Anti-allergic activity of some selected plants in the genus Boesenbergia and Kaempferia

Ethanolic and water extracts from the rhizomes of eight selected Zingiberaceous plants, including Boesenbergiathorelii, Boesenbergia sp 1, Boesenbergia sp 2, Boesenbergia sp 3, Kaempferia angustifolia, Kaempferia marginata,Kaempferia rotunda and Kaempferia sp were tested for their anti-allergic activities using the rat basophilic leukemia strain2H3 (RBL-2H3) cell line. Both the ethanolic (EtOH) and water extracts of Boesenbergia thorelii exhibited the most potentanti-allergic effects against antigen-induced â-hexosaminidase release as a marker of degranulation in RBL-2H3 cells, withIC50 values of 23.0 and 26.3 g/ml, respectively. Other extracts also had some activity from Boesenbergia sp 2 (EtOH, IC50 =38.3 g/ml), Kaempferia marginata (water, IC50 = 38.4 g/ml), Boesenbergia sp 3 (EtOH, IC50 = 49.4 g/ml) and Kaempferiaangustifolia (water, IC50 = 55.6 g/ml), whereas other Boesenbergia and Kaempferia spp had little or no activity. These findingssupport the use of Boesenbergia thorelii for the treatment of allergies and allergy-related diseases

A Screening strategy for selection of Anti-HIV-1 Integrase and anti-HIV-1 Protease Inhibitors from extracts of Indian Medicinal plants

Ethanolic and water extracts from six species of Indian medicinal plants mainly distributed in the region of Western Ghats, India such as Morinda citrifolia (leaf), Garcinia indica (leaf), Garcinia cambogia (leaf), Salacia oblonga (leaf), Coccinium fenestratum (stem bark) and Calophyllum inophyllum (bark) were tested for their inhibitory activities against two prime enzymes of HIV which are HIV-1 protease (HIV-PR) and HIV-1 integrase (HIV-IN). The results revealed that the ethanolic and water extract of the bark extract of Calophyllum inophyllum exhibited potent anti-HIV-IN activity with IC50 values of 9.8 and 5.6 μg/ml, respectively. Whereas  those for anti-HIV-1 PR effect were found to be 63.8 and 16.3 μg/ml, respectively.  This result strongly supports the basis for the use of C. inophyllum for AIDS treatment by local traditional practitioners of Ayurveda and Unani system of Indian medicine and it is the first report on HIV-1 Protease and HIV-1 Integrase enzyme inhibition by this plant extract

Plumbagin production by root cultures of Plumbago rosea

Root cultures of Plumbago rosea Linn. were established from young leaf explants on solid Gamborg's B5 (B5) medium supplemented with the combination of \u3b1-naphthalene acetic acid (NAA) and kinetin in the concentration ranges of 0.5-2.0 mg/l and 0.1-0.5 mg/l, respectively. The production of plumbagin, determined by TLC-densitometry was higher [0.016 \ub1 0.0030% dry weight (DW)] in cultured roots obtained from B5 medium supplemented with 1.0 mg/l NAA and 0.1 mg/l kinetin. Plant selection increased the plumbagin production to 0.129 \ub1 0.0139% DW, while variation of sucrose and nitrogen (as (NH4)2SO4) concentration in B5 media slightly increase the plumbagin synthesis to 0.023 \ub1 0.0017 and 0.020 \ub1 0.0015% DW, respectively

