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The quality of herbal drugs is usually controlled using several tests recommended in a monograph. HPTLC is the method of choice for identification in many pharmacopoeias. If combined with a suitable reference material for comparison, HPTLC can provide information beyond identification and thus may simplify quality control. This paper describes, as a proof of concept, how HPTLC can be applied to define specifications for an herbal reference material and to control the quality of an herbal drug according to these specifications. Based on multiple batches of cultivated Angelica gigas root, a specific HPTLC method for identification was optimized. This method can distinguish 27 related species. It also can detect the presence of mixtures of A. gigas with two other Angelica species traded as "Dang gui" and is suitable as well for quantitative assessment of samples in a test for minimum content of the sum of decursin and decursinol angelate. The new concept of "comprehensive HPTLC fingerprinting" is proposed: HPTLC fingerprints (images), which are used for identification, are converted into peak profiles and the intensities of selected zones are quantitatively compared to those of the corresponding zones of the reference material. Following a collaborative trial involving three laboratories in three countries, the method was applied to check the quality of further candidates for establishing an appropriate reference material. In conclusion, this case demonstrates that a single HPTLC analysis can provide information about identity, purity, and minimum content of markers of an herbal drug. [ABSTRACT FROM AUTHOR]

The aim of this study was to prove whether Ginkgo biloba food supplements on the European market comply with pharmaceutical quality, and whether their composition satisfies the European Pharmacopoeia criteria. Medicinal products containing a standardised Ginkgo leaf extract are used for the improvement of cognitive impairment and quality of life in mild dementia. Further, Ginkgonis folium is used for the treatment of peripheral circulation disorders. Pharmacopoeial Ginkgo dry extract contains 22.0-27.0% flavonoids and 5.4-6.6% terpene lactones (ginkgolides, bilobalide). In addition to its widespread use as an herbal medicine (herbal medicinal product), the same extract can be an ingredient in food supplements. The content of active secondary metabolites was quantified in a number of European food supplements containing Ginkgo dry extract or Ginkgo leaf. Flavonoids were quantified using a modified pharmacopoeial HPLC-UV method, and terpene lactones (ginkgolides A, B, C, and bilobalide) using LC-MS/MS. Some Ginkgo leaf supplement samples were also analysed by microscopy. The quality of food supplements on the European market is dubious. In this paper, we present selected examples of several methods of adulteration and falsification, including higher/lower doses of Ginkgo dry extractor Ginkgo leaf than declared and the addition of undeclared extraneous materials. These examples reveal several patterns in the manufacturing of adulterated products. [ABSTRACT FROM AUTHOR]

Isocorynoxeine, one of the major alkaloids from Uncaria Hook, shows the effects of lowering blood pressure, vasodilatation, and protection against ischemia-induced neuronal damage. In this paper, the metabolism of isocorynoxeine was investigated in rats. Twelve metabolites and the parent drug were isolated by using solvent extraction and repeated chromatographic methods, and determined by spectroscopic methods including UV, MS, NMR, and CD experiments. Seven new compounds were identified as 11-hydroxyisocorynoxeine, 5-oxoisocorynoxeinic acid-22-O-β-Dglucuronide, 10-hydroxyisocorynoxeine, 17-Odemethyl-16,17-dihydro-5-oxoisocorynoxeine, 5-oxoisocorynoxeinic acid, 21-hydroxy-5-oxoisocorynoxeine, and oxireno[18, 19]-5-oxoisocorynoxeine, together with six known compounds identified as isocorynoxeine, 18,19-dehydrocorynoxinic acid, 18,19-dehydrocorynoxinic acid B, corynoxeine, isocorynoxeine-N-oxide, and corynoxeine-N-oxide. Possible metabolic pathways of isocorynoxeine are proposed. Furthermore, the activity assay for the parent drug and some of its metabolites showed that isocorynoxeine exhibited a significant neuroprotective effect against glutamate-induced HT22 cell death at the maximum concentration. However, little or weak neuroprotective activities were observed for M-3, M-6, M-7, and M-10. Our present study is important to further understand their metabolic fate and disposition in humans. [ABSTRACT FROM AUTHOR]

