Chemical Constituents of Anaxagorea Javanica and Their Antioxidant and Anti-Inflammatory Activities

Anaxagorea javanica Blume (synonym A. scortechinii King) or locally known as ‘bunga pompun’, ‘kekapur’, ‘larak lecek’, ‘akar angin’, ‘kinchong’ or ‘atis’ is an endermic plant in Malaysia. The plant belongs to Annonaceae family and is traditionally used for the treatment after childbirth. Phytochemical investigation on the bark and root of this plant yielded seventeen pure compounds, comprising steroids, fatty acids, simple phenolics, alkaloids, flavonoids and sesquiterpenes. In total, seven alkaloids were isolated, out of which two new derivatives of copyrine alkaloid were 4,11-dimethoxyeupolauridine (87) and 2-methoxy-3-hydroxyeupolauridine (88) in addition to four known compounds, eupolauridine (22), 11- methoxyeupolauridine (86), sampangine (95) and 3-methoxysampangine (96). Another known alkaloid came from oxoaporphine was lysicamine (91). The isolation of copyrine and oxoaporphine alkaloids was a first time from the genus. Other known compounds isolated, included a mixture of β-sitosterol (49) and stigmasterol (94), quercetin (46), 7α-hydroxystigmasterol (92), 7-oxostigmasterol (93), 4-hydroxybutanamide (95), tetradecanoic acid (96), syringic aldehyde (97) and 2,3-dihydroxy-1-(4’-hydroxy-3’,5’-dimethoxyphenyl)-1-propanone (98). A novel sesquiterpene identified as 2,2,9-trimethyl-5-methylene-12-oxa-bicyclo[6.3.1]dodecane-4,9-diol (85) (nordine) was also isolated. All structures were elucidated by spectroscopic techniques and by comparison with data available from literature. Studies on the biological activities related to inflammation were conducted using nitric oxide (NO) and 5-lipoxygenase (5-LOX) inhibitory assay as a priminary screening as well as antioxidant assay. The results showed that both hexane and dichloromethane extracts from the barks possessed weak inhibition on NO production at the highest concentration of 200 μg/ml without cytotoxic effect. Meanwhile, inhibition of lipoxygenase activity was shown only by methanolic and acetone extracts from roots at 100 μg/ml with an IC50 of 48.21 and 63.87 μg/ml, respectively. However, all the crude extracts from barks and roots are poor radical scavenger inhibitors. Further in vitro investigation on the selected pure compounds showed that only sampangine (89) and 3- methoxysampangine (90) significantly inhibited NO production with IC50 values of 18.17 and 32.25 μg/ml, respectively, at the highest concentration of 25 μg/ml tested

Ficus carica

This paper describes the botanical features of Ficus carica L. (Moraceae), its wide variety of chemical constituents, its use in traditional medicine as remedies for many health problems, and its biological activities. The plant has been used traditionally to treat various ailments such as gastric problems, inflammation, and cancer. Phytochemical studies on the leaves and fruits of the plant have shown that they are rich in phenolics, organic acids, and volatile compounds. However, there is little information on the phytochemicals present in the stem and root. Reports on the biological activities of the plant are mainly on its crude extracts which have been proven to possess many biological activities. Some of the most interesting therapeutic effects include anticancer, hepatoprotective, hypoglycemic, hypolipidemic, and antimicrobial activities. Thus, studies related to identification of the bioactive compounds and correlating them to their biological activities are very useful for further research to explore the potential of F. carica as a source of therapeutic agents

Inhibition of the chemiluminescence and chemotactic activity of phagocytes for selected Ficus species extract and their lipoxygenase and xanthine oxidase enzyme inhibitory

