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Mucositis is the oxidation and inflammation of mucosal tissues. Transmucosal delivery can be applicable with herbal plant extracts providing anti-inflammatory activity. Thus, this research aimed to formulate an anti-inflammatory remedy from extracts obtained from the Indian gooseberry (IGB) and sappanwood heartwood (SPW) for encapsulation as mucus-penetrating nanovesicles. A suitable method was determined by maximizing antioxidant activity (AOA) and total phenolic content (TPC); the synergistic recipe was AOA and anti-inflammatory activity (AIA). The niosomal suspensions prepared by the ethanol injection method were optimized with the goal of high encapsulation efficiency and small particle size. The mucus-penetrating property was assessed by using modified Franz diffusion cells. Soxhlet extraction was the most suitable method for preparing effective extracts that could rapidly provide a high extraction yield without hindering AOA and TPC. IGB and SPW were effective in AOA and AIA, respectively. Thus, an increase in SPW in the remedies raised AIA but not AOA. Despite a synergism in the AOA of all recipes, the AIA was specifically synergistic in herbal remedy 1 (HR1). It could diminish the cytotoxic effect of SPW. The niosomal suspensions containing Span60, Tween80, and cholesterol could provide nanoparticles with a high encapsulation efficiency and large particle sizes, in which the incorporation of poloxamer 407 caused a decrease in mucus penetration upon altering the diffusion mechanism. This research pioneered the utilization of the recipe formulated from IGB and SPW. The novel anti-inflammatory recipe developed with mucus-penetrating drug delivery is applicable for treating mucositis. [Display omitted] • Soxhlet extraction rapidly enriched yields of IGB and SPW without hindering antioxidant activity. • IGB was powerful in antioxidant activity and SPW was effective in anti-inflammatory activity. • IGB and SPW could be synergistically mixed as an anti-inflammatory recipe with lower cytotoxicity. • TW80 ameliorated encapsulation efficiency and size of SP60-based niosomes containing P407. • P407 improved mucus-penetrating property of niosomes by altering the diffusion mechanism. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance The rhizomes of Dioscorea membrancea Pierre have been used in Thai traditional medicine as an ingredient formula for liver cancer and cholangiocarcinoma treatment. Aim of the study To investigate the cytotoxic activity of ethanolic extract and constituents of D. membrancea to support its traditional use. Materials and methods The SRB assay was used to determine the cytotoxic activity against hepatocellular carcinoma (HepG2), cholangiocarcinoma (KKU-M156) cells and one normal human keratinocyte immortal cells (HaCaT) with its ethanolic extract and isolated compounds. Bioassay guided isolation was used for isolating cytotoxic compounds. Results The ethanolic extract of D . membranacea rhizome showed weak cytotoxic against KKU-M156 and HepG2 (IC 50 at 72 h exposure=30.49±0.82 and 38.97±2.04 µg/mL respectively). A new steroid [epipanthogenin B ( 1 )], a known steroid [panthogenin B ( 2 )], two napthofuranoxepins [dioscorealide A ( 3 ) and dioscorealide B ( 4 )], phenanthraquinone [dioscoreanone ( 5 )] and two phenanthrene [5,6-dihydroxy-2,4-dimethoxy-9,10-dihydrophenanthrene ( 6 ) and 2,5,6-trihydroxy-3,4-dimethoxy, 9, 10-dihydrophenanthrene ( 7 )] were isolated from active chloroform fraction. Compound 4 showed the highest cytotoxicity against HepG2 (IC 50 at 72 h exposure=2.87±0.21 µM) and KKU-M156 (IC 50 at 72 h exposure=1.67±0.10 µM) and less toxicity against normal cell line (HaCaT) (IC 50 at 72 h exposure>100 µM). Compound 5 showed selective cytotoxic activity against KKU-M156 (IC 50 at 72 h exposure=3.46±0.11 µM). Compounds 6 and 7 showed weak cytotoxic activity against HepG2 (IC 50 at 72 h exposure=24.96±2.32 and 51.31±3.52 µM). Compounds ( 1 – 3 ) showed no cytotoxic activity against HepG2 and KKU-M156 cell lines (IC 50 at 72 h exposure>100 µM). Conclusion Seven compounds were isolated from active chloroform fraction of the ethanolic extract of D . membranacea rhizomes. Only dioscorealide B ( 4 ) might be served as a good anticancer agent for liver cancer and cholangiocarcinoma cancer because it can kill cancer cell but not toxic on normal cell. This research support Thai traditional medicine use of D. membranacea for liver cancer and cholangiocarcinoma cancer treatment. [ABSTRACT FROM AUTHOR]