In this paper, the chemical composition and biological activity of the essential oil of Artemisia absinthium was studied. The aim of this study was to investigate the potential of ethnopharmacological uses of this plant species in the treatment of gastrointestinal diseases and wounds, and as an insect repellent. The aerial part of the plant was hydrodistilled, and the chemical composition of the essential oil was analyzed by gas chromatography and gas chromatography/mass spectrometry. Forty-seven compounds, corresponding to 94.65% of the total oil, were identified, with the main constituents being sabinene (24.49%), sabinyl acetate (13.64%), and α-phellandrene (10.29%). The oil yield was 0.23% (v/w). The antimicrobial activity of the oil was investigated against ten bacterial isolates (from patients wounds and stools) and seven American Type Culture Collection strains using a microwell dilution assay. The minimal inhibitory/bactericidal concentration of the oil ranged from <0.08 to 2.43 mg/mL and from 0.08 to 38.80 mg/mL, respectively. The antioxidant activity of the essential oil was evaluated using 2,2-diphenyl-1-picrylhydrazil and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) radical-scavenging methods and assessed as significant. Skin irritation potential and acute toxicity of the oil were also investigated. Results of the skin irritant reaction showed that none of the 30 volunteers developed a positive skin irritant reaction to undiluted A. absinthium essential oil. Acute oral exposure to the essential oil did not cause mortality in the treated mice, but it did cause neurological, muscle, and gastrointestinal problems. A subchronic toxicity test on Drosophila melanogaster showed that the essential oil of A. absinthium is toxic for developing insect larvae. Starting with the concentration of 0.38% of essential oil in medium, significant mortality of larvae exposed to the oil was noted when compared to the control. Probit analysis revealed that the LC50 value of A. absinthium essential oil for D. melanogaster larvae after 15 days of exposure was 6.31 % (49 mg/mL). The essential oil also affected the development of D. melanogaster larvae and significantly delayed achievement of the pupa stadium. [ABSTRACT FROM AUTHOR]

Artemisia species possess pharmacological properties that are used for medical purposes worldwide. In this paper, the essential oils from the aerial parts of Artemisia nilagirica and Artemisia maritima from the western Indian Himalaya region are described. The main compounds analyzed by simultaneous GC/MS and GC/FID were camphor and 1,8-cineole from A. maritima, and camphor and artemisia ketone from A. nilagirica. Additionally, the oilswere evaluated for their antibacterial, antifungal, mosquito biting deterrent, and larvicidal activities. A. nilagirica essential oil demonstrated nonselective antifungal activity against plant pathogens Colletotrichum acutatum, Colletotrichum fragariae, and Colletotrichum gloeosporioides, whereas A. maritima did not showantifungal activity. Both Artemisia spp. exhibited considerable mosquito biting deterrence, whereas only A. nilagirica showed larvicidal activity against Aedes aegypti. Antibacterial effects assessed by an agar dilution assay demonstrated greater activity of A. maritima essential oil against Staphylococcus aureus and Pseudomonas aeruginosa compared to A. nilagirica. [ABSTRACT FROM AUTHOR]

Osteoporosis is one of the major metabolic bone diseases and is among the most challenging non-communicable diseases to treat. Although there is an increasing interest in identifying bioactive molecules for the prevention and management of osteoporosis, such studies principally focus only on differentiation and mineralization of osteoblasts or inhibition of osteoclast activity. Stimulation of osteoblast migration must be a promising osteoanabolic strategy for improved metabolic bone disease therapy. In this study, we show that an anthraquinone derivative, aurantio-obtusin, stimulated chemotactic migration of MC3T3-E1 osteoblast cells in a concentration-dependent manner. The use of a real-time chemotaxis analyzing system, TAXIScan, facilitated the evaluation of both velocity and directionality of osteoblast migration in response to the compound. Besides migration, the compound stimulated osteoblast differentiation andmineralization. Taken together, the data presented in this paper demonstrate that aurantio-obtusin is a promising osteoanabolic compound of natural origin with potential therapeutic applications in the prevention of osteoporosis and other metabolic bone diseases. [ABSTRACT FROM AUTHOR]

This paper reports the phytochemical investigation of the 50% aq. EtOH extract of Houttuynia cordata, an effective TCM and functional food in China, which led to the isolation of 17 flavonoids including four new ones. The four new compounds were flavonoid derivatives tethered with houttuynin (3-oxododecanal). Each of the new compounds was obtained as a pair of inseparable diasteriomeric epimers due to the chiral carbon of hemiketal at C-3". This phenomenon is rooted in the ring-chain tautomerism of the hemiketal functional group in solution, which was proved by dynamic NMR experiments. The new compounds 1-4 displayed inhibitory activities against herpes simplex virus 1, with respective IC50 values of 38.46, 14.10, 62.00 and 70.76 μM, which was associated with the medicinal functions of H. cordata. [ABSTRACT FROM AUTHOR]

