Patchouli alcohol

Int Immunopharmacol. 2013 Jun;16(2):184-90.

Patchouli alcohol, an essential oil of Pogostemon cablin, exhibits anti-tumorigenic activity in human colorectal cancer cells.[Pubmed: 23602914]

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.
METHODS AND RESULTS:
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.
CONCLUSIONS:
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, and subsequent downregulation of c-myc and activation of NF-κB pathway.

J Agric Food Chem. 2003 Jul 30;51(16):4585-8.

Toxicity and repellency of patchouli oil and patchouli alcohol against Formosan subterranean termites Coptotermes formosanus Shiraki (Isoptera: Rhinotermitidae).[Pubmed: 14705881 ]

Patchouli oil obtained from Pogostemon cablin (Blanco) Benth and its main constituent, Patchouli alcohol, were tested for their repellency and toxicity against Formosan subterranean termites (Coptotermes formosanus Shiraki). Both were found to be toxic and repellent. Unusual tissue destruction was noted inside the exoskeleton of the termite after Patchouli alcohol was topically applied to the dorsum.

Chem Biol Interact. 2014 Oct 5;222:27-36.

Gastroprotective effect and mechanism of patchouli alcohol against ethanol, indomethacin and stress-induced ulcer in rats.[Pubmed: 25168850 ]

Pogostemonis Herba is an important Chinese medicine widely used in the treatment of gastrointestinal dysfunction. Patchouli alcohol (PA), a tricyclic sesquiterpene, is the major active constituent of Pogostemonis Herba. This study aimed to investigate the possible anti-ulcerogenic potential of PA and the underlying mechanism against ethanol, indomethacin and water immersion restraint-induced gastric ulcers in rats.
METHODS AND RESULTS:
Gross and histological gastric lesions, biochemical and immunological parameters were taken into consideration. The gastric mucus content and the antisecretory activity were analyzed through pylorus ligature model in rats. Results indicated that oral administration with PA significantly reduced the ulcer areas induced by ethanol, indomethacin and water immersion restraint. PA pretreatment significantly promoted gastric prostaglandin E2 (PGE2) and non-protein sulfhydryl group (NP-SH) levels, upregulated the cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) mRNA expression, and considerably boosted the gastric blood flow (GBF) and gastric mucus production in comparison with vehicle. In addition, PA modulated the levels of interleukin-6 (IL-6), interleukin-10 (IL-10) and tumor necrosis factor-α (TNF-α). The levels of glutathione (GSH), catalase (CAT) and malonaldehyde (MDA) were also restored by PA. However, the gastric secretion parameters (pH, volume of gastric juice and pepsin) did not show any significant alteration.
CONCLUSIONS:
These findings suggest that PA exhibited significant gastroprotective effects against gastric ulceration. The underlying mechanisms might involve the stimulation of COX-mediated PGE2, improvement of antioxidant and anti-inflammatory status, preservation of GBF and NP-SH, as well as boost of gastric mucus production.

Trop. J.Pharm. Res., 2013, 12(4):559-65.

Immunomodulatory Potential of Patchouli Alcohol Isolated from Pogostemon cablin (Blanco) Benth (Lamiaceae) in Mice[Reference: WebLink]

To isolate and purify Patchouli alcohol (PA), a tricyclic sesquiterpene constituent of Pogostemon cablin, and investigate its immunomodulatory potential in Kunming mice.
METHODS AND RESULTS:
PA was prepared from an ethanol aqueous extract of P. cablin by silica gel column chromatography, and further purified by crystallization using n-hexane. Purity was assessed by analytical gas chromatography (GC) and confirmation of chemical structure performed by Fourier transform infrared (FTIR), nuclear magnetic resonance (NMR) spectroscopy and mass spectrometry (MS). The effect of PA from Pogostemon cablin on immunological function was studied by macrophage phagocytosis, immune organ index, serum immunoglobulin level and delayed type hypersensitivity (DTH) in mice that were administered orally doses of 20, 40 and 80 mg/kg. The purity of PA was 99.3%. The oral administration of PA (40, or 80 mg/kg body weight) significantly increased the phagocytic index (p < 0.05), compared with prednisone acetate (PR) group. Administration of PA (80 mg/kg) boosted the production of circulating serum IgM (0.081 ± 0.010) and IgG (1.296 ± 0.120), while IgM and IgG in PR group was 0.069 ± 0.011 (p < 0.01) and 1.180 ± 0.070 (p < 0.01) respectively. However, PA (20 mg/kg) treatment elicited significant decrease in DTH induced by 2, 4-dinitro-chlorobenzene (DNCB) in mice (1.03 ± 0.40, p < 0.05), in comparison to DNCB-induced group (1.67 ± 0.84 mg).
CONCLUSIONS:
These results suggest that PA has significant immunomodulatory properties which probably act by activating mononuclear phagocytic system, augmenting humoral immune response while suppressing cellular immune response.

Front Pharmacol . 2018 Nov 22;9:1347.