Ethnopharmacological relevance The rhizomes of Dioscorea membranacea Pierre (DM) have been used as ingredients in anticancer herbal formulations in Thai traditional medicine (TTM). Thus, the aim of this study was to investigate the active constituents of DM for cytotoxic activity in order to support its TTM use. Materials and methods A bioassay-guided isolation procedure was used to separate the cytotoxic constituents from ethanolic extract of Dioscorea membranacea rhizomes by testing against five human cancer cell lines, i.e. large cell lung carcinoma, COR-L23; liver cancer cells, HepG2; prostate cancer cells, PC3; breast cancer cells MCF-7; cervical cancer cells, Hela; and one normal human lung cell line (MRC 5) using the SRB assay. Results Two known dihydrophenanthrene compounds [2,4 dimethoxy-5,6-dihydroxy-9,10-dihydrophenanthrene ( 1 ) and 5-hydroxy-2,4,6-trimethoxy-9,10-dihydrophenanthrene ( 2 )], and a new dihydrophenanthrene compound, 5,6,2 -trihydroxy 3,4-methoxy, 9,10-dihydrophenanthrene ( 3 ) were isolated and fully characterized. 1 showed the highest cytotoxic activity against COR-L23, MCF-7 and PC3 cell lines (IC 50 =14.89, 17.49 and 19.04 µM, respectively), and 2 showed selective cytotoxic activity against PC3 (IC 50 =23.54 µM). The new compound 3 showed selective cytotoxic activity against only MCF-7 cells (IC 50 =31.41 µM). Interestingly the crude extract of DM was much less toxic to the normal cell line (MRC-5) (IC 50 >50 µg/ml) compared to the five cancer cell lines, (IC 50 value ranged between 6 and 29 µg/ml). Conclusion The phytochemicals isolated from DM may serve as lead compounds for the design of new anti-cancer agents with better selective cytotoxic indices. [ABSTRACT FROM AUTHOR]

Prasachandaeng (PSD) remedy from the Thailand National List of Essential Medicines (NLEM) has been used as an antipyretic for chronic fever in both adults and children for centuries. Its therapeutic effect in treating fever and its safety have not been studied in animal models. We evaluated its antipyretic activity on lipopolysaccharide (LPS)-induced fever and safety in the liver in comparison with acetaminophen (ACP). Correlation between biochemistry of liver function and the level of cytochrome P450 (CYP2E1) was also evaluated using an ELISA kit. All doses of PSD powder (PSDP) and a 95% ethanol extract of PSD (PSDE) (50, 200, and 400 mg/kg) showed a significant antipyretic effect (* p < 0.05) as compared to ACP. We investigated clinical biochemistry of liver and kidney functions, histopathology, and concentrations of CYP2E1. All treatment groups demonstrated a normal range of clinical biochemistry of liver and kidney functions in comparison with ACP on days 1, 3, 7, and 10. Serum AST, ALP, and LDH levels of PSDE and PSDP showed mean values less than that of ACP on the corresponding days (* p < 0.05). None of the treatment groups showed evidence of hepatocellular damage, nor did they affect CYPE21. The results of histopathology on liver tissue correlated with the biochemistry of liver functions which indicated no hepatotoxicity effect in liver tissue during the seven day treatment. These findings suggest that both forms of PSD remedy possessed marked antipyretic activity and were not hepatotoxic during the seven days of administration in rats. [Display omitted] • Investigation of antipyretic efficacy and safety of Prasachandaeng remedy. • All doses of PSDE and PSDP were found to have antipyretic activity similar to acetaminophen. • Acetaminophen (150 mg/kg b.w.), PSDE (50 mg/kg b.w.) and PSDP (400 mg/kg b.w.) did not show hepatotoxicity. • These findings indicated that both forms of PSD remedy possessed marked antipyretic activity and lack of hepatotoxicity over seven days of oral administration in rats. • These are the first evidence-based experimental data of pharmacological efficacy of an antipyretic drug from NLEM. [ABSTRACT FROM AUTHOR]

