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A total of 25 phenolic compounds were studied for their inhibitory effects against herpes simplex virus (HSV)-1, HSV-2, and human immunodeficiency virus (HIV)-1. These include five flavonoids (1–5) and two dimeric stilbenes (6,7) from Artocarpus gomezianus Wall. ex tréc., five phloroglucinol derivatives (8–12) from Mallotus pallidus (Airy Shaw) Airy Shaw, and 13 courmarins (13–25) from Triphasia trifolia (Burm.f.) P. Wilson. The data obtained in this study suggest the bis-hydroxyphenyl structure as a potential target for anti-HSV and HIV drugs development. [ABSTRACT FROM AUTHOR]

The phytochemical investigation of the whole plants of Coelogyne fuscescens Lindl. var. brunnea led to the discovery of three new phenolic glycosides, i.e., coelofusides A-C ( 1-3 ) and 12 known compounds ( 4-15 ). For the first time, we reported the nuclear magnetic resonance (NMR) data of 4- O -(6'- O -glucosyl-4″-hydroxybenzoyl)-4-hydroxybenzyl alcohol ( 4 ) in this study. The identification of the structures of newly discovered compounds was done through the analysis of their spectroscopic data [NMR, mass spectrometry, ultraviolet, Fourier transform infrared, optical rotation, and circular dichroism (CD)]. In comparison to anticancer drugs (i.e., etoposide and carboplatin), we evaluated anticancer potential of the isolated compounds on two different breast cancer cell lines, namely, T47D and MDA-MB-231. Human fibroblast HaCaT cells were used as the control cells. After a 48 h incubation, flavidin ( 8 ), coelonin ( 10 ), 3,4-dihydroxybenzaldehyde ( 11 ), and oxoflavidin ( 12 ) showed significant cytotoxic effects against breast cancer cells. Among them, oxoflavidin ( 12 ) exhibited the most potent cytotoxicity on MDA-MB-231 with an IC 50 value of 26.26 ± 4.33 μM. In the nuclear staining assay, oxoflavidin induced apoptosis after 48 h in both T47D and MDA-MB-231 cells in a dose-dependent manner. Furthermore, oxoflavidin upregulated the expression of apoptotic genes, such as p53, Bax, poly(ADP-ribose) polymerase, caspase-3, and caspase-9 genes while significantly decreasing antiapoptotic protein (Bcl-2) expression levels., Competing Interests: The authors declare no competing financial interest., (© 2024 The Authors. Published by American Chemical Society.)

Dendrobium plants are widely used in traditional Chinese medicine. Their secondary metabolites such as bibenzyls and phenanthrenes show various pharmacological benefits such as immunomodulation and inhibitory effects on cancer cell growth. However, our previous study also showed that some of these promising compounds (i.e., gigantol and cypripedin) also induced the expression of inflammatory cytokines including TNF in human monocytes, and thus raising concerns about the use of these compounds in clinical application. Furthermore, the effects of these compounds on other immune cell populations, apart from monocytes, remain to be investigated. In this study, we evaluated immunomodulatory effects of seven known bibenzyl compounds purified from Dendrobium species in human peripheral blood mononuclear cells (PBMCs) that were stimulated with lipopolysaccharide (LPS). Firstly, using flow cytometry, moscatilin (3) and crepidatin (4) showed the most promising dose-dependent immunomodulatory effects among all seven bibenzyls, determined by significant reduction of TNF expression in LPS-stimulated CD14+ monocytes. Only crepidatin at the concentration of 20 μM showed a significant cytotoxicity, i.e., an increased cell death in late apoptotic state. In addition, deep immune profiling using high-dimensional single-cell mass cytometry (CyTOF) revealed broad effects of Dendrobium compounds on diverse immune cell types. Our findings suggest that to precisely evaluate therapeutic as well as adverse effects of active natural compounds, a multi-parameter immune profiling targeting diverse immune cell population is required., Competing Interests: The authors have declared that no competing interests exist., (Copyright: © 2024 Kongkatitham et al. This is an open access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.)