Unraveling the Novel Protective Effect of Patchouli Alcohol Against Helicobacter pylori-Induced Gastritis: Insights Into the Molecular Mechanism in vitro and in vivo[Pubmed: 30524287]

Abstract Patchouli alcohol (PA), a natural tricyclic sesquiterpene extracted from Pogostemon cablin (Blanco) Benth. (Labiatae), has been found to exhibit anti-Helicobacter pylori and anti-inflammatory properties. In this study, we investigated the protective effect of PA against H. pylori-induced gastritis in vitro and in vivo, and determined the underlying mechanism. In the in vivo experiment, a C57BL/6 mouse model of gastritis was established using H. pylori SS1, and treatments with standard triple therapy or 5, 10, and 20 mg/kg PA were performed for 2 weeks. Results indicated that PA effectively attenuated oxidative stress by decreasing contents of intracellular reactive oxygen species (ROS) and malonyldialdehyde (MDA), and increasing levels of non-protein sulfhydryl (NP-SH), catalase and glutathione (GSH)/glutathione disulphide (GSSG). Additionally, treatment with PA significantly attenuated the secretions of interleukin 1 beta (IL-1β), keratinocyte chemoattractant and interleukin 6 (IL-6). PA (20 mg/kg) significantly protected the gastric mucosa from H. pylori-induced damage. In the in vitro experiment, GES-1 cells were cocultured with H. pylori NCTC11637 at MOI = 100:1 and treated with different doses of PA (5, 10, and 20 μg/ml). Results indicated that PA not only significantly increased the cell viability and decreased cellular lactate dehydrogenase (LDH) leakage, but also markedly elevated the mitochondrial membrane potential and remarkably attenuated GES-1 cellular apoptosis, thereby protecting gastric epithelial cells against injuries caused by H. pylori. PA also inhibited the secretions of pro-inflammatory factors, such as monocyte chemotactic protein 1 (MCP-1), tumor necrosis factor-α (TNF-α) and IL-6. Furthermore, after PA treatment, the combination of NACHT, LRR, and PYD domains-containing protein 3 (NLRP3) and cysteine-aspartic proteases 1 (CASPASE-1), the expression levels of NLRP3 inflammasome-related proteins, such as thioredoxin-interacting protein (TXNIP), pro-CASPASE-1, cle-CASPASE-1, and NLRP3 and genes (NLRP3 and CASPASE1) were significantly decreased as compared to the model group. In conclusion, treatment with PA for 2 weeks exhibited highly efficient protective effect against H. pylori-induced gastritis and related damages. The underlying mechanism might involve antioxidant activity, inhibition of pro-inflammatory factor and regulation of NLRP3 inflammasome function. PA exerted anti-H. pylori and anti-gastritis effects and thus had the potential to be a promising candidate for treatment of H. pylori-related diseases. Keywords: Helicobacter pylori; gastric epithelial cell; gastritis; inflammasome; oxidative injury; Patchouli alcohol.

Phytother Res. 2015 Jan;29(1):67-72.

Selective antibacterial activity of patchouli alcohol against Helicobacter pylori based on inhibition of urease.[Pubmed: 25243578]

The aim of this study is to evaluate the antibacterial activity and urease inhibitory effects of Patchouli alcohol (PA), the bioactive ingredient isolated from Pogostemonis Herba, which has been widely used for the treatment of gastrointestinal disorders.
METHODS AND RESULTS:
The activities of Patchouli alcohol against selected bacteria and fungi were determined by agar dilution method. It was demonstrated that Patchouli alcohol exhibited selective antibacterial activity against Helicobacter pylori, without influencing the major normal gastrointestinal bacteria. Noticeably, the antibacterial activity of Patchouli alcohol was superior to that of amoxicillin, with minimal inhibition concentration value of 78 µg/mL. On the other hand, Patchouli alcohol inhibited ureases from H.pylori and jack bean in concentration-dependent fashion with IC50 values of 2.67 ± 0.79 mM and 2.99 ± 0.41 mM, respectively. Lineweaver-Burk plots indicated that the type of inhibition was non-competitive against H.pylori urease whereas uncompetitive against jack bean urease. Reactivation of Patchouli alcohol-inactivated urease assay showed DL-dithiothreitol, the thiol reagent, synergistically inactivated urease with Patchouli alcohol instead of enzymatic activity recovery.
CONCLUSIONS:
In conclusion, the selective H.pylori antibacterial activity along with urease inhibitory potential of Patchouli alcohol could make it a possible drug candidate for the treatment of H.pylori infection.

Exp Ther Med. 2011 May;2(3):545-550.

Anti-inflammatory effect of patchouli alcohol isolated from Pogostemonis Herba in LPS-stimulated RAW264.7 macrophages.[Pubmed: 22977538]

Pogostemonis Herba has long been used in traditional Chinese medicine for the treatment of inflammation-related disorders. Patchouli alcohol (PA) isolated from Pogostemonis Herba is a tricyclic sesquiterpene that is known to exert a variety of pharmacological activities.
METHODS AND RESULTS:
The present study aimed to investigate the anti-inflammatory effect of PA on lipopolysaccharide (LPS)-stimulated RAW264.7 cells. Pre-treatment with PA at concentrations of 10, 20 or 40 μM dose-dependently decreased the production of tumor necrosis factor (TNF)-α, interleukin (IL)-1β, IL-6, nitric oxide (NO) and prostaglandin E(2) in LPS-stimulated RAW264.7 cells. In addition, PA treatment also reversed the increased mRNA expression of TNF-α, IL-1β, IL-6, inducible nitric oxide synthase (iNOS) and cyclooxygenase (COX)-2 caused by LPS in RAW264.7 cells.
CONCLUSIONS:
These results indicate that PA is an important anti-inflammatory constituent of Pogostemonis Herba and that its anti-inflammatory effect may be mediated, at least in part, by down-regulation of the mRNA expression of a panel of inflammatory mediators, such as TNF-α, IL-1β, IL-6, iNOS and COX-2.

Eur J Pharm Sci. 2014 Oct 15;63:113-23.

Effects of topical application of patchouli alcohol on the UV-induced skin photoaging in mice.[Pubmed: 25033712]

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.
METHODS AND RESULTS:
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.
CONCLUSIONS:
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.