Cytotoxic constituents of Abutilon indicum leaves against U87MG human glioblastoma cells

The study was aimed to identify cytotoxic leads from Abutilon indicum leaves for treating glioblastoma. The petroleum ether extract, methanol extract (AIM), chloroform and ethyl acetate sub-fractions (AIM-C and AIM-E, respectively) prepared from AIM were tested for cytotoxicity on U87MG human glioblastoma cells using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. These extracts exhibited considerable activity (IC₅₀ values of 42.6–64.5 μg/mL). The most active AIM-C fraction was repeatedly chromatographed to yield four known compounds, methyl trans-p-coumarate (1), methyl caffeate (2), syringic acid (3) and pinellic acid (4). Cell viability assay of 1–4 against U87MG cells indicated 2 as most active (IC₅₀ value of 8.2 μg/mL), whereas the other three compounds were much less active. Interestingly, compounds 1–4 were non-toxic towards normal human cells (HEK-293). The content of 2 in AIM-C was estimated as 3% by HPLC. Hence, presence of some more active substances besides methyl caffeate (2) in AIM-C is anticipated.     

Anti-inflammatory and analgesic effects of human placenta extract

In this study, we investigated the effects of human placenta extract (HPE, Laennec inj.) on pro-inflammatory cytokines and mediators secreted from lipopolysaccharide-stimulated RAW264.7 macrophages. We found that HPE significantly inhibited the production of nitric oxide, tumour necrosis factor-α and cyclooxygenase-2. We studied the anti-inflammatory and analgesic potential of HPE in murine models of inflammation/inflammatory pain. Rats were assigned to six groups and were administered either saline or HPE (0.33, 1, 3 and 6 mL kg?1) intraperitoneally. Diclofenac was used as a positive control. HPE attenuated the swelling of the rat's hind paw. The vascular permeability induced by acetic acid was significantly reduced by HPE. HPE reduced the formation of granuloma in carrageenan air pouch and hind paw oedema in complete Freund's adjuvant-induced chronic arthritis in rats. HPE attenuated writhing episodes. An increase in hot-plate latency was observed in mice receiving HPE. HPE also increased the pain threshold in the Randall-Selitto test. In the tail-flick assay, HPE prolonged the reaction time of rats to radiant heat stimulation. These results suggest that HPE has potent anti-inflammatory and anti-nociceptive activities.     

Anti-inflammatory activity of Gentiana striata Maxim

The anti-inflammatory activity and the mechanism of action of Gentiana striata Maxim. has been investigated. The most active phase, the ethyl acetate extract of Gentiana striata Maxim. (EGS), displayed potent inhibitory activity on feet oedema of rheumatoid arthritis (RA) inflicted rats. This anti-inflammatory activity might be partly based on the notable reduction of prostaglandin E2 (PGE?) and nitric oxide (NO) levels. Six further compounds isolated from EGS have previously been reported as having anti-inflammatory activity.     

Investigation of thermal behavior of Heliotropium indicum L. lyophilized extract by TG and DSC

Thermogravimetric (TG) techniques and differential scanning calorimetry (DSC) used for the study of pre-formulation or drug–adjuvant compatibility have been gaining importance in Brazil. These techniques are being used for the verification of possible interactions between drugs and adjuvants. Aiming at studying the behavior of a plant extract and its mixture with adjuvants, using these thermoanalytical techniques the plant species Heliotropium indicum L. was used. This plant which is originally from India and has been well acclimatized in Brazil has healing and anti-inflammatory properties. The methodology for obtaining the extract followed the Brazilian Pharmacopoeia methodology. And the incorporation of the extract with adjuvants was through binary mixtures (1:1 w/w). The TG and DSC curves were obtained under nitrogen atmosphere (25 mL min^?1) at a heating rate of 5 °C min^?1; TG tests were analyzed within a temperature range from 25 to 600 °C and DSC from 25 to 300 °C. The TG curves show good thermal stability of the extract and its mixtures with adjuvants up to 150 °C, except the propylene glycol (PLG). The DSC curves revealed an incompatibility of the extract with methylparaben and PLG mixture.     

Anti-inflammatory and antibacterial activity study of some novel quinazolinones

Anti-inflammatory and antibacterial activities of some novel quinazolinones were determined. Evaluation of anti-inflammatory activity of test compounds was performed using carrageenan induced paw edema in rats. Oral administration of test compounds 25 mg/kg and 50 mg/kg reduced the paw edema significantly (P < 0.05) in a dose dependent manner compared to carrageenan induced rats. The test compounds were also screened for their antibacterial activity against the strains of Staphylococcus aureus and Escherichia coli at the concentrations of 200 μg/ml and 1 mg/ml. The test compounds showed better activity as that of the standard lincomycin at the tested higher concentration against S. aureus. None of the compounds exhibit comparable activity to that of the standard ceftazidime against E. coli.     

