Flavonoids are mainly contained in the vegetables and medicinal herbs. Until now, over 5,000 kinds of flavonoid have been identified and their biological activities have been reported. Among them, we are interested in oroxylin A and spinosin because of their specific structures having bulky group at C-6 of ring A. Oroxylin A is contained in the Scutellaria baicalensis and exhibits cognitive enhancing activity as a GABA_A receptor antagonist, which is different from those of mainly contained in the S. baicalenis, baicalein or wogonin. Spinosin is isolated from Zizyphus jujuba var. spinosa and mainly studied as a hypnotic or anxiolytic agent because of traditional knowledge about its original herb. As far as we know, the cognitive function of spinosin was first identified by our group. In this review, we discuss how such flavonoids exert their pharmacological activities associated with cognitive function based on the receptor binding study and behavioral studies. Traditional knowledge and reverse pharmacology may be addressed in the research field of phytochemical pharmacology and useful to unveil the secret of phytochemicals.

Endophytes are defined as microorganisms that spend part of lifetime interior of plant tissues without causing negative effects. They have been used for agricultural purpose, biofuel production, bioremediation, medication, etc. In particular, endophytes have been emerged as a good source for bioactive secondary metabolites. A large number of secondary metabolites are currently being reported. In this report, we focus on the secondary metabolites that were originated from endophytic fungi inhabiting medicinal plants. They were classified into several groups such as nitrogenous compounds, steroids, sulfide-containing metabolites, terpenoids, polyketides, and miscellaneous for discussion of chemical structures and biological activities.

The efficacy and side effects associated with anticancer drugs have attracted an extensive research focus. Onconephrology is an evolving field of nephrology that deals with the study of kidney diseases in cancer patients. Most renal diseases in cancer patients are unique, and management of renal disease can be challenging especially in the presence of continuing use of the nephrotoxic drugs. Cisplatin is one of the most important chemotherapeutic agents used in the treatment of various malignancies, such as head, neck, ovarian, and cervical cancers. The major limitation in the clinical use of cisplatin is its tendency to induce adverse effects, such as nephrotoxicity. Recently, plant-derived phytochemicals have emerged as novel agents providing protection against cisplatin-induced renal cytotoxicity. Owing to the diversity of phytochemicals, they cover a wide spectrum of therapeutic indications in cancer and inflammation and have been a productive source of lead compounds for the development of novel medications. Of these agents, the effectiveness of triterpenoids, isolated from various medicinal plants, against cisplatin-induced renal cytotoxicity has been reported most frequently compared to other phytochemicals. Triterpenes are one of the most numerous and diverse groups of plant natural products. Triterpenes ameliorate cisplatin-induced renal damage through multiple pathways by inhibiting reactive oxygen species, inflammation, down-regulation of the MAPK, apoptosis, and NF-κB signaling pathways and upregulation of Nrf2-mediated antioxidant defense mechanisms. Here, we reviewed recent findings on the natural compounds with protective potential in cisplatin-induced renal cytotoxicity, provided an overview of the protective effects and mechanisms that have been identified to date, and discussed strategies to reduce renal cytotoxicity induced by anticancer drugs.

The study was conducted for quantitive determination of macronutrients, micronutrients and heavy metals present in Spilanthes acmella Hutch and Dalz, a traditionally used important medicinal plant. The results illustrated the presence of substantial amounts of essential nutrient elements in different parts of the plant. K and Mg were detected in the range between 36.35 ± 1.01 to 67.78 ± 1.33 g/kg and 2.17 ± 0.13 to 7.02 ± 0.84 g/kg of DWS respectively. While the essential micronutrients Fe, Na, Mn, Zn and Cu were detected in the range between 62.62 ± 12.72 to 856.95 ± 76.61 mg/kg, 365.47 ± 23.84 to 633.03 ± 38.12 mg/kg, 51.66 ± 7.77 to 186.33 ± 13.92 mg/kg, 41.87 ± 2.85 to 53.89 ± 3.79 mg/kg and 18.49 ± 2.07 to 48.71 ± 4.89 mg/kg of DWS respectively. Besides, heavy metals (Cd, Ni and Pb) detected in some of the plant samples were beyond the maximum permissible limit (MPL) of FAO/WHO for herbal medicines. The concentrations of the essential nutrient elements except zinc were significantly different in different parts of the plant (p < 0.001). Further variation in the concentrations of the elements in the plant was observed with respect to seasonal changes and geographical conditions. Nevertheless the findings corroborate ethnomedicinal significance of the plant and signify the possibilibity of utilizing its standardized products for preparation of food supplements as well as multidimensional therapeutic herbal medicines.