Three new phenanthrene derivatives ( 1 , 2 , 4 ), one new fluorenone ( 3 ), and four known compounds ( 5 - 8 ) were isolated from the ethyl acetate extract of Dendrobium crumenatum Sw. stems using column chromatography. The chemical structures were elucidated by analysis of spectroscopic data. The absolute configuration of 4 was determined by electronic circular dichroism calculation. We also evaluated the immunomodulatory effects of compounds isolated from D. crumenatum in human peripheral blood mononuclear cells from healthy individuals and those from patients with multiple sclerosis in vitro. Dendrocrumenol B ( 2 ) and dendrocrumenol D ( 4 ) showed strong immunomodulatory effects on both CD3 + T cells and CD14 + monocytes. Compounds 2 and 4 could reduce IL-2 and TNF production in T cells and monocytes that were treated with phorbol-12-myristate-13-acetate and ionomycin (PMA/Iono). Deep immune profiling using high-dimensional single-cell mass cytometry could confirm immunomodulatory effects of 4 , quantified by the reduction of activated T cell population under PMA/Iono stimulation, in comparison to the stimulated T cells without treatment.

Central nervous system (CNS) diseases are a significant health burden globally, with the development of novel drugs lagging behind clinical needs. Orchidaceae plants have been traditionally used to treat CNS diseases, leading to the identification of therapeutic leads against CNS diseases from the Aerides falcata orchid plant in the present study. The study isolated and characterized ten compounds, including a previously undescribed biphenanthrene derivative, Aerifalcatin (1), for the first time from the A. falcata extract. The novel compound 1 and known compounds, such as 2,7-dihydroxy-3,4,6-trimethoxyphenanthrene (5), agrostonin (7), and syringaresinol (9), showed potential activity in CNS-associated disease models. Notably, compounds 1, 5, 7, and 9 demonstrated the ability to alleviate LPS-induced NO release in BV-2 microglial cells, with IC 50 values of 0.9, 2.5, 2.6, and 1.4 μM, respectively. These compounds also significantly inhibited the release of pro-inflammatory cytokines, IL-6 and TNF-α, reflecting their potential anti-neuroinflammatory effects. Additionally, compounds 1, 7, and 9 were found to reduce cell growth and migration of glioblastoma and neuroblastoma cells, indicating their potential use as anticancer agents in the CNS. In summary, the bioactive agents isolated from the A. falcata extract offer plausible therapeutic options for CNS diseases., Competing Interests: The authors declare no conflict of interest., (This journal is © The Royal Society of Chemistry.)

Oxidative stress is a significant factor in the development of age-related macular degeneration (AMD), which results from cell damage, dysfunction, and death in the retinal pigmented epithelium (RPE). The use of natural compounds with antioxidant properties to protect RPE cells from oxidative stress has been explored in Dendrobium , a genus of orchid plants belonging to the family Orchidaceae. Two new compounds and seven known compounds from the MeOH extract of the whole plant of Dendrobium virgineum were successfully isolated and structurally characterized. Out of all the compounds isolated, 2-methoxy-9,10-dihydrophenanthrene-4,5-diol ( 3 ) showed the highest protective effect against hydrogen peroxide (H 2 O 2 )-induced oxidative stress in human retinal pigment epithelial (ARPE-19) cells. Therefore, it was selected to evaluate its protective effect and mechanism on oxidative-stress-induced ARPE-19 cells. Cells were pre-treated with compound 3 at 25, 50, and 100 µg/mL for 24 h and then induced with 400 µM H 2 O 2 for 1 h. The results demonstrated that compound 3 significantly ( p < 0.05) increased cell viability by 10-35%, decreased ROS production by 10-30%, and reduced phosphorylation of p38, ERK1/2, and SAPK/JNK by 20-70% in a dose-dependent manner without toxicity. Furthermore, compound 3 significantly ( p < 0.05) modulated the expression of apoptosis pathway proteins (cytochrome c, Bax and Bcl-2) by 20-80%, and enhanced SOD, CAT, and GPX activities, and GSH levels in a dose-dependent manner. These results suggest that compound 3 protects ARPE-19 cells against oxidative stress through MAPKs and apoptosis pathways, including the antioxidant system. Thus, compound 3 could be considered as an antioxidant agent for preventing AMD development by protecting RPE cells from oxidative stress and maintaining the retina. These findings open up new possibilities for the use of natural compounds in the treatment of AMD and other oxidative-stress-related conditions., Competing Interests: The authors declare no conflict of interest.