New Glycosidic Constituents of Abutilon pakistanicum

Pakisides A and B ( 1 and 2 , resp.), new catalpol‐type iridoid glycosides, and a new glycoside, 3 , of scutellarein have been isolated from the AcOEt‐soluble fraction of the whole plant of Abutilon pakistanicum, along with buddlejoside and lapachol. The structures of new compounds were elucidated by spectroscopic techniques including ¹H‐and ¹³C‐NMR (DEPT), and 2D‐NMR experiments.     

Anti-inflammatory and analgesic activity of Alkanna bracteosa and Alkanna tricophila

Alkanna bracteosa and Alkanna tricophila, Boraginaceae, have been reported to be useful for their anti-inflammatory and wound-healing effects in traditional medicine. Methanol extracts of A. bracteosa and A. tricophila were evaluated for their potential analgesic and anti-inflammatory properties. Alkanna bracteosa was observed to produce a maximum of 42% reduction of hind paw licking in acute as well as 68% alleviation in inflammatory phase of formalin test in mice and about 30% declination of carrageenan-induced rats paw swelling at doses 100-400?mg?kg?1 in comparison to negative control; on the other hand, A. tricophila required at least 200?mg?kg?1 to exhibit a significant reduction in paw licking or oedemas at the early phase of formalin test and the late phase of carrageenan test, respectively. Our results suggest that the extracts may be of use for their analgesic and anti-inflammatory effects.     

Anti-inflammatory and antioxidant activity of Ficus carica Linn. leaves

Ficus carica Linn. (Moraceae) is commonly known as edible fig. The leaves, roots, fruits and latex of the plant are medicinally used in different diseases. The leaves are claimed to be effective in various inflammatory conditions like painful or swollen piles, insect sting and bites. However, there has been no report on anti-inflammatory and antioxidant activity of F. carica leaves. Therefore the aim of this study was to evaluate the anti-inflammatory and antioxidant activity of F. carica leaves. Our study validated the traditional claim with pharmacological data. Anti-inflammatory and antioxidant activity of the drug could be due to the presence of steroids and flavanoids, respectively, which are reported to be present in the drug. Furthermore, the anti-inflammatory activity of the drug could be due to its free radical scavenging activity. Further work is also required to isolate and characterise the active constituents responsible for the anti-inflammatory activities.     

Anti-inflammatory activity of new guaiane type sesquiterpene from Wikstroemia indica

In our investigation of in vitro anti-allergic screening of medicinal herbal extracts, the ethyl acetate extract of the root of Wikstroemia indica was observed to inhibit nitric oxide (NO) production in a lipopolysaccharide (LPS) and recombinant mouse interferon-gamma (IFN-gamma) activated murine macrophage-like cell line, RAW 264.7. Fractionation of the active extract led to the isolation of one new guaiane type sesquiterpene, indicanone (1), and two known biflavonoids, sikokianin B (2) and sikokianin C (3). 1 inhibited NO production with IC50 values at 9.3 microM and also inhibit the inducible nitric oxide synhase (iNOS) gene expression. This is the first report of NO production inhibitory activity of Wikstroemia indica and supports the pharmacological use of it, which has been employed as an herbal medicine for the treatment of inflammation.     

Anti-inflammatory activity of hautriwaic acid isolated from Dodonaea viscosa leaves

The aim of this study was to identify an anti-inflammatory compound from D. viscosa leaves. The structure of this bioactive substance was elucidated by IR and NMR studies, which indicated that this natural product corresponds to hautriwaic acid (HA). This diterpene exhibited good anti-inflammatory activity in 12-O-tetradecanoylphorbol 13-acetate (TPA) mice ear edema models by applications at doses of 0.25, 0.5 and 1.0 mg/ear (60.2, 70.2 and 87.1% inhibition, respectively); additionally Dodonaea viscosa dichloro-methane extract (DvDE) displays a 97.8% anti-inflammatory effect at 3 mg/kg. Multiple applications of DvDE at doses of 100 mg/kg on TPA mice ear edema inhibited the edema-associated inflammation by 71.8%, while HA at doses of 15 mg/kg, reduced edema to 64% and indomethacin 40%.     

