2.2.15, all the compounds except 2 and 5 effectively reduced HBV DNA level in the release of mature HBV particles from HepG2.2.15 cultivation. Of the ten active compounds, treatment with 1, 3, and 12 led to significant reduction in the extracellular HBV DNA level, suggesting that they could be potent phytochemical agents against hepatitis B virus.     

Potential hepatoprotective activity of ononitol monohydrate isolated from Cassia tora L. on carbon tetrachloride induced hepatotoxicity in wistar rats

Ononitol monohydrate, structurally similar to glycoside was isolated from Cassia tora L. leaves. Fifty Male rats were divided into five groups. Group I served as normal control. Group II, III and IV rats were induced hepatotoxicity by CCl₄ administering single dose of CCl₄ on 8th day only. Group III was treated with ononitol monohydrate (20 mg/kg body weight) and group IV was treated with reference drug silymarin (20 mg/kg body weight) both dissolved in corn oil and administering for 8 days. Ononitol monohydrate with corn oil alone was given for 8 days (group V). At the end of the experimental period all the animals were sacrificed and analyzed for biochemical parameters to assess the effect of ononitol monohydrate treatment in CCl₄ induced hepatotoxicity. In in vivo study, ononitol monohydrate decreased the levels of serum transaminase, lipid peroxidation and TNF-α but increased the levels of antioxidant and hepatic glutathione enzyme activities. Compared with reference drug silymarin ononitol monohydrate possessesed high hepatoprotective activity. Histopathological results also suggested the hepatoprotective activity of ononitol monohydrate with no adverse effect. Hence we conclude that ononitol monohydrate is a potent hepatoprotective agent.     

Cloning and characterisation of a gene encoding an antiviral protein from Clerodendrum aculeatum L.

The Clerodendrum aculeatum-systemic resistence inducing (CA-SRI) protein, a 34 kDa basic protein, plays a key role in inducing strong systemic resistance in susceptible plants against various plant viruses [22]. We have cloned the cDNA encoding the CA-SRI from C. aculeatum leaves using antibodies raised against the purified protein and degenerate oligonucleotide probes derived from microsequencing of the CA-SRI protein. The full-length cDNA consisted of 1218 nucleotides with an open reading frame of 906 bp. The deduced amino acid sequence of CA-SRI protein showed varying homology (ranging from 11 to 54%) to the ribosome inactivating proteins (RIPs) from other plant species. CA-SRI inhibited in vitro protein synthesis both in rabbit reticulocyte lysate and wheat germ lysate but not in Escherichia coli in vitro translation system. The CA-SRI open reading frame was expressed in an E. coli expression vector and the purified recombinant protein inhibited protein synthesis in rabbit reticulocyte lysate. Southern blot analysis indicated that the CA-SRI gene may be present in low copy number.     

In vitro adventitious shoot formation from leaf cultures of Clerodendrum inerme (L) Gaertn.

In vitro adventitious shoots (about 28) of Clerodendrum inerme were regenerated from leaf segments on MS medium containing BA (4 mg/L). These shoots developed directly from the leaf explants without callusing after 5 weeks. Leaf explant when cultured in MS medium containing BA (2 mg/L) and NAA (0.5 mg/L) developed compact callus that became nodular and regenerated shoots (about 50) after 5 weeks. The in vitro developed shoots were rooted in MS medium supplemented with IAA (2 mg/L). The hardened plantlets were successfully established in the field with 90% survival.     

Acylated phenylethanoid oligoglycosides with hepatoprotective activity from the desert plant Cistanche tubulosa

The methanolic extract from fresh stems of Cistanche tubulosa (Orobanchaceae) was found to show hepatoprotective effects against d-galactosamine (d-GalN)/lipopolysaccharide (LPS)-induced liver injury in mice. From the extract, three new phenylethanoid oligoglycosides, kankanosides H₁ (1), H₂ (2), and I (3), were isolated together with 16 phenylethanoid glycosides (4–19) and two acylated oligosugars (20, 21). The structures of 1–3 were determined on the basis of spectroscopic properties as well as of chemical evidence. Among the isolates, echinacoside (4, IC₅₀ = 10.2 μM), acteoside (5, 4.6 μM), isoacteoside (6, 5.3 μM), 2′-acetylacteoside (8, 4.8 μM), and tubuloside A (10, 8.6 μM) inhibited d-GalN-induced death of hepatocytes. These five isolates, 4 (31.1 μM), 5 (17.8 μM), 6 (22.7 μM), 8 (25.7 μM), and 10 (23.2 μM), and cistantubuloside B₁ (11, 21.4 μM) also reduced TNF-α-induced cytotoxicity in L929 cells. Moreover, principal constituents (4–6) exhibited in vivo hepatoprotective effects at doses of 25–100 mg/kg, po.     