The root of Boesenbergia rotunda , a culinary plant commonly known as fingerroot, has previously been reported to possess anti-obesity activity, with four flavonoids identified as active principles, including pinostrobin, panduratin A, cardamonin, and isopanduratin A. However, the molecular mechanisms underlying the antiadipogenic potential of isopanduratin A remain unknown. In this study, isopanduratin A at non-cytotoxic concentrations (1-10 μM) significantly suppressed lipid accumulation in murine (3T3-L1) and human (PCS-210-010) adipocytes in a dose-dependent manner. Downregulation of adipogenic effectors (FAS, PLIN1, LPL, and adiponectin) and adipogenic transcription factors (SREBP-1c, PPARγ, and C/EBPα) occurred in differentiated 3T3-L1 cells treated with varying concentrations of isopanduratin A. The compound deactivated the upstream regulatory signals of AKT/GSK3β and MAPKs (ERK, JNK, and p38) but stimulated the AMPK-ACC pathway. The inhibitory trend of isopanduratin A was also observed with the proliferation of 3T3-L1 cells. The compound also paused the passage of 3T3-L1 cells by inducing cell cycle arrest at the G0/G1 phase, supported by altered levels of cyclins D1 and D3 and CDK2. Impaired p-ERK/ERK signaling might be responsible for the delay in mitotic clonal expansion. These findings revealed that isopanduratin A is a strong adipogenic suppressor with multi-target mechanisms and contributes significantly to anti-obesogenic activity. These results suggest the potential of fingerroot as a functional food for weight control and obesity prevention.

The most prevalent lung cancer is non-small cell lung cancer (NSCLC). This lung cancer type often develops other organ-specific metastases that are critical burdens in the treatment process. Orchid species in the genus Vanda have shown their potential in folkloric medication of diverse diseases but not all its species have been investigated, and little is known about their anticancer activities against NSCLC. Here, we firstly profiled the specialized metabolites of Vanda&nbsp;bensonii and examined their capability to inhibit growth and metastasis of NSCLC using NCI-H460 cells as a study model. Four phytochemicals, including phloretic acid methyl ester ( 1 ), cymbinodin-A ( 2 ), ephemeranthoquinone B ( 3 ), and protocatechuic acid ( 4 ), were isolated from the whole plant methanolic extract of V. bensonii . The most distinguished cytotoxic effect on NCI-H460 cells was observed in the treatments with crude methanolic extract and compound 2 with the half maximal inhibitory concentrations of 40.39 μg mL -1 and 50.82 μM, respectively. At non-cytotoxic doses (10 μg mL -1 or 10 μM), only compound 1 could significantly limit NCI-H460 cell proliferation when treated for 48 h, while others excluding compound 4 showed significant reduction in cell proliferation after treating for 72 h. Compound 1 also significantly decreased the migration rate of NCI-H460 cells examined through a wound-healing assay. Additionally, the crude extract and compound 1 strongly affected survival and growth of NCI-H460 cells under anchorage-independent conditions. Our findings proved that natural products from V. bensonii could be promising candidates for the future pharmacotherapy of NSCLC.