Icariin is a major active component isolated from the traditional Chinese herb Epimedium brevicornum, with a wide range of pharmacological and biological activities. In this paper, we investigated the effects of icariin on hyperlipidemia, and further evaluated whether icariin could improve unfavorable hemorheological parameters, attenuate platelet activation and facilitate the balance between plasmic plasminogen activator inhibitor-1 and tissue-type plasminogen activator activities in rabbits fed a high-cholesterol diet. Icariin reduced the levels of serum total cholesterol and low-density lipoprotein cholesterol, as well as the atherosclerotic burden. In addition, this compound has been found to improve the imbalance between plasmic plasminogen activator inhibitor-1 and tissue-type plasminogen activator activities, reduce platelet adhesiveness and aggregation and modulate unfavorable hemorheological variables in hypercholesterolemia. In conclusion, icariin has lipid-lowering effects and may be used in the treatment and prevention of thrombosis in the atherosclerotic process. [ABSTRACT FROM AUTHOR]

In our previous study, fourty-eight compounds have been isolated and identified from the roots of Picrasma quassioides, which have been widely used as a traditional Chinese medicine for clearing heat and for detoxification as described in the Chinese Pharmacopoeia. β-Carboline alkaloids are commonly considered as main active constituents of P. quassioides, but the molecular mechanism remains yet unknown. In the present paper, one new β-carboline alkaloid together with two known β-carboline alkaloids have been investigated for their anti-inflammatory effect and mechanism of action in cultured macrophage RAW 264.7 cells. Griess assay was used to evaluate the inhibitory effect on the overproduction of nitric oxide. ELISA was used to determine the level of proinflammatory cytokines including TNF-α and IL-6. The inhibitory effect on the enzymatic activity of COX-2 and inducible nitric oxide synthase were tested by colorimetric and fluorimetric methods, respectively. Western blot was used to detect the expression of inducible nitric oxide synthase and COX-2. All three β-carboline alkaloids suppressed LPS-stimulated nitric oxide production and proinflammatory cytokines secretion, including TNF-α and IL-6 in a dose-dependent manner. They also strongly inhibited the expression of inducible nitric oxide synthase and inducible nitric oxide synthase enzymatic activity, whereas the expression of COX-2 and COX-2 enzymatic activity were not affected. These results indicated that potent inhibition of nitric oxide, TNF-α, and IL-6, but not COX-2 expression and COX-2 activity, might constitute the anti-inflammatory mechanism of β-carboline alkaloids. β-Carboline alkaloids suppressed the overproduction of nitric oxide through downregulation of inducible nitric oxide synthase expression and inducible nitric oxide synthase enzymatic activity in an LPS-stimulated macrophage. [ABSTRACT FROM AUTHOR]

In this paper, we report a case of misidentification of medicinal plants involving dried petals of Papaver rhoeas (red poppy) contaminated with Papaver bracteatum (scarlet poppy) petals. Preliminary TLC analysis indicated the presence of thebaine either in the fluid extracts or in the petals. It was therefore necessary to carry out an accurate botanic examination of the plant material, which revealed contamination of the red poppy petals with scarlet poppy petals. Moreover, to confirm the adulteration, we developed and validated an efficient, reversed-phase ion pair HPLC method for determination of the alkaloids specific for the Papaver species. Six petal batches and five commercial fluid extracts were analyzed. Only one petal batch from Iran contained thebaine and its analogue oripavine while the alkaloids typical for the Papaver bracteatum species were identified in all fluid extracts, meaning that they were all prepared with contaminated petals. [ABSTRACT FROM AUTHOR]

Multidrug resistance (MDR) of tumor cells is one of the major problems encountered during cancer chemotherapy. In this paper, we isolated eight triterpenoids from Poria cocos and evaluated their effects on reversing MDR of KBV200 cells. Eight triterpenoids increase significantly vincristine-induced cytotoxicity in drug-resistant KBV200 cells at the concentrations of 12.5 µg/mL and 25 µg/mL. Dehydrotumulosic acid showed the best reversal effect: it increased KBV200 apoptosis induced by vincristine and inhibited P-gp function through enhancing the accumulation and retention of fluorescent P-gp substrate rhodamine 123 in KBV200 cells but had no effect on P-gp expression. [ABSTRACT FROM AUTHOR]

Three new β-indoloquinazoline alkaloids, orirenierine A (1), B (2) and C (4), together with eleven known compounds were isolated from the methanol extract of the stems of Oricia renieri. The structures of all compounds were determined by comprehensive analyses of their spectroscopic data and comparison with literature information. The alkaloids 9-11 were isolated for the first time from this genus. All compounds were tested for their activity against bacteria, fungi, and plant pathogen oomycetes using the paper disk agar diffusion assay. The agar diffusion test gave only low antimicrobial activities, corresponding to MICs > 1 mg/mL. However, compounds 1-4 and 11 exhibited a strong suppressive effect on phagocytosis response upon activation with serum opsonized zymosan in the range of IC50 = 2.6- 6.5 μM, while low cytotoxic activity against the human Caucasian prostate adenocarcinoma cell line PC-3 was observed with IC50 values ranging from 22.9 to 39.4 μM. [ABSTRACT FROM AUTHOR]