PMID: 

J Nat Med. 2012 Jan ;66(1):55-61. Epub 2011 Jun 14. PMID: 21671149

Abstract Title: 

Patchouli alcohol: in vitro direct anti-influenza virus sesquiterpene in Pogostemon cablin Benth.

Abstract: 

During the screening of anti-influenza virus substances from traditional herbal medicines, the methanol extract from the leaves of Pogostemon cablin Benth. showed potent in vitro antiviral activity (99.8% inhibition at a concentration of 10μg/mL) against influenza virus A/PR/8/34 (H1N1). The anti-influenza virus principle was isolated from the hexane-soluble fraction, through solvent fractionation, repeated silica gel column chromatography, and reversed-phase HPLC. The major active principle was a volatile substance that was identified as a sesquiterpene, patchouli alcohol (1), on the basis of its spectral analyses. When anti-influenza virus activity against A/PR/8/34 was evaluated by the plaque forming assay, patchouli alcohol reduced the number of plaques by 75% at 2 μg/mL and 89% at 10 μg/mL. Patchouli alcohol showed dose-dependent anti-influenza virus activity, and its IC(50) value was estimated to be 2.635 μM. Although 11 different sesquiterpenes were tested for antiviral activity against influenza virus A/PR/8/34, no or negligible activity was observed except for patchouli alcohol. Patchouli alcohol did not showanti-influenza virus activity against A/Guizhou/54/89 (H3N2), but showed weak activity against B/Ibaraki/2/85 (IC(50) = 40.82 μM). Patchouli alcohol did not show inhibitory activity against influenza virus neuraminidase.

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PMID: 

Molecules. 2011 Aug 3 ;16(8):6489-501. Epub 2011 Aug 3. PMID: 21814161

Abstract Title: 

Inhibitory effect and possible mechanism of action of patchouli alcohol against influenza A (H2N2) virus.

Abstract: 

In the present study, the anti-influenza A (H2N2) virus activity of patchouli alcohol was studied in vitro, in vivo and in silico. The CC₅₀ of patchouli alcohol was above 20 µM. Patchouli alcohol could inhibit influenza virus with an IC₅₀ of 4.03 ± 0.23 µM. MTT assay showed that the inhibition by patchouli alcohol appears strongly after penetration of the virus into the cell. In the influenza mouse model, patchouli alcoholshowed obvious protection against the viral infection at a dose of 5 mg/kg/day. Flexible docking and molecular dynamic simulations indicated that patchouli alcohol was bound to the neuraminidase protein of influenza virus, with an interaction energy of -40.38 kcal mol⁻¹. The invariant key active-site residues Asp151, Arg152, Glu119, Glu276 and Tyr406 played important roles during the binding process. Based on spatial and energetic criteria, patchouli alcohol interfered with the NA functions. Results presented here suggest that patchouli alcohol possesses anti-influenza A (H2N2) virus properties, and therefore is a potential source of anti-influenza agents for the pharmaceutical industry.

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PMID: 

Fitoterapia. 2011 Dec ;82(8):1295-301. Epub 2011 Sep 19. PMID: 21958968

Abstract Title: 

Anti-inflammatory activity of patchouli alcohol isolated from Pogostemonis Herba in animal models.

Abstract: 

Pogostemonis Herba has long been used in traditional Chinese medicine for the treatment of inflammatory disorders. Patchouli alcohol (PA), a tricyclic sesquiterpene isolated from Pogostemonis Herba, is known to possess a variety of pharmacological activities. The present study aimed to investigate the in vivo anti-inflammatory effect of PA using two common inflammatory animal models i.e., xylene-induced ear edema in mice and carrageenan-induced paw edema in rats. The degree of edema in both inflammatory animals, as well as the protein and mRNA expression of some inflammatory mediators including tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), prostaglandin E₂ (PGE₂) and nitric oxide (NO) in the hind paw of carrageenan-treated rats were measured. Results showed that PA (10-40 mg/kg) significantly inhibited the ear edema induced by xylene in mice and the paw edema induced by carrageenan in rats. In addition, treatment with PA (10-40 mg/kg) also dose-dependently decreased the production of TNF-α, IL-1β, PGE₂ and NO in the hind paw of carrageenan-treated rats. Furthermore, PA treatment also suppressed the mRNA expression of TNF-α, IL-1β, inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in the hind paw of carrageenan-treated rats. These results suggest that PA possesses potent anti-inflammatory activity, which may be mediated, at least in part, by down-regulating the mRNA expression of a panel of inflammatory mediators including TNF-α, IL-1β, iNOS and COX-2.

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PMID: 

ScientificWorldJournal. 2013 ;2013:434151. Epub 2013 Dec 9. PMID: 24385881

Abstract Title: 

Anti-inflammatory property of the ethanol extract of the root and rhizome of Pogostemon cablin (Blanco) Benth.