Obesity is a critical factor for chronic metabolic syndromes. The culinary plant fingerroot ( Boesenbergia rotunda ) has been reported for its anti-obesity activity. The anti-adipogenic effects of pandurantin A, a main component of fingerroot cultivated in Indonesia, have been studied. Nevertheless, the suppressive effect and related mechanisms of pinostrobin, a major constituent of Thai fingerroot, on adipogenesis have never been thoroughly investigated. This study aimed to evaluate the potential of pinostrobin to inhibit adipocyte differentiation. Culturing pre-adipocytes from both mouse (3T3-L1) and human (PCS-210-010) with pinostrobin at non-toxic concentrations (5-20 µM) for 48 h obviously hindered their differentiation into mature adipocyte as evidenced by reduced cellular lipid droplets. The lower levels of lipid metabolism-mediating proteins, namely C/EBPα, PPARγ, and SREBP-1c, as well as cellular triglyceride content were demonstrated in pinostrobin-treated 3T3-L1 cells when compared to the untreated control group. Additionally, pinostrobin modulated the signals of MAPK (p38 and JNK) and Akt (Akt/GSK3β, Akt/AMPKα-ACC). These findings suggest the benefit of fingerroot as a source of phytopharmaceuticals for obesity prevention and management, with pinostrobin as the active principle.

Although many natural products have proven their potential to regulate obesity through the modulation of adipocyte biology, none of them has yet been approved for clinical use in obesity therapy. This work aims to isolate valuable secondary metabolites from an orchid species ( Dendrobium heterocarpum ) and evaluate their possible roles in the growth and differentiation of 3T3-L1 pre-adipocytes. Six compounds were isolated from the orchid's methanolic extracts and identified as amoenylin ( 1 ), methyl 3-(4-hydroxyphenyl) propionate ( 2 ), 3,4-dihydroxy-5,4'-dimethoxybibenzyl ( 3 ), dendrocandin B ( 4 ), dendrofalconerol A ( 5 ), and syringaresinol ( 6 ). Among these phytochemicals, compounds 2 , 3 , and 6 exhibited lower effects on the viability of 3T3-L1 cells, offering non-cytotoxic concentrations of ≲10 µM. Compared to others tested, compound 3 was responsible for the maximum reduction of lipid storage in 3T3-L1 adipocytes (IC 50 = 6.30 ± 0.10 µM). A set of protein expression studies unveiled that compound 3 at non-cytotoxic doses could suppress the expression of some key transcription factors in adipocyte differentiation (i.e., PPARγ and C/EBPα). Furthermore, this compound could deactivate some proteins involved in the MAPK pathways (i.e., JNK, ERK, and p38). Our findings prove that D . heterocarpum is a promising source to explore bioactive molecules capable of modulating adipocytic growth and development, which can potentially be assessed and innovated further as pharmaceutical products to defeat obesity.

From the whole plant of Dendrobium senile , a new phenanthrene namely 2,5,7-trihydroxy-4-methoxyphenanthrene ( 1 ) was isolated, together with seven known compounds including moscatin ( 2 ), 2,5-dihydroxy-4,9-dimethoxyphenanthrene ( 3 ), moscatilin ( 4 ), aloifol I ( 5 ), 4,4',8,8'-tetramethoxy[1,1'-biphenanthrene]-2,2',7,7'-tetrol ( 6 ), 2,2',7,7'-tetrahydroxy-4,4'-dimethoxy-1,1'-biphenanthrene ( 7 ) and bleformin G ( 8 ). The structure of the new compound was elucidated by analysis of its spectroscopic data. Moscatin ( 2 ) and 2,5-dihydroxy-4,9-dimethoxyphenanthrene ( 3 ) showed appreciable pancreatic lipase inhibitory effects when compared with the positive control orlistat.

From the aerial parts of Cymbidium ensifolium, three new dihydrophenanthrene derivatives, namely, cymensifins A, B, and C (1−3) were isolated, together with two known compounds, cypripedin (4) and gigantol (5). Their structures were elucidated by analysis of their spectroscopic data. The anticancer potential against various types of human cancer cells, including lung, breast, and colon cancers as well as toxicity to normal dermal papilla cells were assessed via cell viability and nuclear staining assays. Despite lower cytotoxicity in lung cancer H460 cells, the higher % apoptosis and lower % cell viability were presented in breast cancer MCF7 and colon cancer CaCo2 cells treated with 50 µM cymensifin A (1) for 24 h compared with the treatment of 50 µM cisplatin, an available chemotherapeutic drug. Intriguingly, the half-maximum inhibitory concentration (IC50) of cymensifin A in dermal papilla cells at >200 µM suggested its selective anticancer activity. The obtained information supports the further development of a dihydrophenanthrene derivative from C. ensifolium as an effective chemotherapy with a high safety profile for the treatment of various cancers.