The effects of crude methanol from seven Ficus species on reactive oxygen species (ROS) production were evaluated using luminol based chemiluminescence assay and their inhibition of PMNs chemotaxis was investigated using Boyden chamber technique. Crude methanol of F. aurantiaca, F. parietalis, and F. annulata showed strong activity against PMN chemotaxis with IC 50 values of 1.4, 0.3 and 2.2 µg/mL, respectively, while crude methanol from F. aurantiaca and F. parietalis on whole blood and ROS production of PMNs exhibited high inhibitory activity for luminol enhanced chemiluminescence with IC 50 values of 1.4, 0.9, and 1.0, 0.4 µg/mL, respectively. In xanthine oxidase inhibition assay, crude methanol from F. aurantiaca (stem), F. parietalis (stem), and F. annulata (leaf) exhibited greater than 92% inhibition at concentration of 100 µg/mL (with IC50 values of 0.9, 1.0 and 8.9 µg/mL, respectively) while some extracts of other species showed more than 60% inhibitions at this concentration. In soybean lipoxygenase (SBL) assay, the methanolic extracts of these 3 species showed potent SBL inhibition with IC50 values of 0.3, 0.7, and 6.3 µg/mL, respectively. The overall results suggest that F. parietalis, F. annulata, and F. aurantiaca might be a prospective source of anti-inflammatory mediators and as a source of new immunomodulatory agents

Inhibitory Effects of Standardized Extracts of Phyllanthus amarus

The standardized methanol extracts of Phyllanthus amarus and P. urinaria, collected from Malaysia and Indonesia, and their isolated chemical markers, phyllanthin and hypophyllanthin, were evaluated for their effects on the chemotaxis, phagocytosis and chemiluminescence of human phagocytes. All the plant extracts strongly inhibited the migration of polymorphonuclear leukocytes (PMNs) with the Malaysian P. amarus showing the strongest inhibitory activity (IC50 value, 1.1 µg/mL). There was moderate inhibition by the extracts of the bacteria engulfment by the phagocytes with the Malaysian P. amarus exhibiting the highest inhibition (50.8% of phagocytizing cells). The Malaysian P. amarus and P. urinaria showed strong reactive oxygen species (ROS) inhibitory activity, with both extracts exhibiting IC50 value of 0.7 µg/mL. Phyllanthin and hypophyllanthin exhibited relatively strong activity against PMNs chemotaxis, with IC50 values slightly lower than that of ibuprofen (1.4 µg/mL). Phyllanthin exhibited strong inhibitory activity on the oxidative burst with an IC50 value comparable to that of aspirin (1.9 µg/mL). Phyllanthin exhibited strong engulfment inhibitory activity with percentage of phagocytizing cells of 14.2 and 27.1% for neutrophils and monocytes, respectively. The strong inhibitory activity of the extracts was due to the presence of high amounts of phyllanthin and hypophyllanthin although other constituents may also contribute

Design and characterisation of curcumin-loaded nanostructured lipid carriers for safe and efficient topical drug delivery in the treatment of pressure ulcer

Pressure ulcers (PU) are chronic lesions with a high prevalence in at-risk populations. Although curcumin has various therapeutic properties, its use as a dermal therapeutic agent is limited by its poor solubility and permeability. This study aimed to develop nanostructured lipid carriers (NLCs) to facilitate the topical use of curcumin as wound healing agent in treating PU. The optimised curcumin-NLCs were characterised for their physicochemical properties, drug release, and skin permeation, while effectiveness and toxicity were investigated via cell viability, scratch assays, and an in vivo skin irritation test. The optimised curcumin-NLCs comprised 3.5% solid lipids, 1% surfactant, and 2% co-surfactant with an average particle size of 134.68±6.0 nm, polydispersity index of 0.248±0.00, zeta potential of −44.94±5.44, percentage of encapsulation efficiency of 93.42±0.32%, and drug loading of 0.11±0.00%. CurcuminNLCs showed stable physicochemical properties and extended drug release for up to 48 h, with a cumulative release of 77.72% following a first-order kinetics. The formulation exhibited slower curcumin permeation than the free curcumin. Furthermore, the safe and non-toxic curcumin-NLCs were highly effective at 0.98 µM and showed a high rate of wound closure without skin irritation. Collectively, the NLCs developed for topical delivery of curcumin demonstrated prolonged and sustained release and improved wound healing activity, which indicates that curcuminNLCs are a viable strategy for treating PU