Antioxidant and hepatoprotective activity of Aphanizomenon flos-aquae Linn against paracetamol intoxication in rats

Paracetamol caused liver damage as evident by significant increase in the activities of aspartate and alanine transferases. There were general statistically significant losses in the activities of superoxide dismutase, catalase, glutathione peroxidase and glutathione transferase and an increase in thiobarbituric acid reactive substances in the liver of paracetamol treated group compared with the control group. However, treatment with ethanol extract of A. flos-aquae (EEAFA) was able to counteract these effects. Protection offered by silymarin (standard reference drug) seemed relatively greater. The results suggest that EEAFA can act as hepatoprotective agent against paracetamol induced toxicity as an antioxidant.     

The structural analysis and its hepatoprotective activity of melanin isolated from Lachnum sp

In the present study, an intracellular melanin (LIM) isolated from Lachnum YM30 was obtained by submerged fermentation, extraction and purification. The possible structural formula of LIM was concluded, based on Ultraviolet (UV) analysis, IR analysis, elemental analysis, Nuclear Magnetic Resonance (NMR) and ESI-MS analysis, which showed the typical feature of fungal eumelanin. The hepatoprotective effect of LIM was evaluated in an acute LPS/D-GalN induced liver injury mouse model that was proved by the declining of alanine aminotransferase (ALT) and aspartate transaminase (AST), enhancing the content of anti-inflammatory factors interleukin-4 (IL-4) and interleukin-10 (IL-10). Concurrently, LIM could alleviate LPS/D-GalN toxicity through the effects of NF-kappa B (NF-κB) signaling pathway and its related cytokines interleukin-1β (IL-1β), tumor necrosis factor alpha (TNF-α) and interleukin-8 (IL-8). The mechanisms underlying the protective effect might be related to inhibition of nuclear factor-kappa B activation and the functional groups of LIM. And compared with the single positive drug treatment or the melanin, the results showed that the combined treatment group could further reduce the inflammatory reaction of the model mice.     

Eight new glycosides with hepatoprotective activity isolated from the aerial parts of Morinda parvifolia

Eight new glycosides, morindaparvins P–W, were isolated from the butanol extract of the aerial parts of Morinda parvifolia. These new structures were elucidated by comprehensive spectroscopic analysis and by comparing the experimental and calculated electronic circular dichroism spectra. The butanol extract was observed to significantly reduce the levels of alanine aminotransferase, aspartate transaminase, and lactate dehydrogenase in the sera of mice with concanavalin A-induced hepatitis. At a concentration of 10 μM, five compounds (1, and 4–7) isolated from the butanol extract possessed hepatoprotective activities against the damage induced by acetaminophen in human HepG2 liver cancer cells.     

Antioxidant activity and hepatoprotective potential of Hammada scoparia against ethanol-induced liver injury in rats

The present work was aimed at studying the antioxidative activity and hepatoprotective effects of methanolic extract (ME) of Hammada scoparia leaves against ethanol-induced liver injury in male rats. The animals were treated daily with 35 % ethanol solution (4 g?kg^?1?day^?1) during 4 weeks. This treatment led to an increase in the lipid peroxidation, a decrease in antioxidative enzymes (catalase, superoxide dismutase, and glutathione peroxidase) in liver, and a considerable increase in the serum levels of aspartate and alanine aminotransferase and alkaline phospahatase. However, treatment with ME protects efficiently the hepatic function of alcoholic rats by the considerable decrease in aminotransferase contents in serum of ethanol-treated rats. The glycogen synthase kinase-3 β was inhibited after ME administration, which leads to an enhancement of glutathione peroxidase activity in the liver and a decrease in lipid peroxidation rate by 76 %. These biochemical changes were consistent with histopathological observations, suggesting marked hepatoprotective effect of ME. These results strongly suggest that treatment with methanolic extract normalizes various biochemical parameters and protects the liver against ethanol induced oxidative damage in rats.