Chemical investigation of Dendrobium delacourii revealed 11 phenolic compounds, and the structures of these compounds were determined by analysis of their NMR and HR-ESI-MS data. All compounds were investigated for their α -glucosidase inhibitory activity and anti-adipogenic properties. Phoyunnanin E ( 10 ) and phoyunnanin C ( 11 ) showed the most potent α -glucosidase inhibition by comparing with acarbose, which was used as a positive control. Kinetic study revealed the non-competitive inhibitors against the enzyme. For anti-adipogenic activity, densifloral B ( 3 ) showed the strongest inhibition when compared with oxyresveratrol (positive control). In addition, densifloral B might be responsible for the inhibition of adipocyte differentiation via downregulating the expression of peroxisome proliferator-activated receptor gamma (PPARγ) and CCAAT enhancer-binding protein alpha (C/EBP α ), which are major transcription factors in adipogenesis.

Oxyresveratrol has recently attracted much research attention due to its simple chemical structure and diverse therapeutic potentials. Previous reviews describe the chemistry and biological activities of this phytoalexin, but additional coverage and greater accessibility are still needed. The current review provides a more comprehensive summary, covering research from 1955 to the present year. Oxyresveratrol occurs in both gymnosperms and angiosperms. However, it has never been reported in plants in the subclass Sympetalae, and this point might be of both chemotaxonomic and biosynthetic importance. Oxyresveratrol can be easily obtained from plant materials by conventional methods, and several systems for both qualitative and quantitative analysis of oxyresveratrol contents in plant materials and plant products are available. Oxyresveratrol possesses diverse biological and pharmacological activities such as the inhibition of tyrosinase and melanogenesis, antioxidant and anti-inflammatory activities, and protective effects against neurological disorders and digestive ailments. However, the unfavorable pharmacokinetic properties of oxyresveratrol, including low water solubility and poor oral availability and stability, have posed challenges to its development as a useful therapeutic agent. Recently, several delivery systems have emerged, with promising outcomes that may improve chances for the clinical study of oxyresveratrol.

Three novel actinomycete strains, designated as DR6-1 T , DR6-2 and DR6-4, isolated from the roots of Dendrobium heterocarpum Lindl in Thailand were studied using a polyphasic taxonomic approach. The strains grew at 20-37 °C, at pH 5-10 and with 5 % (w/v) NaCl. They contained meso -diaminopimelic acid in the cell-wall peptidoglycan and MK-9(H 4 ) was a major menaquinone. Arabinose and galactose were the major sugars in the cell wall. The predominant cellular fatty acids were iso-C 16 : 0 and iso-C 15 : 0 . The detected polar lipids were diphosphatidylglycerol, hydroxyphosphatidylethanolamine, phosphatidylethanolamine, phosphatidylinositol and phosphatidylglycerol. Strains DR6-1 T , DR6-2 and DR6-4 shared 99.9-100 % 16S rRNA gene sequence similarity and were closely related to Amycolatopsis echigonensis JCM 21831 T (98.7-98.8%). The approximate genome size of strain DR6-1 T was 9.6 Mb with a G+C content of 69.6 mol%. The ANIb and dDDH values between genomic sequences of strain DR6-1 T and Amycolatopsis echigonensis JCM21831 T , Amycolatopsis rubida JCM 10871 T and Amycolatopsis nivea KCTC 39515 T were 90.55, 92.25, 92.60%, and 47.20, 52.10 and 52.50%, respectively. Based on the phenotypic, chemotaxonomic and genotypic characteristics, it has been concluded that strains DR6-1 T , DR6-2 and DR6-4 represent a novel species of the genus Amycolatopsis for which the name Amycolatopsis dendrobii sp. nov. is proposed. The type strain is DR6-1 T (=JCM 33742 T =KCTC 49546 T =TISTR 2840 T ).