The effects of the fractions of Piper sarmentosum leaves on inhibition of adipogenesis of 3T3 L1 preadipocytes

Piper sarmentosum Roxb. was reported to have anti-obesity, hypoglycaemic and anti-oxidant properties. The aim of this study was to identify the fractions of P. sarmentosum leaf extract in inhibiting adipogenesis of 3T3L1 preadipocytes. The crude extract of the P. sarmentosum leaves was fractionated to produce hexane, dichloromethane, methanol, and aqueous fractions. Various dilutions of the fractions; hexane (0.1 - 1 μg/mL), dichloromethane (9.76 - 97.6 μg/mL), methanol (3.6 - 36 mg/mL), and aqueous (1 - 10 mg/mL), were treated onto the 3T3L1 preadipocytes from 3rd to 15th day of culture. The crude extract (1 - 10 mg/mL) and glycyrrhizic acid (GCA) (0.24 - 2.4 mg/mL) were used as positive controls. The viability of the adipocytes was measured by MTT assay at the 15th day of culture. The content of each fraction was quantified with reference standards of naringin, naringenin, pellitorine, sarmentosine and β-sitosterol by using HPLC. The results showed that 49.1% of the crude extract contained aqueous fraction, 0.12% in hexane fraction, 9.7% in dichloromethane fraction and 36% in methanol fraction. The aqueous fraction and crude extract at the dose of 7 mg/mL and GCA at the dose of 1.92 mg/mL showed potent inhibitory effects on the adipogenesis. However, none of the reference standards were identified from the fractions using HPLC analysis. In conclusion, the aqueous fraction was the main fraction in the crude extract of the P. sarmentosum and contributed a significant role in inhibiting adipogenesis of the 3T3L1 preadipocytes

Perbandingan Pelbagai Kaedah Pengekstrakan Air Labisia pumila var. alata

The water decoction of Labisia pumila var. alata is used traditionally in childbirth, as well as for the treatment of flatulence, dysentery, dysmenorrhoea and join pains. This study was carried out to determine the best method and optimum parameters of aqueous axtraction of the leaves and roots of this species. The laboratory methos esed were maceration, ddecoction, reflux and Saxhlet, whereas the parameters studied were temperature, duration and pH of axtraction. The yields and thin layer chromatographic profiles of the freeze-dried extracts were analysed. The study showed that in general the percentage yields of the water soluble extracts were higher for the roots than the leaves, as well as the extracts obtained from heating than those obtained at room temperature. The most effective extraction parameters for L. pumila var. alata were as follows:maceration (25 C, at least 6 hr), decoction (60 C, not exceeding 10 min) and reflux (100 C, not exceeding 4 hr). Saxhlet method was found to be the least effective. The pH analysis had shown the possibility of degradation of some of the phytochemicals at extreme pH values of 1,2 and 14

Xanthine oxidase inhibitory and DPPH radical scavenging activities of some primulaceae species

Xanthine oxidase (XO) is an enzyme that catalyzes the metabolism of hypoxanthine and xanthine into uric acid. XO also serves as an important biological source of free radicals that contribute to oxidative damage involved in many pathological processes. Antioxidant effects of several Primulaceae species have been reported but their XO inhibitory activity has not been investigated. Thus, this study was conducted to determine the XO inhibitory and free radical scavenging activities of Primulaceae species and to correlate these activities with their total phenolic contents (TPC). A total of 129 extracts of different plant parts of twelve Primulaceae species were assayed for XO inhibition spectrophotometrically at 290 nm using allopurinol as a positive control. The antioxidant activity was determined using 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging assay and TPC of the extracts were determined by the Folin-Ciocalteau method. The Pearson correlation analysis indicated that the TPC of the extracts showed moderate positive correlations with XO inhibition (r=0.31, p<0.05) and DPPH antioxidant activity (r=0.31, p<0.05) for all of the dichloromethane extracts. Amongst the extracts tested, the dichloromethane extract of the roots of Labisia pumila var. alata showed the strongest inhibitory effects for XO (IC50 4.8 μg/mL) and DPPH free radical capacity (IC50 1.7 μg/mL). The results suggested that Primulaceae species, particularly the dichloromethane extract of L. pumila var. alata roots, are the potential source of useful leads for the development of XO inhibitors