Anti-inflammatory effects of Scutellaria baicalensis water extract in LPS-induced THP-1 Macrophages through metabolomics study

(1) Background: Scutellaria baicalensis (Huang Qin) is a traditional Chinese Medicine possess beneficial effects of anti-inflammation in various diseases. In this study, we aimed to use untargeted metabolomics approach to investigate the possible underlying metabolic mechanisms of anti-inflammation effects of Scutellaria baicalensis in LPS-induced macrophages.; (2) Methods: Scutellaria baicalensis water extract (SBE) were applied to the THP-1 cells which were induced by phorbol 12-myristate 13-acetate (PMA) into macrophages under the LPS treated conditions. The cell lysate were collected and metabolites were extracted before characterizing by ultra-performance liquid chromatography (UPLC) combined with Q-Exactive mass/mass spectrometry (LC-MS/MS). The differential accumulated metabolites and related metabolism pathways affected by SBE in LPS-induced macrophages were identified. Further investigation of the secretion and expression of inflammatory cytokines IL-1β, TNF-ɑ and VEGFR were tested by real-time polymerase chain reaction (RT-PCR). (3) Results: The metabolome profile have indicated that retinol metabolism, arachidonic acid metabolism and linoleic acid metaoblism pathways were the most significantly enriched pathways response to SBE in LPS induced inflammatory model. Besides, SBE could inhibit the expression of the pro-inflammatory cytokines IL-1β and TNF-ɑ, and downregulation of the macrophage migration accelerator VEGFR1 in a dose dependent manner; (4) Conclusions: These findings indicated that SBE may exerted anti-inflammatory ability by regulating multiple fatty acids metabolism pathways as well as inhibiting the secretion of pro-inflammatory cytokines and VEGFR. This study provides evidences for Scutellaria baicalensis as the material for developing natural, effective anti-inflammatory products.     

Anti-inflammatory activity of saponins from roots of Impatiens parviflora DC.

Abstract

Two triterpene saponins (IPS-1, IPS-2) for the first time were isolated from the roots of Impatiens parviflora DC. (Balsaminaceae). Their anti-inflammatory activity was evaluated by means of two in vitro models: anti-hyaluronidase and anti-denaturation assays. Both saponins were shown to be potent hyaluronidase inhibitors that affect the enzyme in a dose-dependent manner. The anti-hyaluronidase effect of IPS-2 (IC₅₀?=?286.7?µg/mL) was higher than that of the reference drug: escin (IC₅₀?=?303.93?µg/mL). Both saponins protected bovine serum albumin from heat-induced denaturation in a dose-dependent manner. IPS-1 demonstrated higher anti-denaturation effect (IC₅₀?=?86.7?µg/ml) than IPS-2 (IC₅₀?=?109.76?µg/mL) or the standard drug: acetylsalicylic acid (IC₅₀?=?262.22?µg/mL). In conclusion, potent activity of IPS-1, IPS-2 in both in vitro assays shows that saponins from I. parviflora have anti-inflammatory activity. The obtained results allow to suggest that such compounds may be beneficial in inflammatory conditions, especially associated with excessive degradation of hyaluronic acid.     

Anti-inflammatory activity of heterocyclic systems using abietic acid as starting material

A series of pyridines, pyrimidinone, oxazinones, and their derivatives were synthesized as anti-inflammatory agents using abietic acid (7-isopropyl-1,4a-dimethyl-1,2,3,4,4a,4b,5,6,10,10a-decahydrophenanthrene-1-carboxylic acid) as the starting material. The arylidiene derivative was treated with cyanothioacetamide to give cyano pyridine-thione, which was reacted with ethyl chloroacetate to yield the corresponding cyano ester. The ester was hydrolysed to the sodium salt, which was reacted with acetic anhydride to afford 2-methyloxazinone, which was treated with ammonium acetate to afford 2-methylpyrimidinone followed by methylation with methyl iodide to yield 2,3-dimethyl- pyrimidinone. In addition, the oxazinone derivative was reacted with aniline or hydrazine hydrate to give 3-phenyl- or 3-aminopyrimidinones. The latter reacted with thiophene-2-carboxaldehyde or phenylisothiocyanate to afford Schiff’s bases or thiosemicarbazide derivatives. The pharmacological screening showed that many of these compounds have good anti-inflammatory activity comparable to Prednisolone^® as reference drug.     