Large amounts of Morus alba L. (MA) roots are needed as the source of active stilbenes in the industrial production of traditional medicines and cosmeceuticals. A recent investigation demonstrated resveratrol and its derivatives to be promising anti-COVID-19 agents. However, conventional cultivation of MA does not meet the demand for its stilbenes, and root quality usually varies between crops. This study established the in vitro non-GMO root culture of MA and optimized the root density, precursor feeding, and elicitors for stilbene productivity. A root culture with optimal inoculum density (3 g/flask of 30 mL medium) accumulated mulberroside A, oxyresveratrol, and resveratrol at 18.7 ± 1.00 mg/g, 136 ± 5.05 µg/g, and 41.6 ± 5.84 µg/g dry weight (DW), respectively. The feeding of L-tyrosine shortened the time required to reach the stilbene productive stage. Root cultures co-treated with 200 µM methyl jasmonate and 2 mg/mL yeast extract accumulated the highest contents of mulberroside A (30.3 ± 2.68 mg/g DW), oxyresveratrol (68.6 ± 3.53 µg/g DW), and resveratrol (10.2 ± 0.53 µg/g DW). In summary, root culture is a promising and sustainable source of stilbenes for the development of health products and agents for further investigation as potential anti-COVID-19 agents.

A phytochemical investigation on the whole plants of Aerides multiflora revealed the presence of three new biphenanthrene derivatives named aerimultins A-C ( 1 - 3 ) and a new natural phenylpropanoid ester dihydrosinapyl dihydroferulate ( 4 ), together with six known compounds ( 5 - 10 ). The structures of the new compounds were elucidated by analysis of their spectroscopic data. All of the isolates were evaluated for their α -glucosidase inhibitory activity. Aerimultin C ( 3 ) showed the most potent activity. The other compounds, except for compound 4 , also exhibited stronger activity than the positive control acarbose. Compound 3 showed non-competitive inhibition of the enzyme as determined from a Lineweaver-Burk plot. This study is the first phytochemical and biological investigation of A. multiflora .

Five compounds including a new bisbibenzyl named dendropachol ( 1 ) and four known compounds ( 2-5 ) comprising 4,5-dihydroxy-2,3-dimethoxy-9,10-dihydrophenanthrene ( 2 ), gigantol ( 3 ), moscatilin ( 4 ) and 4,5,4'-trihydroxy-3,3'-dimethoxybibenzyl ( 5 ) were isolated from a methanolic extract of Dendrobium pachyglossum (Orchidaceae). The chemical structures of the isolated compounds were characterized by spectroscopic methods. Dendropachol ( 1 ) was investigated for its protective effects on hydrogen peroxide (H 2 O 2 )-induced oxidative stress in HaCaT keratinocytes. Compound 1 showed strong free radical scavenging compared to the positive control. For the cytoprotective effect, compound 1 increased the activities of GPx and CAT and the level of GSH but reduced intracellular reactive oxygen species (ROS) generation and accumulation. In addition, compound 1 significantly diminished the expression of p53, Bax, and cytochrome C proteins, decreased the activities of caspase-3 and caspase-9, and increased Bcl-2 protein. The results suggested that compound 1 exhibited antioxidant activities and protective effects in keratinocytes against oxidative stress induced by H 2 O 2 .

Four new phenanthrene derivatives, gastrobellinols A-D ( 1-4 ), were isolated from the methanolic extract of Gastrochilus bellinus (Rchb.f.) Kuntze, along with eleven known phenolic compounds including agrostophyllin ( 5 ), agrostophyllidin ( 6 ), coniferyl aldehyde ( 7 ), 4-hydroxybenzaldehyde ( 8 ), agrostophyllone ( 9 ), gigantol ( 10 ), 4-(methoxylmethyl)phenol ( 11 ), syringaldehyde ( 12 ), 1-(4'-hydroxybenzyl)-imbricartin ( 13 ), 6-methoxycoelonin ( 14 ), and imbricatin ( 15 ). Their structures were determined by spectroscopic methods. Each isolate was evaluated for α-glucosidase inhibitory activity. Compounds 1 , 2 , 3 , 7 , 9 , 13 , and 15 showed higher activity than the drug acarbose. Gastrobellinol C ( 3 ) exhibited the strongest α -glucosidase inhibition with an IC 50 value of 45.92 μM. A kinetic study of 3 showed competitive inhibition on the α -glucosidase enzyme. This is the first report on the phytochemical constituents and α -glucosidase inhibitory activity of G. bellinus.