4,5,4′-Trihydroxychalcone, 8,8′-(ethene-1,2-diyl)-dinaphtalene-1,4,5-triol and rutin from Gynura segetum inhibit phagocytosis, lymphocyte proliferation, cytokine release and nitric oxide production from phagocytic cells

Abstract Background Gynura segetum is used traditionally to treat various ailments related to the immune system, which include cancer, inflammation, rheumatism, diabetes, hypertension, and viral infections but little studies have been carried out to validate their ethnopharmacological aspects. In this study the immunosuppressive effects of G. segetum and its constituents were investigated. Methods Isolation of compounds from G. segetum leaves was conducted using vacuum liquid chromatography (VLC) and column chromatography (CC). Two new compounds, namely 4,5,4'-trihydroxychalcone and 8,8'-(ethene-1,2-diyl)-dinaphtalene-1,4,5-triol, together with stigmasterol and β-sitosterol were isolated from G. segetum methanol extract and their structures were determined spectroscopically. The presence of gallic acid and rutin in the extract was determined quantitatively by a validated HPLC method. G. segetum methanol extract and its constituents were investigated for their effects on chemotaxis, phagocytosis, β2 integrin (CD18) expression, and reactive oxygen species (ROS) of polymorphonuclear leukocytes (PMNs), lymphocytes proliferation, cytokine release and nitric oxide (NO) production of phagocytes. Results All the samples significantly inhibited all the innate immune responses tested except CD 18 expression on surface of leukocytes. Among the samples, 8,8'-(ethene-1,2-diyl)-dinaphtalene-1,4,5-triol exhibited the strongest inhibitory on chemotaxis, phagocytosis, ROS and NO production. The compound exhibited exceptionally strong inhibitions on ROS and chemotaxis activities with IC50 values lower than the positive controls, aspirin and ibuprofen, respectively. 4,5,4'-Trihydroxychalcone revealed the strongest immunosuppressive activity on proliferation of lymphocytes (IC50 value of 1.52 μM) and on release of IL-1β (IC50 value of 6.69 μM). Meanwhile rutin was the most potent sample against release of TNF-α from monocytes (IC50, 16.96 μM). Conclusion The extract showed strong immunosuppressive effects on various components of the immune system and these activities were possibly contributed mainly by 4,5,4'-trihydroxychalcone, 8,8'-(ethene-1,2-diyl)-dinaphtalene-1,4,5-triol and rutin

Annonaceae: Breaking the Wall of Inflammation

Inventories of tropical forests have listed Annonaceae as one of the most diverse plant families. For centuries, it is employed in traditional medicines to cure various pathological conditions including snakebite, analgesic, astringent, diarrhea, dysentery, arthritis pain, rheumatism, neuralgia, and weight loss etc. Phytochemical analysis of Annonaceae family have reported the occurrence of alkaloids, flavonoids, triterpenes, diterpenes and diterpene flavone glycosides, sterols, lignans, and annonaceous acetogenin characteristically affiliated with Annonaceae sp. Numerous past studies have underlined the pleotropic pharmacological activities of the crude extracts and isolated compounds from Annonaceae species. This review is an effort to abridge the ethnobotany, morphology, phytochemistry, toxicity, and particularly focusing on the anti-inflammatory activity of the Annonaceae species