This study focused on investigation of the immunosuppressive inhibitory effect through determination of IL-2 production of nine compounds (1 - 9) isolated from Chlamydomonas sp. KSF108. Among them, compounds 1, 5, and 6 displayed moderately inhibitory effects on IL-2 production at a concentration of 100 µM. In addition, the related ones including cytotoxic, anti-inflammatory, and anti-oxidant activities were also elucidated. 6 further displayed cytotoxic activity against the MCF-7 cell line, with an IC₅₀ value of 17.2 µM and 4, 6 - 7, and 9 possessed significant DPPH radical scavenging activity, with IC₅₀ values ranging from 3.1 to 4.4 µM. To the best of our knowledge, this is the first report on the bioactivity of isolated chemical constituents from the genus Chlamydomonas. Compounds 1 and 5 investigated for the first time in the activity of immunosuppressivity and 6 may come to serve as the most important marker in broad-spectrum activities of the secondary metabolites identified from C. sp. KSF108.

Citrus junos seeds (CS) have been traditionally used for the treatment of cancer and neuralgia. They are also used to manufacture edible oil and cosmetic perfume. A large amount of CS shells without oil (CSS) are discarded after the oil in CS is used as foods or herbal remedy. To efficiently utilize CSS as a by-products, it needs to be studied through chemical analysis. Therefore, we developed an ultra-performance liquid chromatography (UPLC)-diode array detection (DAD) method for simultaneous determination and quantitative analysis of five components (two flavonoids and threes limonoids) in CSS. A Waters Acquity UPLC HSS T3 column C18 (2.1 × 100 mm, 1.8 ㎛) was used for this separation. It was maintained at 40 ℃. The mobile phase used for the analysis was distilled water and acetonitrile with gradient elution. To identify the quantity of the five components, a mass spectrometer (MS) with an electrospray ionization (ESI) source was used. The regression equation showed great linearity, with correlation coefficient ≥ 0.9912. Limits of detection (LOD) and limits of quantification (LOQ) of the five compounds were 0.09 - 0.13 and 0.26 - 0.38 ㎍/mL, respectively. Recoveries of extraction ranged from 97.45% to 101.91%. Relative standard deviation (RSD) values of intra- and inter-day precision were 0.06 - 1.15% and 0.19 - 0.25%, respectively. This UPLC-DAD method can be validated to simultaneously analyze quantities of marker flavonoids and limonoids in CSS.

The plant Dendropanax morbifera Léveille is effective folk medicines for the treatment of several conditions, such as infectious diseases, skin diseases, and other illnesses. Although the inhibitory effects of D. morbifera on the proliferation and migration of vascular smooth muscle cells (VSMCs) have been shown in our previous study, its effects in vivo remain to be elucidated. In this study, we aimed to investigate the protective effects of the extracts from D. morbifera (EDM) on neointimal hyperplasia of rat carotid artery and explore the underlying mechanisms. We observed that the ratio of intima to media thickness (I/M) was significantly decreased in the EDM-treated groups by ~80% compared to that of the control. The expression of Ki-67 and proliferating cell nuclear antigen was decreased by ~70% in the EDM-treated groups compared to that of the control. In addition, matrix metalloproteinase (MMP)2 and MMP9 significantly reduced in the neointimal layer of the EDM-treated groups. Moreover, the decreased levels of contractile phenotypic markers of VSMCs, such as α-smooth muscle actin, myocardin, and smooth muscle-myosin heavy chain, were successfully restored by EDM treatment. Furthermore, the levels of synthetic phenotypic markers, cellular retinal binding protein 1 and connexin 43 were also restored to normal levels. These results suggest that EDM inhibits vascular neointimal hyperplasia induced by balloon injury in rats via phenotypic modulation of VSMCs. Therefore, EDM may be a potential drug candidate for the prevention of restenosis.