Abstract: An investigation of the chemical constituents in a dichloromethnae extract of Goniothalamus undulatus root led to the isolation of three known styryl lactones (5-acetoxyisogoniothalamin oxide, O-acetylaltholactone and altholactone), and four known annonaceous acetogenins (annonacin, cis-annonacin, goniothalamicin and cis-goniothalamicin). These compounds were subjected to a sulphorhodamine B (SRB) cytotoxicity assay against human large cell lung carcinoma (COR-L23), and normal human fetal fibroblast (MRC-5), cell lines. The isolated acetogenins showed higher cytotoxic activity against COR-L23 compared to the styryl lactones, with IC50 values in the range of 0.5–1.7μM and 7.4–15.4μM, respectively. A similar pattern of cytotoxicity was also observed against the other cell line (MRC-5); acetogenins IC50 values were in the range of 11.8–31.4μM, and those for styryl lactones were in the range of 48.7–102.8μM. This is the first report of a bioassay-guided isolation of chemical constituents from G. undulatus and on cytotoxic studies of the isolated compounds using these particular lung cancer cell lines. [Copyright &y& Elsevier]

Background: Skew deviation is an acquired vertical ocular misalignment caused by damage to the prenuclear vestibular inputs to the ocular motor nuclei. A-pattern strabismus often has bilaterally symmetric vertical incomitance and overdepression in adduction (superior oblique overaction) and can be associated with developmental delay, cerebral palsy, hydrocephalus, spina bifida, or posterior fossa or other brainstem disease. The purpose of this study is to describe the ocular motility and torsion findings in patients with A-pattern strabismus and bilateral overdepression in adduction (superior oblique muscle overaction) and to propose a possible brainstem mechanism underlying these observations. Results: Most of the 13 patients identified had other neurologic abnormalities, including spina bifida, hydrocephalus, perinatal stroke, or global delay. Only 2 patients had vertical ocular misalignment in primary gaze. Of the 13, 7 had incomitant vertical tropias during lateral gaze, and 12 had bilateral incyclotorsion documented on fundus examination. Despite having bilateral overdepression in adduction (superior oblique overaction), 11 of the 13 had no difference in vertical ocular misalignment with alternating head tilt rather than reversing hypotropias as would be expected from primary oblique dysfunction. The findings are consistent with damage to the utricular pathways corresponding to the anterior semicircular canal and a resulting posterior canal predominance to the extraocular muscle subnuclei that creates increased tonus to the depressors, bilaterally. Conclusions: A-pattern strabismus may, in some cases, represent a special form of skew deviation. The ocular motility and clinical findings are consistent with bilateral damage to the utricular pathways corresponding to the anterior semicircular canals rather than bilateral primary superior oblique muscle overaction.▪ [Copyright &y& Elsevier]

Abstract: Thai medicinal plants locally known as Hua-Khao-Yen were examined for their inhibitory activities against lipopolysaccharide (LPS) induced nitric oxide (NO) production in RAW 264.7 cell lines. Among the plant species studied, an ethanolic extract of Dioscorea membranacea exhibited the most potent inhibitory activity, with an IC50 value of 23.6μg/ml. From this extract, eight compounds [two naphthofuranoxepins (1, 2), one phenanthraquinone (3), three steroids (4–6) and two steroidal saponins (7, 8)] were isolated and further investigated for their inhibitory properties of NO production. It was found that diosgenin-3-O-α-l-rhamnosyl (1→2)-β-d-glucopyranoside (7) possessed the highest activity (IC50 =3.5μM), followed by dioscoreanone (3, IC50 =9.8μM) and dioscorealide B (2, IC50 =24.9μM). Regarding structural requirements of diosgenin derivatives for NO production inhibitory activity, compound 7 which has a rhamnoglucosyl moiety at C-3 exhibited much higher activity than compounds that have either a diglucosyl substitution (8) or its aglycone (9); whereas, hydroxyl substitution at position 8 of naphthofuranoxepin derivatives conferred higher activity than the methoxyl group. It is concluded that diosgenin-3-O-α-l-rhamnosyl (1→2)-β-d-glucopyranoside (7), dioscoreanone (3) and dioscorealide B (2) are active principles for NO inhibitory activity of Dioscorea membranacea. Compounds 1–3 were also tested for the inhibitory effect on LPS-induced TNF-α release in RAW 264.7 cells. The result revealed that 3 possessed potent activity against TNF-α release with an IC50 value of 17.6μM, whereas, 1 and 2 exhibited mild activity. The present study may support the use of Dioscorea membranacea by Thai traditional doctors for treatment of the inflammatory diseases. [Copyright &y& Elsevier]