Anti-cancer activity of compounds from Cassia garrettiana heartwood

The ethanol extract of Cassia garrettiana heartwood showed marked inhibitory activity against several cancer cell lines including HT-29, HeLa, MCF-7 and KB cells. Therefore, its extract and compounds were investigated for their anticancer effect using the Sulforhodamine B (SRB) assay. The ethanol extract of C. garrettiana heartwood was separated to give five compounds which are chrysophanol (1), piceatannol (2), aloe-emodin (3), emodin (4) and cassigarol E (5). Of the tested samples, chrysophanol (1) showed the highest anti-cancer activity against KB cells (IC50 = 0.045 g/mL), aloe emodin (3) was the most active against HT-29 (IC50 = 0.29 g/mL), emodin (4) was against HeLa cells (IC50 = 0.82 g/mL), and cassigarol E (5) was active against MCF-7 (IC50 = 0.021 g/mL), whereas piceatannol (2) was inactive in all tested cell lines. This is the first report of anti-cancer effect against HT-29, HeLa, MCF-7 and KB cells of C. garrettiana heartwood

Inhibitory activities of Thai medicinal plants against herpes simplex type 1, poliovirus type 1, and measles virus

Forty-eight ethanol- and 43 water-extracts of 49 traditional Thai medicines were evaluated for antiviral activities by a plaque reduction assay. For preliminary characterization of the mode of their antiviral action, poliovirus type 1, measles virus and herpes simplex virus type 1 (HSV-1) that are different in nucleic acid component and enveloped structure were used in this study. Fifty-two, 28 and 29 extracts exhibited inhibitory activities against poliovirus, measles virus and HSV-1, respectively. Of 29 extracts with anti-HSV-1 activities, the inhibitory activities of Rhinacanthus nasutus (leaf), Terminalia citrina (fruit) and Thevetia peruviana (leaf) were observed in both ethanol and water extracts. The ethanol extracts of Derris scandens (leaf) and Plumbago indica (leaf) and the water extract of Capsicum frutescens (fruit) were active against only HSV-1, suggesting the mechanism of their antiviral action likely unique to HSV-1 but neither poliovirus nor measles virus. Contrarily, 26 extracts displayed inhibitory activities against poliovirus and/or measles virus. These findings suggest that the 29 extracts from traditional Thai medicines are potential candidates for anti-HSV agents. 49種のタイ伝統薬物から作製した48のエタノールエキス,43の水エキスに対する抗ウイルス活性をプラーク減少法で検索した。本研究では,核酸やエンベロープ構造の異なるポリオウイルス1型,麻疹ウイルス,単純ヘルペスウイルス1型に対して検討を行なった。その結果ポリオウイルス1型に対しては52種,麻疹ウイルスには28種,単純ヘルペスウイルス1型には29種のエキスが阻害活性を示した。単純ヘルペス1型に有効であった29種の中では,Rhinacanthus nasutus(葉),Terminalia citrina(果実),Thevetia peruviana(葉)はエタノール,水の両エキスで阻害作用を示した。Derris scandens(葉),Plumbago indica(葉)およびCapsicum frutescens(果実)のエタノールエキスは単純ヘルペスウイルス1型にのみ活性があった。このことはポリオウイルスや麻疹ウイルスには無効で,単純ヘルペス1型のみに特異的に有効であることを示唆している。一方,26種のエキスはポリオウイルスあるいは麻疹ウイルス,また両方に有効であった。これらの結果はタイ伝統薬物からの29のエキスが抗ヘルペス剤として有力な候補となることを示している

Inhibitory effects of flavonoids on human immunodeficiency virus type-I integrase