A new cinnamyl acid derivative, willughbein A (1) along with pinoresinol (2), alyterinate A (3), and scopoletin (4), were isolated from the roots of Willughbeia coriacea Wall. The structure of 1 has been determined based on HRESIMS, 1D, and 2D NMR spectral data. All of the isolates were evaluated for their cytotoxicity against three human cancer cells (HeLa, T47D, MCF-7, and P-388). Compound 3 showed moderate activity against P-388 cells with an IC₅₀ value of 3.04 ㎍/mL.

Osteoporosis is a worldwide disease leading to significant economic and societal burdens globally. Osteoporosis is caused by unbalanced bone remodeling between the rate of osteoclast bone resorption and osteoblast bone formation. Acer tegmentosum Maxim (AT) is a traditional herbal medicine containing multiple biological activities such as anti-oxidant and anti-inflammatory purposes. However, its role in osteoporosis has not been fully studied. Therefore, we investigated whether AT has a potent inhibitory effect on osteoporosis and its mechanism through a systemic evaluation in ovariectomized (OVX) mice. OVX mice were orally administrated with the AT at doses of 50, 100, and 200 mg/kg for 10 weeks. Histological images and histomorphometry analyses were performed by H&E and Toluidine blue satin, and the expression levels of receptor activator for nuclear factor-kB ligand (RANKL), nuclear factor of activated T cells cytoplasm 1 (NFATc1), c-Fos, and matrix metalloproteinase 9 (MMP9) related to the osteoclast differentiation were investigated using immunohistochemical analysis. Administration of AT prevented bone loss and the alternations of osteoporotic bone parameters at the distinct regions of the distal femur and spongiosa region in OVX mice. Further, administration of AT increased periosteal bone formation in a dose-dependent manner. Meanwhile, AT inhibited not only the expression of NFATc1 and c-Fos, which are two major regulators of osteoclastogenesis but also reduced bone resorbed encoding expression of MMP9 and RANKL. Our results indicated that administration of AT prevented bone loss and the alternations of osteoporotic bone parameters at the distinct regions of the distal femur and spongiosa region in OVX mice. Also AT has the bone protective effect through the suppression of osteoclast and promotion of osteoblast, suggesting that it could be a preventive and therapeutic candidate for anti-osteoporosis.

Artemisia capillaris Thunb. (Compositae) is a traditional medicinal plant with various pharmacological activities. To elucidate new anti-allergic and anti-inflammatory constituents, the aerial parts of A. capillaries were investigated to afford a new compound, (6E,8E)-6-methylundeca-6,8-diene-2,5,10-trione (17) together with 19 known compounds (1 - 16, 18 - 20). The structures of these compounds were determined by extensive spectroscopic analyses including 1D, 2D NMR, HREIMS, and optical rotation [α]_D. The absolute configuration of compound 2 was determined to be S form for the first time. All isolates (1 - 20) were tested their inhibitory effects on interleukin 2 (IL-2) expression in T cells and NO production in lipopolysaccharide (LPS)-stimulated RAW246.7. Among them, compounds 10, 11, 19, and 20 reduced IL-2 expression in a dose-dependent manner. In addition, compound 10 also inhibited NO production with an IC₅₀ value of 37.3 ± 0.4 μM.

Isolation of oils from leaves of Juniperus phoenicea and Juniperus oxycedrus was obtained by steam distillation extraction method. The compositions of essential oils (EOs) were studied by means of GC-MS and GC-FID, using the internal standard method and relative response factors. Around ninety eight compounds were determined in total, representing 98.25 g/100 g of EO of J. phoenicea and 98.48 g/100 g of EO of J. oxycedrus, respectively. The volatile leaf oils were dominated by the terpenic hydrocarbon fractions (79.87 g/100 g) and (61.27 g/100 g) characterized by high contents of α-pinene (64.6 g/100 g) and (54.0 g/100 g) in J. phoenicea and J. oxycedrus, respectively, as the main component. Also, the enantiomeric distribution of α-pinene, sabinene, camphene, δ-3-carene, β-pinene, limonene, linalool, terpinen-4-ol, bornyl acetate, and borneol in both oils is presented for the first time.