Abstract: 

The aim of this study was to investigate the anti-inflammatory property of the ethanol extract of the root and rhizome of Pogostemon cablin (ERP). The anti-inflammatory effect was evaluated using four animal models including xylene-induced mouse ear edema, acetic acid-induced mouse vascular permeability, carrageenan-induced mouse pleurisy, and carrageenan-induced mouse hind paw edema. Results indicated that oral administration of ERP (120, 240, and 480 mg/kg) significantly attenuated xylene-induced ear edema, decreased acetic acid-induced capillary permeability, inhibited carrageenan-induced neutrophils recruitment, and reduced carrageenan-induced paw edema, in a dose-dependent manner. Histopathologically, ERP (480 mg/kg) abated inflammatoryresponse of the edema paw. Preliminary mechanism studies demonstrated that ERP decreased the level of MPO and MDA, increased the activities of anti-oxidant enzymes (SOD, GPx, and GRd), attenuated the productions of TNF-α, IL-1β, IL-6, PGE₂ and NO, and suppressed the activities of COX-2 and iNOS.This work demonstrates that ERP has considerable anti-inflammatory potential, which provided experimental evidences for the traditional application of the root and rhizome of Pogostemon cablin in inflammatory diseases.

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PMID: 

Int Immunopharmacol. 2013 Jun ;16(2):184-90. Epub 2013 Apr 17. PMID: 23602914

Abstract Title: 

Patchouli alcohol, an essential oil of Pogostemon cablin, exhibits anti-tumorigenic activity in human colorectal cancer cells.

Abstract: 

Patchouli alcohol (PA) is one of the important compounds isolated from the essential oil of Pogostemon cablin (patchouli). PA has neuroprotective, anti-influenza and anti-inflammatory activities. However, anti-cancer activity of PA has not been studied so far. We performed in vitro study to investigate whether PA affects proliferation and apoptosis of human colorectal cancer cells, and to define potential molecular mechanisms. PA suppressed cell growth and induced apoptosis in a dose-dependent manner in human colorectal cancer cells (HCT116, SW480). In addition, PA decreased cell growth in MCF7, BxPC3, PC3, and HUVEC cells. Exposure of PA to HCT116 and SW480 cells activated p21 expression and suppressed the expressions of cyclin D1 and cyclin-dependent kinase 4 (CDK4) in a dose-dependent manner. In addition, PA attenuated the expressions of HDAC2 (histone deacetylase 2) and c-myc, and HDAC enzyme activity. We also observed that PA induced the transcriptional activity of NF-κB through an increase of nuclear translocation of p65. These findings suggest that PA exerts an anti-cancer activity by decreasing cell growth and increasing apoptosis in human colorectal cancer cells. The proposed mechanisms include the inhibition of HDAC2 expression and HDAC enzyme activity, andsubsequent downregulation of c-myc and activation of NF-κB pathway.

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PMID: 

Curr Microbiol. 2013 Oct ;67(4):431-6. Epub 2013 May 17. PMID: 23680974

Abstract Title: 

Immunologic mechanism of Patchouli alcohol anti-H1N1 influenza virus may through regulation of the RLH signal pathway in vitro.

Abstract: 

Patchouli alcohol (PA) is a kind of methanol extracted from traditional Chinese medicine Pogostemonis Herba. Our research aimed to observe the anti-influenza virus role of PA in vitro. 16HBE (human respiratory epithelial cell) was infected by H1N1 (A/FM1/1/47) to set the cell model. Then the 16HBE was co-cultivated with three kinds of immune cells: dendritic cells, macrophages, and monocytes, PA (the concentration is 10 μg/mL) was added as a treatment intervention for 24 h. The immune cells and the supernate were collected for RT-PCR and ELISA detection related to RLH (RIG-1-like helicases) pathway. Results showed that the IL-4 and IFN-γ in supernate were increased after H1N1 infection, and the PA treatment suppressed the expression of cytokines and the mRNA of RLH pathway. PA anti-influenza virus may through regulate the RLH singal pathway.

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PMID: 

Arch Pharm Res. 2014 Feb ;37(2):253-62. Epub 2013 Oct 30. PMID: 24166708

Abstract Title: 

Protective effects of Pogostemon cablin Bentham water extract on inflammatory cytokine expression in TNBS-induced colitis in rats.

Abstract: 

In inflammatory bowel disease (IBD), colon epithelial cells express a variety of inflammatory mediators, including chemokines, which perpetuate inflammatory response. In the current study, we report that water extract of Pogostemon cablin Bentham aerial parts (PCW), which has traditionally been used for treatment of the common cold and infectious disease, suppressed colon inflammation. Treatment with PCW resulted in effective inhibition of tumor necrosis factor (TNF)-α-induced adhesion of monocytes to HT-29 human colonic epithelial cells. In a trinitrobenzene sulfonic acid (TNBS)-induced rat model of IBD, PCW suppressed clinical signs of colitis, including weight loss, colon tissue myeloperoxidase activity, a marker for inflammatory cell infiltration, and cyclooxygenase-2 expression in a dose-dependent manner. In addition, PCW suppressed TNBS-induced mRNA expression of IL-8, MCP-1, and IL-6 in rat colon. The nuclear level of NF-κB in TNBS-treated rat colon and NF-κB luciferase reporter gene activity in TNF-α-treated HT-29 cells were significantly inhibited by PCW. Taken together, the results of this study suggest that PCW suppressed colon inflammation via suppression of NF-κB-dependent expression of pro-inflammatory cytokines.