Anti-inflammatory activity of alkaloids: an update from 2000 to 2010

Many natural substances with proven anti-inflammatory activity have been isolated throughout the years. The aim of this review is to review naturally sourced alkaloids with anti-inflammatory effects reported from 2000 to 2010. The assays were conducted mostly in vivo, and carrageenan-induced pedal edema was the most used experimental model. Of the 49 alkaloids evaluated, 40 demonstrated anti-inflammatory activity. Of these the most studied type were the isoquinolines. This review was based on NAPRALERT data bank, Web of Science and Chemical Abstracts. In this review, 95 references are cited.     

Anti-inflammatory activity of a novel flavonol glycoside from the Bauhinia variegata Linn

Bauhinia variegata Linn. (Leguminosae) is commonly known as 'Kachnar' in Hindi. It is distributed almost throught India. Its powdered bark is traditionally used for tonic, astrain, ulcers. It is also useful in skin diseases. The roots are used as antidote to snake poison. The present article deals with the isolation and structural elucidation of a novel flavonol glycoside 5,7,3',4'-tetrahydroxy-3-methoxy-7-O-alpha-L-rhamnopyranosyl(1-->3)-O-beta-galactopyranoside (1) from the roots of Bauhinia Variegata and its structure was identified by spectral analysis and chemical degradations. The novel compound (1) showed anti-inflammatory activity.     

Pharmacological activity of ethanolic extract of Alhagi maurorum roots

The ethanolic extract (EE) of Ahagi maurorum powdered roots was examined for its pharmacological activity and showed the following results: (1) Administration of EE intraperitoneally into mice decreased the body temperature in a dose-dependent manner. The decreases ranged from 0.2 to 3.3 °C. (2) Treatment of the frog tissue with EE blocked the action of the neurotransmitter, acetyl choline (Ach). Thus, EE seemed to act as a skeletal muscle relaxant. (3) Intraperitoneal administration of EE into the anaesthetized rats decreased heart rate by 22.5%, thus, EE seemed to be a bradycardiogenic drug. (4) The extract induced relaxations to the guinea-pig ureter and suppressed histamine-induced spasms. It seemed to possess a spasmolytic action and a ureter relaxing action that can enhance getting rid of renal stones and relieve of the accompanying pain (contraction of the ureter). (5) The extract did not possess the property of enhancing dissolution of oxalate calculi.     

双波长分光光度法测定青麻果实中锌含量

在pH=6.0的六亚甲基四胺缓冲溶液中,Zn~(2+)与二甲酚橙形成红色配合物,以试剂空白为参比,在570nm处褪色,在440nm处生色,实验表明在一定范围内△A=A440-A570与Zn~(2+)浓度呈线性,建立了双波长分光光度法测定青麻果实中Zn~(2+)含量的方法。最佳实验条件下,Zn~(2+)含量在0.1~0.6μg/mL范围内符合Lambert-Bill定律,检出限为1.5×10~(-2)μg/mL。结果表明,方法的相对标准偏差小于5%,加标回收率为95.0%~96.0%。方法简便快速。     

Properties of colony promoting activity in procine kidney extract

Aqueous extracts prepared from procine kidneys (PKE) possess colony-promoting activity (CPA) which increases the number of granulocyte and macrophage colonies in semi-solid cultures of mouse bone marrow cells (BMC) in the presence of colony-stimulating factor (GM-CSF). PKE was totally inactivated by 15 mM N-ethylmaleimide, but was resistant to 5 mM dithiothreitol (DTT), 50 mM sodium metaperiodate and a mixture of diisopropylether-n-BuOH (3:2). The proportion of deoxyribonucleic acid (DNA)-synthesizing cells of the PKE-responsive cells was about one-half in comparison to those of CSF-responsive cells, as estimated using the hydroxyurea (HU) suicide method. Upon marrow preincubation with PKE in liquid culture for 24 h, the suicide rate of the colony forming unit in culture (CFU-C) by HU increased to 3 times compared to that of the control. Since cyclophosphamide (CY) induces a change in the number of CFU-C, the effects of PKE on BMC obtained from CY injected mice were investigated. On day 1, the number of PKE-responsive cells significantly increased by about 2.3 times in comparison with that of control, whereas the number of CFU-C per 1 x 10(4) cells significantly decreased to about one-eighth of that of control. These results suggest that a sulfhydryl group(s) is required for the appearance of the colony-promoting activity of PKE, and glycoproteins, glycopeptides or hydrophobic components are not required; they also suggest that PKE may act on immature granulocyte/macrophage progenitors, which are younger than CSF-responsive CFU-C.