Two new compounds, dihydrodengibsinin ( 1 ) and dendrogibsol ( 2 ), were isolated from the whole plant of Dendrobium gibsonii , together with seven known compounds ( 3 - 9 ). The structures of the new compounds were elucidated by their spectroscopic data. All these isolates were evaluated for their α-glucosidase inhibitory activities. Dendrogibsol ( 2 ) and lusianthridin ( 7 ) showed strong α-glucosidase inhibitory activity when compared with acarbose. An enzyme kinetic study revealed that dendrogibsol ( 2 ) is a noncompetitive inhibitor of α-glucosidase.

Dendrobium bibenzyls and phenanthrenes such as chrysotoxine, cypripedin, gigantol and moscatilin have been reported to show promising inhibitory effects on lung cancer growth and metastasis in ex vivo human cell line models, suggesting their potential for clinical application in patients with lung cancer. However, it remains to be determined whether these therapeutic effects can be also seen in primary human cells and/or in vivo. In this study, we comparatively investigated the immune modulatory effects of bibenzyls and phenanthrenes, including a novel Dendrobium bibenzyl derivative, in primary human monocytes. All compounds were isolated and purified from a Thai orchid Dendrobium lindleyi Steud, a new source of therapeutic compounds with promising potential of tissue culture production. We detected increased frequencies of TNF- and IL-6-expressing monocytes after treatment with gigantol and cypripedin, whereas chrysotoxine and moscatilin did not alter the expression of these cytokines in monocytes. Interestingly, the new 4,5-dihydroxy-3,3',4'-trimethoxybibenzyl derivative showed dose-dependent immune modulatory effects in lipopolysaccharide (LPS)-treated CD14lo and CD14hi monocytes. Together, our findings show immune modulatory effects of the new bibenzyl derivative from Dendrobium lindleyi on different monocyte sub-populations. However, therapeutic consequences of these different monocyte populations on human diseases including cancer remain to be investigated., Competing Interests: The authors declare no competing financial interests.

The phytochemical investigation of Huberantha jenkinsii resulted in the isolation of two new and five known compounds. The new compounds were characterized as undescribed 8-oxoprotoberberine alkaloids and named huberanthines A and B, whereas the known compounds were identified as allantoin, oxylopinine, N - trans -feruloyl tyramine, N-trans-p- coumaroyl tyramine, and mangiferin. The structure determination was accomplished by spectroscopic methods. To evaluate therapeutic potential in diabetes and Parkinson's disease, the isolates were subjected to assays for their α-glucosidase inhibitory activity, cellular glucose uptake stimulatory activity, and protective activity against neurotoxicity induced by 6-hydroxydopamine (6-OHDA). The results suggested that mangiferin was the most promising lead compound, demonstrating significant activity in all the test systems.

Phytochemical investigation of the whole plant of Dendrobium scabrilingue resulted in the isolation of two new compounds namely dendroscabrols A ( 1 ) and B ( 2 ), along with eight known compounds ( 3 - 10 ). The structures of these compounds were determined by NMR and HR-ESI-MS experiments. All of the isolates were evaluated for their α-glucosidase inhibitory effect. Dendroscabrol B ( 2 ) and RF-3192C ( 10 ) showed the most potent α-glucosidase inhibitory activity. Dendroscabrol A ( 1 ), gigantol ( 5 ), coelonin ( 7 ) and lusianthridin ( 9 ) also exhibited strong activity as compared with the positive control acarbose.