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PMID: 

Eur J Pharm Sci. 2014 Oct 15 ;63:113-23. Epub 2014 Jul 14. PMID: 25033712

Abstract Title: 

Effects of topical application of patchouli alcohol on the UV-induced skin photoaging in mice.

Abstract: 

Ultraviolet (UV) irradiation, known to generate reactive oxygen species (ROS) excessively and elicit inflammatory response, is a potent inducer for skin photoaging. Overproduction of ROS in conjunction with the resulting inflammation stimulate the over-expression of matrix metalloproteinases (MMPs), which in turn causes degradation of extracellular matrix, leading finally to coarse wrinkling, dryness, and laxity of the skin. In this study, patchouli alcohol (PA, C15H26O), an active chemical ingredient reputed for free radical scavenging and anti-inflammatory properties, was investigated for its anti-photoaging action using a mouse model whose dorsal skin was depilated. The dorsal skin areas of six-week-old mice were smeared with PA solution or vehicle, followed by UV irradiation for nine consecutive weeks. Protective effects of PA were evaluated macroscopically and histologically, as well as by assaying the antioxidant enzymes (SOD, GSH-Px) activities, the contents of inflammatory factors (IL-10, IL-6, TNF-α), and the levels of MMP-1 and MMP-3. Our findings amply demonstrated that PA significantly accelerated the recovery of the UV-induced skin lesions, evidently through anti-oxidant and anti-inflammatory action, as well as down-regulation of the MMP-1 and MMP-3 expression.

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PMID: 

Inflammation. 2014 Oct ;37(5):1757-62. PMID: 24839088

Abstract Title: 

Patchouli alcohol dampens lipopolysaccharide induced mastitis in mice.

Abstract: 

Patchouli alcohol (PA), a tricyclic sesquiterpene isolated from Pogostemonis Herba, has been known to exhibit antioxidant, anti-inflammatory, and other important therapeutic activities. The aim of this study was to investigate the effects of PA on LPS-induced mastitis in vivo and the possible mechanism. The mouse model of mastitis was induced by injection of LPS through the duct of mammary gland. Mice were pretreated with dexamethasone or PA 1 h before and 12 h after induction of LPS. The myeloperoxidase activity and inflammatory cytokines production in mammary tissues were determined. The effects of PA on NF-κB signal pathways were analyzed by Western blotting. The results showed that PA inhibited the LPS-induced TNF-α, IL-6, and IL-1β production in a dose manner. It was also observed that PA attenuated mammary histopathologic changes. Furthermore, Western blot analysis showed that PA could inhibit the phosphorylation of NF-κB and IκB induced by LPS. These results indicate that PA inhibits NF-κB signaling pathways to attenuate inflammatory injury induced by LPS. PA may be a potent therapeutic reagent for the prevention of mastitis.

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PMID: 

Pharmacogn Mag. 2015 Apr-Jun;11(42):311-9. PMID: 25829770

Abstract Title: 

Effects of Pogostemon cablin Blanco extract on hypoxia induced rabbit cardiomyocyte injury.

Abstract: 

BACKGROUND: Pogostemonis Herba, the dried aerial part of Pogostemon cablin Blanco, is a well-known materia medica in Asia that is widely used for syndrome of gastrointestinal dysfunctions.OBJECTIVE: This study was undertaken to examine whether Pogostemon cablin extract (PCe) might have any beneficial effect on hypoxia induced rabbit cardiomyocyte injury.MATERIALS AND METHODS: Isolated cardiomyocytes were divided into three groups and the changes of cell viability in cardiomyocytes of hypoxic and hypoxia/reoxygenation group were determined. The effect of PCe on reactive oxygen species (ROS) generation, intracellular formation of ROS was also measured by monitoring the 2',7'-dichlorofluorescein fluorescence.RESULTS: PCe effectively protected the cells against both the hypoxia and reoxygenation induced injury, and the protective effect of PCe is not mediated by interaction with adenosine triphosphate-sensitive K(+) channels. In the presence of PCe, production of ROS under chemical hypoxia was remarkably reduced which suggests that PCe might exert its effect as a ROS scavenger.CONCLUSION: The present study provides clear evidence for the beneficial effect of PCe on cardiomyocyte injury during hypoxia or reoxygenation following prolonged hypoxia.

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