One hundred and eighty-three flavonoids were screened for their inhibitory effects on HIV-l integrase (IN) using a multiplate integration assay (MIA). Of the tested flavonoids, 6-hydroxyluteolin, scutellarein, pedalitin, scutellarin, baicalein dimer, hypolaetin, 7-O-benzyl-6-hydroxyluteolin and baicalein showed appreciable inhibition with IC_ values of 0.4, 0.6, 1.3, 1.7, 2.0, 2.1, 3.0 and 3.6 μM, respectively. The potent inhibition was observed with flavonoids having at least one pair of vicinal hydroxyl groups and the activity was highly dependent on the number of vicinal hydroxyl groups. On the other hand, the inhibitory activity tended to be decreased by replacing a hydroxyl group with one of methoxyl, acetoxyl, isopropoxyl, isopentenyl, benzyloxyl, glucuronyl and glycosyl groups. No flavanones, flavanonols and chalcones examined in this experiment showed any significant inhibitory activity. マルチプレートインテグレーション法を用いて183種のフラボノイド類のHIV-1インテグラーゼ阻害効果を検討した。これらのうち6-hydroxyluteolin, scutellarein, pedalitin, scutellarin, baicalein二量体,hypolaetin,7-O-benzyl-6-hydroxyluteolinおよびbaicaleinは強い阻害を示し,それらの50%阻害濃度はそれぞれ0.4, 0.6, 1.3, 1.7, 2.0 ,2.1 ,3.0および3.6μMであった。フラボノイド類による阻害には少なくとも一対の隣接したヒドロキシル基が必要であった。また,隣接したヒドロキシル基の数が増加するに従い,HIV-1インテダラーゼ阻害活性も上昇した。他方,ヒドロキシル基がmethoxyl基, acetoxyl基, isopropoxyl基, isopentenyl基, benzyloxyl基, glucuronyl基 及びglycosyl基に置換されると阻害活性は減少あるいは消失した。試験したフラバノン,フラバノール,カルコン類には顕著な阻害活性は認められなかった

Antibacterial, Anti-HIV-1 Protease and Cytotoxic Activities of Aqueous Ethanolic Extracts from Combretum Adenogonium Steud. Ex A. Rich (Combretaceae).

\ud \ud Records have shown that Combretum adenogonium Steud. Ex A. Rich (Combretaceae) is used in traditional medicine systems of several tribes in Tanzania. This study focused on the investigation of antibacterial activity, anti-HIV-1 protease activity, toxicity properties and classes of phytochemicals in extracts from C. adenogonium Steud. Ex A. Rich (Combretaceae) to evaluate potential of these extracts for development as herbal remedies. Dried plant material were ground to fine powder and extracted using 80% aqueous ethanol to afford root, leaf and stem bark extracts. The extracts were assayed for anti-HIV-1 protease activities, antibacterial activities using microdilution methods and cytotoxicity using brine shrimps lethality assay. Screening for major phytochemical classes was carried out using standard chemical tests. All extracts exhibited antibacterial activity to at least one of the test bacteria with MIC-values ranging from 0.31-5.0 mg/ml. Two extracts, namely, root and stem bark exhibited anti-HIV-1 PR activity with IC50 values of 24.7 and 26.5 μg/ml, respectively. Stem bark and leaf extracts showed mild toxicity with LC50 values of 65.768 μg/ml and 76.965 μg/ml, respectively, whereas roots were relatively non-toxic (LC50 = 110.042 μg/ml). Phytochemical screening of the extracts indicated presence of flavonoids, terpenoids, alkaloids, tannins, glycosides and saponins. These results provide promising baseline information for the potential development of C. adenogonium extracts in treatment of bacterial and HIV/AIDS-related opportunistic infections

Anti - HIV-1 integrase activity of Thai Medicinal Plants

For the purpose of discovering anti-HIV-1 agents from natural sources, the aqueous and EtOH extracts of eight Thaiplants including Clerodendron indicum (whole plant), Tiliacora triandra (stem), Capparis micracantha (wood), Harrissoniaperforata (wood), Ficus glomerata (wood), Diospyros decandra (wood), Dracaena loureiri (heartwood), and Tinospora crispa (stem) were screened for their inhibitory activities against HIV-1 integrase (IN) using the multiplate integration assay(MIA). Of the EtOH extracts, Ficus glomerata (wood) was the most potent with an IC50 value of 7.8 g/ml; whereas the water extract of Harrisonia perforata (wood) was the most potent aqueous extract with an IC50 value of 2.3 g/ml. The isolation of active principles against HIV-1 IN from Ficus glomerata is now actively pursued