Abstract: Extracts of five species of Thai medicinal plants, locally known as Hua-Khao-Yen, were screened for anti-allergic activities using RBL-2H3 cells. Of the five species studied, the ethanolic extract of Dioscorea membranacea exhibited potent inhibitory activity against β-hexosaminidase release as a marker of degranulation in RBL-2H3 cells, with an IC50 value of 37.5μg/mL. Eight compounds were isolated from this crude ethanolic extract, [two naphthofuranoxepins (1, 2), one phenanthraquinone (3), three steroids (4–6), and two steroidal saponins (7, 8)], and tested for their anti-allergic activities. The results showed that dioscorealide B (2) possessed the highest activity with an IC50 value of 5.7μM, followed by dioscoreanone (3, IC50 =7.7μM), dioscorealide A (1, IC50 =27.9μM), and diosgenin (9, IC50 =29.9μM). Structure–activity relationship studies of naphthofuranoxepins on anti-allergic activity revealed that the hydroxylation at position 8 conferred higher activity than methoxylation. For diosgenin derivatives, the aglycone was found to possess higher activity than the diglucosylated molecule; whereas substitution with rhamnoglucosides apparently results in loss of activity. Furthermore, effects of dioscorealide A, dioscorealide B, and dioscoreanone on antigen-induced release of TNF-α and IL-4 in the late phase reaction were also examined. [Copyright &y& Elsevier]

Abstract: Ethanolic- and water extracts from five species of Thai medicinal plants known as Hua-Khao-Yen were tested for their inhibitory effects against HIV-1 protease (HIV-PR) and HIV-1 integrase (HIV-1 IN). The result revealed that the ethanolic (EtOH) extract of Smilax corbularia exhibited anti-HIV-1 IN activity with an IC50 value of 1.9μg/ml, followed by the water extract of Dioscorea birmanica (IC50 =4.5μg/ml), the EtOH extract of Dioscorea birmanica (IC50 =4.7μg/ml), the water extract of Smilax corbularia (IC50 =5.4μg/ml), the EtOH extract of Smilax glabra (IC50 =6.7μg/ml) and the water extract of Smilax glabra (IC50 =8.5μg/ml). The extracts of Pygmaeopremna herbacea and Dioscorea membranacea were apparently inactive (IC50 >100μg/ml). Interestingly, only the EtOH extract of Dioscorea membranacea showed appreciable activity (IC50 =48μg/ml) against HIV-1 PR, while the other extracts possessed mild activity. This result strongly supported the basis for the use of Smilax corbularia and Dioscorea membranacea for AIDS treatment by Thai traditional doctors. [Copyright &y& Elsevier]

The SRB assay was used to test cytotoxicity against three human cancer cell lines and one normal cell line of 11 Thai medicinal plant species used by traditional doctors in treating cancer patients. The extraction procedures used were similar to those practised by Thai traditional doctors (ethanolic and water extracts). Extracts were tested against the human large cell lung carcinoma cell line COR-L23, the human breast adenocarcinoma cell line MCF-7 and human colon adenocarcinoma cell line LS-174T and normal human keratinocytes SVK-14. The results showed that three plants; Dioscorea membranacea Pierre ex Prain & Burkill, Dioscorea birmanica Prain & Burkill (Dioscoreaceae) and Siphonodon celastrineus Griff. (Celastraceae), exhibited high cytotoxic activity showing a certain degree of selectivity against the different cell types. [Copyright &y& Elsevier]