Mulberroside A, oxyresveratrol and resveratrol, commonly found in Morus alba L., are potent anti-aging phytostilbenes. In this study, the effect of the addition of 2-hydroxypropyl-β-cyclodextrin on the levels of phytostilbenes in M. alba callus cultures was investigated. Commercial cyclodextrin was used in the hydrolytic and culture processes of the M. alba callus cultures. The hydrolytic study indicated that 2-hydroxypropyl-β-cyclodextrin acted as a retardant for stilbenoid hydrolysis. It reduced mulberroside A deglycosylation and stabilised oxyresveratrol. The elicitation result showed that extracellular oxyresveratrol was increased by adding 2-hydroxypropyl-β-cyclodextrin to the culture media of both free and immobilised M. alba callus (>730-fold and >169-fold, respectively) compared with those of the control. However, the intracellular mulberroside A levels in the treatment groups did not increase compared with those of the control. The results show that the addition of 2-hydroxypropyl-β-cyclodextrin significantly changed the patterns and levels of the stilbenoids in M. alba callus cultures.

Background: Oxyresveratrol is a major bioactive component derived from the heartwood of Artocarpus lacucha. This compound exerts several biological activities, including neuroprotective effects in vitro and in vivo. However, there is limited pharmacokinetic information on this compound, especially its distribution in neuronal tissue and its route of excretion. The aim of this study was to investigate the pharmacokinetic profiles of oxyresveratrol alone and in combination with piperine as a bioenhancer in rats., Methods: Male Wistar rats were administered with oxyresveratrol 10 mg/kg, oxyresveratrol 10 mg/kg plus piperine 1 mg/kg via intravenous or oxyresveratrol 100 mg/kg, oxyresveratrol 100 mg/kg plus piperine 10 mg/kg via oral gavage. Plasma, internal organs, urine, and feces were collected. Determination of the oxyresveratrol concentration in biological samples was performed by liquid chromatography tandem mass spectrometry., Results: The combination with piperine had shown a significantly higher maximum concentration in plasma approximately 1500 μg/L within 1-2 h after oral dosing, and could increase oral bioavailability of oxyresveratrol approximately 2-fold. Oxyresveratrol could widely distributed most of the internal organs with a tissue to plasma ratio of 10-100 fold within 5 min after dosing. Urinary excretion of oxyresveratrol glucuronide was the major route of excretion after administration of oxyresveratrol alone and in combination with piperine., Conclusion: The addition of piperine could enhance some of the pharmacokinetic properties of oxyresveratrol via both intravenous and oral administration. This pharmacokinetic information will be useful for appropriate strategies to develop oxyresveratrol as a phytopharmaceutical product.

Two new 2-arylbenzofurans, namely 13- O -methyllakoochin B ( 1 ) and artogomezianin ( 2 ), were isolated from the root bark of Artocarpus gomezianus , along with six known compounds ( 3 - 8 ). The structures of new compounds were determined by spectroscopic and chemical methods. All of the isolates were evaluated for their α-glucosidase inhibitory activity. Artogomezianin ( 2 ) and lakoochin A ( 3 ) exhibited strong α-glucosidase inhibitory activity with IC 50 values of 18.25 and 26.19 µM, respectively, as compared with the positive control acarbose.

A new phenanthrene dimer, namely dendropalpebrone (1), was isolated from the whole plant of Dendrobium palpebre, along with nine known compounds (2-10). All of the isolates were evaluated for their hydroxyl radical scavenging effects using a deoxyribose assay. Dendroflorin (10) showed an appreciable activity, and therefore was selected for further studied in RAW264.7 cells. Compound 10 significantly decreased ROS in H 2 O 2 -stimulated RAW264.7 cells in a dose-dependent manner, and improved activity of SOD, GPx, and CAT enzymes.

Two new dihydrophenanthrenes, dendroinfundin A (1) and dendroinfundin B (2) were isolated from the whole plant of Dendrobium infundibulum, together with 7 known compounds (3-9). The structures of the new compounds (1 and 2) were established on the basis of their spectroscopic data. All of the isolates were evaluated for their α-glucosidase and pancreatic lipase inhibitory activities. Batatasin III (5) and dendrosinen B (9) showed strong α-glucosidase inhibitory activity. Dendrosinen B (9) also exhibited appreciable pancreatic lipase inhibitory effect.