€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****CARBOHYDRATE RESEARCH***** Aspinall GO Capek P Carpenter RC Gowda DC Szafranek J A novel L-fuco-4-O-methyl-D-glucurono-D-xylan from Hyptis suaveolens. In: Carbohydr Res (1991 Jul 18) 214(1):107-13 ISSN: 0008-6215 The acidic polysaccharide from the seed-coat mucilage of Hyptis suaveolens is a highly branched L-fuco-4-O-methyl-D-glucurono-D-xylan for which a structure is proposed having a 4-linked beta-D-xylan backbone carrying side chains of single 4-O-methyl-alpha-D-glucuronic acid residues at O-2 and 2-O-L-fucopyranosyl-D-xylopyranose units at O-3. The structural analysis involves base-catalyzed beta-elimination of uronic acid residues from the methylated glycan followed by degradation using a modified Svensson oxidation-elimination sequence. Registry Numbers: 136366-18-2 (fuco-4-O-methylglucuronoxylan) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****INTERNATIONAL CONFERENCE ON AIDS***** Miyashiro H Lim JA Nakabayashi T Miyaji M Hattori M Shimotohno K Inhibitory effects of tropical plants on HIV-protease. In: Int Conf AIDS (1994 Aug 7-12) 10(2):112 (abstract no. PA0328) OBJECTIVE: For the purpose of developing new anti-HIV agents from natural sources, various tropical plant extracts were screened for inhibitory effects on HIV-1 protease. METHODS: Various plants and plant materials collected in Sri Lanka and Panama were extracted with water and MeOH to give the respective extracts. Recombinant HIV-1 protease activity was measured by cleavage of a synthetic substrate. RESULTS AND DISCUSSION: The extracts of Areca catechu (seeds), Eugenia jambolana (bark), Saraca indica (bark), Terminalia arjuna (stem bark), Waltheria indica (branch), Erythroxylum citrifolium (trunk), Aegiphila anomala (leaves), Cordia spinescens (leave), Hyptis lantanifolia (aerial part) etc. showed an appreciable inhibition against HIV-1 protease. From the A. catechu extract, some procyanidins were isolated and arecatannin B1 showed a significant HIV-PR inhibitory effect. Since some of these extracts also showed anti-HIV-1 activity, searching for HIV-protease inhibitors in tropical plants is worthy to be considered where effective anti-HIV drugs are really demanded. Registry Numbers: EC 3.4.23.- (HIV Protease) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF ETHNOPHARMACOLOGY***** Rojas A Hernandez L Pereda-Miranda R Mata R Screening for antimicrobial activity of crude drug extracts and pure natural products from Mexican medicinal plants. In: J Ethnopharmacol (1992 Jan) 35(3):275-83 ISSN: 0378-8741 Preliminary antimicrobial screening against Candida albicans and selected Gram-positive and Gram-negative bacteria of methanol extracts prepared from eight Mexican medicinal plants, noted for their antiseptic properties, was conducted. The significant activity exhibited for extracts of Ratibida latipalearis, Teloxys graveolens, Dodonaea viscosa, Hyptis albida, H. pectinata, H. Suaveolens and H. verticillata tends to support their traditional use as anti-infective agents. Only the extract of Hintonia latiflora was inactive. The antimicrobial activities of 44 pure natural compounds and two derivatives were determined. Of these, only 23 compounds were effective in inhibiting the growth of the tested organisms (MIC less than or equal to 100 micrograms/ml). €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF NATURAL PRODUCTS***** Kingston DG Rao MM Zucker WV Plant anticancer agents. IX. Constituents of Hyptis tomentosa. In: J Nat Prod (1979 Sep-Oct) 42(5):496-9 ISSN: 0163-3864 The twigs, leaves, and flowers of Hyptis tomentosa were found to owe their major cytotoxic activity to the presence of desoxypodophyllotoxin (4), but the two weakly cytotoxic flavones 5- hydroxy-4',6,7,8-tetramethoxy flavone (3) and 5-hydroxy-4',3,6,7,8- pentamethoxy flavone (2) also contributed to the total cytotoxicity of the crude extracts. The flavones eupatorin (6) and 5-hydroxy- 3',4',6,7-tetramethoxy flavone (5) were isolated as inactive constituents, together with the lignan sesamin (1). €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Novelo M Cruz JG Hernandez L Pereda-Miranda R Chai H Mar W Pezzuto JM Cytotoxic constituents from Hyptis verticillata. In: J Nat Prod (1993 Oct) 56(10):1728-36 ISSN: 0163-3864 A new cytotoxic (P-388 ED50 4 microgm/ml) arylnaphthalene lignan has been isolated from the Mexican medicinal plant Hyptis verticillata (Lamiaceae) and characterized as 5-methoxydehydropodophyllotoxin [1]. Eight additional lignans were also obtained by bioactivity-directed fractionation using the brine shrimp lethality test. Of these, the dehydro-beta-peltatin methyl ether 2 (P-388 ED50 1.8 microgm/ml) is reported for the first time as a natural product isolate. The other bioactive compounds were identified as dehydropodophyllotoxin [3], deoxydehydropodophyllotoxin [4]. (--)-yatein [5], 4'- demethyldeoxypodophyllotixin [6], isodeoxypodophyllotoxin [7], deoxypicropodophyllin [8], and beta-apopicropodophyllin [9]. Each of these compounds was evaluated against a panel of cell lines comprising a number of human cancer cell types [breast, colon, fibrosarcoma, lung, prostate, KB, and KB-VI (a multi-drug resistant cell line derived from KB)] and murine lymphocytic leukemia (P-388). Lignans 1-4 showed marginal cytotoxic activity against the human cell lines tested. In contrast, compounds 5-9 demonstrated a general nonspecific activity comparable to that of podophyllotoxin [12] (ED50 < 10-2 microgm/ml). In addition, the antimitotic potential of these compounds was determined in the astrocytoma (ASK) assay. Finally, the plant was also shown to contain the flavonoid sideritoflavone (KB ED50 1.6 microgm/ml) and the known pentacyclic triterpenoids ursolic, maslinic, 2 alpha-hydroxyursolic and oleanolic acids. Registry Numbers: 151703-06-9 (5-methoxydehydropodophyllotoxin) 518-28-5 (Podophyllotoxin) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ Pereda-Miranda R Hernandez L Villavicencio MJ Novelo M Ibarra P Chai H Pezzuto JM Structure and stereochemistry of pectinolides A-C, novel antimicrobial and cytotoxic 5,6-dihydro-alpha-pyrones from Hyptis pectinata. In: J Nat Prod (1993 Apr) 56(4):583-93 ISSN: 0163-3864 By bioactivity-directed fractionation, three new antimicrobial and cytotoxic 5,6-dihydro-alpha-pyrones, pectinolides A-C, have been isolated from Hyptis pectinata (Lamiaceae). The absolute stereochemistry of pectinolide A [1] was established as 6S-[(3S- acetyloxy)-1Z-heptenyl]-5S-(acetyloxy)-5 ,6-dihydro-2H-pyran-2-one, on the basis of spectral, chiroptical, and chemical evidence. The structures of pectinolides B [2] and C [3] were determined as the monodeacetylated forms of 1 by comparison of their spectral data and chemical correlation with the prototype compound. Staphylococcus aureus and Bacillus subtilis were sensitive to pectinolide A [1] in the concentration range of 6.25-12.5 micrograms/ml. Compounds 1-3 exhibited significant cytotoxic activity (ED50 < 4 micrograms/ml) against a variety of tumor cell lines. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****JOURNAL OF PHARMACEUTICAL SCIENCES***** Sheth K Jolad S Wiedhopf R Cole JR TUMOR-INHIBITORY AGENT FROM HYPTIS EMORYI (LABIATAE) In: J Pharm Sci (1972) 61(11):1819 ISSN: 0022-3549 The chloroform extract of the above-ground parts of Hyptis emoryi Torr. (Labiatae) was active against the Walker carcinoma 256 tumor system (5WA16); activity was detected in Sprague rats (36% T/C at 600 mg/kg and 47% T/C at 400 mg/kg). One of two terpene-like compounds isolated from this chloroform extract was the active constituent (15% T/C at 500 mg/kg and 52% T/C at 300 mg/kg) and was identified as betulinic acid. (2 refs) €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****PLANTA MEDICA***** Kuhnt M Probstle A Rimpler H Bauer R Heinrich M Biological and pharmacological activities and further constituents of Hyptis verticillata. In: Planta Med (1995 Jun) 61(3):227-32 ISSN: 0032-0943 Several extracts of Hyptis verticillata and isolated compounds were evaluated for their anti-inflammatory, antibacterial, antisecretory, and cytotoxic properties. The aerial parts yielded (R)-5- hydroxypyrrolidin-2-one and essential oil with the main components alpha-pinene, beta-pinene, and thymol. Spectroscopic methods (UV, IR, 1H-NMR, 13C-NMR, mass, CD) fully characterized (R)-5- hydroxypyrrolidin-2-one, as it was isolated by a bioassay guided fractionation. The essential oil, (R)-5-hydroxypyrrolidin-2-one, as well as the previously isolated rosmarinic acid and dehydropodophyllotoxine contributed to the antibacterial effects of H. verticillata. Furthermore, rosmarinic acid showed significant capillary stabilizing effects. Sideritoflavone inhibited prostaglandin synthase to a significant extent and had antisecretory effects comparable to those of NPPB. The cytotoxicity of the aqueous extract, as demonstrated using KB and HT 29 cell lines, may be of toxicological relevance in cases of internal application. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€ *****REVISTA DO INSTITUTO DE ANTIBIOTICOS, UNIVERSIDADE FEDERAL DE***** De Araujo MD Cavalcanti MD De Mello JF D'Albuquerque IL De Lima OG Monache FD Maciel GM [Antimicrobial substances of superior plants. 45. Primary observations of 2 new quinoids isolated from Hyptis fructicosa Salzm ex Benth(Labiatae)] Substancias antimicrobianas de plantas superiores. Communicac~ao XLV. Primeiras observac~oes sobre dois novos quinonoides isolados de Hyptis fructicosa Salzm ex Benth. (Labiatae) In: Rev Inst Antibiot (Recife) (1974 Dec) 14(1-2):101-4 ISSN: 0080-0228 (Published in Portuguese) The authors present the first observations on the isolation of two quinonoid compounds from Hyptis fructicosa Salzm ex Benth; Labiatae. The referred naturally compounds present antimicrobial and antineoplastic activity against Gram-positive microrganisms and mouse Erlich carcionama, respectivelly. €€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€€