Benjakul (BJK), a Thai traditional medicine preparation, has long been used for balanced health, controlled abnormal of element in the body, carminative, and relief of flatulence. It is composed of five plants: Piper interruptum Opiz., Piper longum L., Piper sarmentosum Roxb., Plumbago indica L., and Zingiber officinale Roscoe. The ethanolic extracts of BJK, its five individual plants, and pure constituents of BJK were investigated for their anti-allergic activity using immunoglobulin E (IgE)-sensitized β-hexosaminidase in the rat basophilic leukemia-2H3 (RBL-2H3) cells and anti-inflammatory activity using lipopolysaccharide (LPS)-induced nitric oxide (NO) and tumor necrosis factor-alpha (TNF-α) in the murine macrophage (RAW 264.7) cells. The ethanolic extracts of BJK showed anti-allergic activity (IC 50 = 12.69 μg/ml) and exhibited potent NO inhibitory effect (IC 50 = 16.60 μg/ml), but inactive on TNF-α release. Moreover, 6-shogaol and plumbagin, two pure compounds from BJK, showed higher anti-allergic activity than the ethanolic BJK extract with IC 50 values of 0.28 and 4.03 μg/ml, respectively. These compounds were significantly higher than chlorpheniramine (CPM), standard drug, with IC 50 value of 17.98 μg/ml. Determination of the anti-inflammatory activity by measuring the inhibition of NO production presented that plumbagin and 6-shogaol exhibited higher than crude BJK extract with IC 50 values of 0.002 and 0.92 μg/ml, respectively. In particular, plumbagin also showed higher anti-inflammatory than prednisolone, positive control, with IC 50 value of 0.59 μg/ml. 6-Shogaol also showed inhibitory effect on TNF-α release (IC 50 = 9.16 μg/ml). These preliminary results may provide some scientific support for the use of BJK for the anti-allergic treatment and inflammatory disorders through the inhibition of NO production. [ABSTRACT FROM AUTHOR]

Abstract: Free radical-induced vascular dysfunction plays a key role in the pathogenesis of vascular disease found in chronic diabetic patients. Morus alba (MA) leaf extract is promoted for good health especially in diabetic patients. Interestingly, antidiabetic and antioxidant activities of MA have been reported in experimental animals. Thus, the hypothesis of this study was that the long-term treatment with MA could improve vascular reactivity of chronic diabetic rats. To test this hypothesis, we examined the effect of long-term treatment with MA on the vascular responses to vasoactive agents in streptozotocin-induced chronic diabetic rats. The diabetic rats were either orally administered with distilled water, MA (0.25, 0.5 and 1 g/kg per day) or subcutaneously injected with insulin (4 U/kg per day) for 8 weeks. After each treatment, the fasting blood glucose, blood pressure, vascular responses to vasoactive agents and tissue malondialdehyde were examined. Morus alba at the doses of 0.5 and 1 g/kg, which significantly reduced blood glucose level, also significantly decreased the high blood pressure in diabetic rats. Vascular responses of the chronic diabetic rats to vasodilators, acetylcholine (3-30 nmol/kg) and sodium nitroprusside (1-10 nmol/kg) were significantly suppressed by 26% to 44% and 45% to 77% respectively, whereas those to vasoconstrictor, phenylephrine (0.01-0.1 μmol/kg) were significantly increased by 23% to 38% as compared to normal rats. Interestingly, the administration of 0.5 and 1 g/kg MA or 4 U/kg insulin significantly restored the vascular reactivities of diabetic rats. Moreover, 8 weeks of diabetes resulted in the elevation of malondialdehyde content in tissues (liver, kidney, heart, and aorta), and MA treatment significantly lessened this increase. These results provide the first evidence for the efficacy of MA in restoring the vascular reactivity of diabetic rats, the mechanism of which may associate with the alleviation of oxidative stress. [Copyright &y& Elsevier]

The leaves of Acanthus ebracteatus, stembark of Oroxylum indicum and the stems of Cryptolepis buchanani and Derris scandens are used as traditional remedies in Thailand for arthritis. Aqueous and alcoholic extracts were tested using three different in vitro systems for effects relevant to anti-inflammatory activity. The aqueous extracts of O. indicum and D. scandens significantly reduced myeloperoxide release. Eicosanoid production was reduced only by the aqueous extracts of A. ebracteatus and D. scandens. D. scandens extract showed potent inhibitory activity against generation of leukotriene B4 and also displayed antioxidant activity. In the rat hind paw edema test, D. scandens extract showed significant activity when given intraperitoneally but did not produce a significant reduction when given orally. The results therefore supported to some extent the traditional use of D. scandens for arthritic conditions and provided slight indication of activity which could explain the use of O. indicum and A. ebracteatus. No relevant activity was demonstrated in any of the tests for C. buchanani extracts. [Copyright &y& Elsevier]